Alan Kozikowski

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Kim Ki Hwan; Gaisina Irina; Gallier Franck; Holzle Denise; Blond Sylvie Y; Mesecar Andrew; Kozikowski Alan P
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors.
Huang Qingqing; Mao Jialin; Wan Baojie; Wang Yuehong; Brun Reto; Franzblau Scott G; Kozikowski Alan P
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
Guo Songpo; Tipparaju Suresh K; Pegan Scott D; Wan Baojie; Mo Shunyan; Orjala Jimmy; Mesecar Andrew D; Franzblau Scott G; Kozikowski Alan P
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents.

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All Publications

2009: Kim Ki Hwan; Gaisina Irina; Gallier Franck; Holzle Denise; Blond Sylvie Y; Mesecar Andrew; Kozikowski Alan P
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors.
Journal of molecular modeling 2009;15(12):1463-79.
2009: Huang Qingqing; Mao Jialin; Wan Baojie; Wang Yuehong; Brun Reto; Franzblau Scott G; Kozikowski Alan P
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
Journal of medicinal chemistry 2009;52(21):6757-67.
2009: Guo Songpo; Tipparaju Suresh K; Pegan Scott D; Wan Baojie; Mo Shunyan; Orjala Jimmy; Mesecar Andrew D; Franzblau Scott G; Kozikowski Alan P
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents.
Bioorganic & medicinal chemistry 2009;17(20):7126-30.
2009: Pieroni Marco; Lilienkampf Annamaria; Wan Baojie; Wang Yuehong; Franzblau Scott G; Kozikowski Alan P
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
Journal of medicinal chemistry 2009;52(20):6287-96.
2009: Valette Héric; Xiao Yingxiang; Peyronneau Marie-Anne; Damont Annelaure; Kozikowski Alan P; Wei Zhi-Liang; Kassiou Michael; Kellar Kenneth J; Dollé Frédéric; Bottlaender Michel
18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboons.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 2009;50(8):1349-55.
2009: Kozikowski Alan P; Eaton J Brek; Bajjuri Krishna Mohan; Chellappan Sheela K; Chen Yihua; Karadi Sudhakar; He Rong; Caldarone Barbara; Manzano Michael; Yuen Po-Wai; Lukas Ronald J
Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression.
ChemMedChem 2009;4(8):1279-91.
2009: Butler Kyle V; He Rong; McLaughlin Kathryn; Vistoli Giulio; Langley Brett; Kozikowski Alan P
Stereoselective HDAC inhibition from cysteine-derived zinc-binding groups.
ChemMedChem 2009;4(8):1292-301.
2009: Kozikowski Alan P; Chen Yihua; Subhasish Tapadar; Lewin Nancy E; Blumberg Peter M; Zhong Zhenyu; D'Annibale Melissa A; Wang Weng-Long; Shen Yong; Langley Brett
Searching for disease modifiers-PKC activation and HDAC inhibition - a dual drug approach to Alzheimer's disease that decreases Abeta production while blocking oxidative stress.
ChemMedChem 2009;4(7):1095-105.
2009: Tapadar Subhasish; He Rong; Luchini Doris N; Billadeau Daniel D; Kozikowski Alan P
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
Bioorganic & medicinal chemistry letters 2009;19(11):3023-6.
2009: Sleiman Sama F; Basso Manuela; Mahishi Lata; Kozikowski Alan P; Donohoe Mary E; Langley Brett; Ratan Rajiv R
Putting the 'HAT' back on survival signalling: the promises and challenges of HDAC inhibition in the treatment of neurological conditions.
Expert opinion on investigational drugs 2009;18(5):573-84.
2009: Chen Yufeng; He Rong; Chen Yihua; D'Annibale Melissa A; Langley Brett; Kozikowski Alan P
Studies of benzamide- and thiol-based histone deacetylase inhibitors in models of oxidative-stress-induced neuronal death: identification of some HDAC3-selective inhibitors.
ChemMedChem 2009;4(5):842-52.
2009: Gaisina Irina N; Gallier Franck; Ougolkov Andrei V; Kim Ki H; Kurome Toru; Guo Songpo; Holzle Denise; Luchini Doris N; Blond Sylvie Y; Billadeau Daniel D; Kozikowski Alan P
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
Journal of medicinal chemistry 2009;52(7):1853-63.
2009: Cho Sung Jin; Jensen Niels H; Kurome Toru; Kadari Sudhakar; Manzano Michael L; Malberg Jessica E; Caldarone Barbara; Roth Bryan L; Kozikowski Alan P
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
Journal of medicinal chemistry 2009;52(7):1885-902.
2009: Lilienkampf Annamaria; Mao Jialin; Wan Baojie; Wang Yuehong; Franzblau Scott G; Kozikowski Alan P
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
Journal of medicinal chemistry 2009;52(7):2109-18.
2009: Tang Hao; Wang Xiang S; Huang Xi-Ping; Roth Bryan L; Butler Kyle V; Kozikowski Alan P; Jung Mira; Tropsha Alexander
Novel inhibitors of human histone deacetylase (HDAC) identified by QSAR modeling of known inhibitors, virtual screening, and experimental validation.
Journal of chemical information and modeling 2009;49(2):461-76.
2009: LaPointe Nichole E; Morfini Gerardo; Pigino Gustavo; Gaisina Irina N; Kozikowski Alan P; Binder Lester I; Brady Scott T
The amino terminus of tau inhibits kinesin-dependent axonal transport: implications for filament toxicity.
Journal of neuroscience research 2009;87(2):440-51.
2009: Chirapu Srinivas Reddy; Pachaiyappan Boobalan; Nural Hikmet F; Cheng Xin; Yuan Hongbin; Lankin David C; Abdul-Hay Samer O; Thatcher Gregory R J; Shen Yong; Kozikowski Alan P; Petukhov Pavel A
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(1):264-74.
2008: Tipparaju Suresh K; Joyasawal Sipak; Pieroni Marco; Kaiser Marcel; Brun Reto; Kozikowski Alan P
In pursuit of natural product leads: synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and its analogues: discovery of N-(2-benzoxazol-2-ylphenyl)benzamides as novel antileishmanial chemotypes.
Journal of medicinal chemistry 2008;51(23):7344-7.
2008: Mao Jialin; Eoh Hyungjin; He Rong; Wang Yuehong; Wan Baojie; Franzblau Scott G; Crick Dean C; Kozikowski Alan P
Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase.
Bioorganic & medicinal chemistry letters 2008;18(19):5320-3.
2008: Yuan Hai; He Rong; Wan Baojie; Wang Yuehong; Pauli Guido F; Franzblau Scott G; Kozikowski Alan P
Modification of the side chain of micromolide, an anti-tuberculosis natural product.
Bioorganic & medicinal chemistry letters 2008;18(19):5311-5.
2008: Dow Geoffrey S; Chen Yufeng; Andrews Katherine T; Caridha Diana; Gerena Lucia; Gettayacamin Montip; Johnson Jacob; Li Qigui; Melendez Victor; Obaldia Nicanor; Tran Thanh N; Kozikowski Alan P
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
Antimicrobial agents and chemotherapy 2008;52(10):3467-77.
2008: Pibiri Fabio; Kozikowski Alan P; Pinna Graziano; Auta James; Kadriu Bashkim; Costa Erminio; Guidotti Alessandro
The combination of huperzine A and imidazenil is an effective strategy to prevent diisopropyl fluorophosphate toxicity in mice.
Proceedings of the National Academy of Sciences of the United States of America 2008;105(37):14169-74.
2008: Tipparaju Suresh K; Mulhearn Debbie C; Klein Gary M; Chen Yufeng; Tapadar Subhasish; Bishop Molly H; Yang Shuo; Chen Juan; Ghassemi Mahmood; Santarsiero Bernard D; Cook James L; Johlfs Mary; Mesecar Andrew D; Johnson Michael E; Kozikowski Alan P
Design and synthesis of aryl ether inhibitors of the Bacillus anthracis enoyl-ACP reductase.
ChemMedChem 2008;3(8):1250-68.
2008: Kozikowski Alan P; Tapadar Subhasish; Luchini Doris N; Kim Ki Hwan; Billadeau Daniel D
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
Journal of medicinal chemistry 2008;51(15):4370-3.
2008: Banerjee Sangeeta R; Foss Catherine A; Castanares Mark; Mease Ronnie C; Byun Youngjoo; Fox James J; Hilton John; Lupold Shawn E; Kozikowski Alan P; Pomper Martin G
Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA).
Journal of medicinal chemistry 2008;51(15):4504-17.
2008: Zhang Bin; West Eric J; Van Ken C; Gurkoff Gene G; Zhou Jia; Zhang Xiu-Mei; Kozikowski Alan P; Lyeth Bruce G
HDAC inhibitor increases histone H3 acetylation and reduces microglia inflammatory response following traumatic brain injury in rats.
Brain research 2008;1226():181-91.
2008: Tipparaju Suresh K; Joyasawal Sipak; Forrester Sara; Mulhearn Debbie C; Pegan Scott; Johnson Michael E; Mesecar Andrew D; Kozikowski Alan P
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.
Bioorganic & medicinal chemistry letters 2008;18(12):3565-9.
2008: Chen Yufeng; Lopez-Sanchez Miriam; Savoy Doris N; Billadeau Daniel D; Dow Geoffrey S; Kozikowski Alan P
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
Journal of medicinal chemistry 2008;51(12):3437-48.
2008: Mease Ronnie C; Dusich Crystal L; Foss Catherine A; Ravert Hayden T; Dannals Robert F; Seidel Jurgen; Prideaux Andrew; Fox James J; Sgouros George; Kozikowski Alan P; Pomper Martin G
N-[N-[(S)-1,3-Dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine, [18F]DCFBC: a new imaging probe for prostate cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 2008;14(10):3036-43.
2008: Kozikowski Alan P; Chen Yufeng; Gaysin Arsen M; Savoy Doris N; Billadeau Daniel D; Kim Ki Hwan
Chemistry, biology, and QSAR studies of substituted biaryl hydroxamates and mercaptoacetamides as HDAC inhibitors-nanomolar-potency inhibitors of pancreatic cancer cell growth.
ChemMedChem 2008;3(3):487-501.
2008: Kozikowski Alan P; Reitz Allen B
Filling the pipeline for neglected diseases: creation of a medicinal chemistry-centric international drug discovery institute [iDDi].
Drug discovery today 2008;13(3-4):97-8.
2008: Guilarte Tomás R; Hammoud Dima A; McGlothan Jennifer L; Caffo Brian S; Foss Catherine A; Kozikowski Alan P; Pomper Martin G
Dysregulation of glutamate carboxypeptidase II in psychiatric disease.
Schizophrenia research 2008;99(1-3):324-32.
2008: Memmott Regan M; Gills Joell J; Hollingshead Melinda; Powers Margaret C; Chen Zhiping; Kemp Bruce; Kozikowski Alan; Dennis Phillip A
Phosphatidylinositol ether lipid analogues induce AMP-activated protein kinase-dependent death in LKB1-mutant non small cell lung cancer cells.
Cancer research 2008;68(2):580-8.
2008: Olszewski Rafal T; Wegorzewska Marta M; Monteiro Ana C; Krolikowski Kristyn A; Zhou Jia; Kozikowski Alan P; Long Katrice; Mastropaolo John; Deutsch Stephen I; Neale Joseph H
Phencyclidine and dizocilpine induced behaviors reduced by N-acetylaspartylglutamate peptidase inhibition via metabotropic glutamate receptors.
Biological psychiatry 2008;63(1):86-91.
2008: Butler Kyle V; Kozikowski Alan P
Chemical origins of isoform selectivity in histone deacetylase inhibitors.
Current pharmaceutical design 2008;14(6):505-28.
2007: Mao Jialin; Wang Yuehong; Wan Baojie; Kozikowski Alan P; Franzblau Scott G
Design, synthesis, and pharmacological evaluation of mefloquine-based ligands as novel antituberculosis agents.
ChemMedChem 2007;2(11):1624-30.
2007: Niemitz Matthias; Laatikainen Reino; Chen Shao-Nong; Kleps Robert; Kozikowski Alan P; Pauli Guido F
Complete (1)H NMR spectral fingerprint of huperzine A.
Magnetic resonance in chemistry : MRC 2007;45(10):878-82.
2007: Gills Joell J; Castillo S Sianna; Zhang Chunyu; Petukhov Pavel A; Memmott Regan M; Hollingshead Melinda; Warfel Noel; Han Jiahuai; Kozikowski Alan P; Dennis Phillip A
Phosphatidylinositol ether lipid analogues that inhibit AKT also independently activate the stress kinase, p38alpha, through MKK3/6-independent and -dependent mechanisms.
The Journal of biological chemistry 2007;282(37):27020-9.
2007: Kozikowski Alan P; Chellappan Sheela K; Xiao Yingxian; Bajjuri Krishna Mohan; Yuan Hongbin; Kellar Kenneth J; Petukhov Pavel A
Chemical medicine: novel 10-substituted cytisine derivatives with increased selectivity for alpha4beta2 nicotinic acetylcholine receptors.
ChemMedChem 2007;2(8):1157-61.
2007: Kozikowski Alan P; Gaisina Irina N; Yuan Hongbin; Petukhov Pavel A; Blond Sylvie Y; Fedolak Allison; Caldarone Barbara; McGonigle Paul
Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. possible new GSK-3beta therapies for bipolar disorders.
Journal of the American Chemical Society 2007;129(26):8328-32.
2007: Kozikowski Alan P; Chen Yufeng; Gaysin Arsen; Chen Bin; D'Annibale Melissa A; Suto Carla M; Langley Brett C
Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies.
Journal of medicinal chemistry 2007;50(13):3054-61.
2007: Mao Jialin; Wan Baojie; Wang Yuehong; Franzblau Scott G; Kozikowski Alan P
HTS, chemical hybridization, and drug design identify a chemically unique antituberculosis agent-coupling serendipity and rational approaches to drug discovery.
ChemMedChem 2007;2(6):811-3.
2007: Tang Lei; Chen Yan; Chen Zili; Blumberg Peter M; Kozikowski Alan P; Wang Zaijie Jim
Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor.
The Journal of pharmacology and experimental therapeutics 2007;321(2):791-8.
2007: Yamamoto Tatsuo; Saito Osamu; Aoe Tomohiko; Bartolozzi Alessandra; Sarva Jayaprakash; Zhou Jia; Kozikowski Alan; Wroblewska Barbara; Bzdega Tomasz; Neale Joseph H
Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats.
The European journal of neuroscience 2007;25(1):147-58.
2007: Kozikowski Alan P; Chellappan Sheela K; Henderson David; Fulton Roger; Giboureau Nicolas; Xiao Yingxian; Wei Zhi-Liang; Guilloteau Denis; Emond Patrick; Dolle Frederic; Kellar Kenneth J; Kassiou Michael
Acetylenic pyridines for use in PET imaging of nicotinic receptors.
ChemMedChem 2007;2(1):54-7.
2006: Xiao Yingxian; Fan Hong; Musachio John L; Wei Zhi-Liang; Chellappan Sheela K; Kozikowski Alan P; Kellar Kenneth J
Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them.
Molecular pharmacology 2006;70(4):1454-60.
2006: Saito Osamu; Aoe Tomohiko; Kozikowski Alan; Sarva Jayaprakash; Neale Joseph H; Yamamoto Tatsuo
Ketamine and N-acetylaspartylglutamate peptidase inhibitor exert analgesia in bone cancer pain.
Canadian journal of anaesthesia = Journal canadien d'anesthésie 2006;53(9):891-8.
2006: Kozikowski Alan P; Roth Bryan; Tropsha Alexander
Why academic drug discovery makes sense.
Science (New York, N.Y.) 2006;313(5791):1235-6.
2006: Jayaprakash Sarva; Iso Yasuyoshi; Wan Baojie; Franzblau Scott G; Kozikowski Alan P
Design, synthesis, and SAR studies of mefloquine-based ligands as potential antituberculosis agents.
ChemMedChem 2006;1(6):593-7.
2006: Micale Nicola; Kozikowski Alan P; Ettari Roberta; Grasso Silvana; Zappalà Maria; Jeong Jong-Jin; Kumar Ajay; Hanspal Manjit; Chishti Athar H
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.
Journal of medicinal chemistry 2006;49(11):3064-7.
2006: Musachio John L; Hong Jinsoo; Ichise Masanori; Seneca Nicholas; Brown Amira K; Liow Jeih-San; Halldin Christer; Innis Robert B; Pike Victor W; He Rong; Zhou Jia; Kozikowski Alan P
Development of new brain imaging agents based upon nocaine-modafinil hybrid monoamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(12):3101-4.
2006: Chellappan Sheela K; Xiao Yingxian; Tueckmantel Werner; Kellar Kenneth J; Kozikowski Alan P
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Journal of medicinal chemistry 2006;49(9):2673-6.
2006: Zhong Chunlong; Zhao Xueren; Van Ken C; Bzdega Tomasz; Smyth Aoife; Zhou Jia; Kozikowski Alan P; Jiang Jiyao; O'Connor William T; Berman Robert F; Neale Joseph H; Lyeth Bruce G
NAAG peptidase inhibitor increases dialysate NAAG and reduces glutamate, aspartate and GABA levels in the dorsal hippocampus following fluid percussion injury in the rat.
Journal of neurochemistry 2006;97(4):1015-25.
2006: Wee Sunmee; Wang Zhixia; He Rong; Zhou Jia; Kozikowski Alan P; Woolverton William L
Role of the increased noradrenergic neurotransmission in drug self-administration.
Drug and alcohol dependence 2006;82(2):151-7.
2006: Mach Ulrich R; Lewin Nancy E; Blumberg Peter M; Kozikowski Alan P
Synthesis and pharmacological evaluation of 8- and 9-substituted benzolactam-v8 derivatives as potent ligands for protein kinase C, a therapeutic target for Alzheimer's disease.
ChemMedChem 2006;1(3):307-14.
2006: Jayaprakash Sarva; Wang Xinning; Heston Warren D; Kozikowski Alan P
Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy.
ChemMedChem 2006;1(3):299-302.
2006: Gills Joell J; Holbeck Susan; Hollingshead Melinda; Hewitt Stephen M; Kozikowski Alan P; Dennis Phillip A
Spectrum of activity and molecular correlates of response to phosphatidylinositol ether lipid analogues, novel lipid-based inhibitors of Akt.
Molecular cancer therapeutics 2006;5(3):713-22.
2006: Kozikowski Alan P; Gaisina Irina N; Petukhov Pavel A; Sridhar Jayalakshmi; King LaShaunda T; Blond Sylvie Y; Duka Tetyana; Rusnak Milan; Sidhu Anita
Highly potent and specific GSK-3beta inhibitors that block tau phosphorylation and decrease alpha-synuclein protein expression in a cellular model of Parkinson's disease.
ChemMedChem 2006;1(2):256-66.
2006: Iso Yasuyoshi; Grajkowska Ewa; Wroblewski Jarda T; Davis Jared; Goeders Nicholas E; Johnson Kenneth M; Sanker Subramaniam; Roth Bryan L; Tueckmantel Werner; Kozikowski Alan P
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Journal of medicinal chemistry 2006;49(3):1080-100.
2006: Kozikowski Alan P; Zhao Lianyun; Zhang Ao; Wang Cheng Z; Flippen-Anderson Judith; Johnson Kenneth M
Structural remodeling of cocaine: design and synthesis of trisubstituted cyclopropanes as selective serotonin reuptake inhibitors.
ChemMedChem 2006;1(1):58-65.
2006: Makarewicz Dorota; Gadamski Roman; Ziembowicz Apolonia; Kozikowski Alan P; Wroblewski Jarda T; Lazarewicz Jerzy W
Neuroprotective effects of the agonist of metabotropic glutamate receptors ABHxD-I in two animal models of cerebral ischaemia.
Resuscitation 2006;68(1):119-26.
2005: Zhou Jia; Neale Joseph H; Pomper Martin G; Kozikowski Alan P
NAAG peptidase inhibitors and their potential for diagnosis and therapy.
Nature reviews. Drug discovery 2005;4(12):1015-26.
2005: He Rong; Kurome Toru; Giberson Kelly M; Johnson Kenneth M; Kozikowski Alan P
Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors.
Journal of medicinal chemistry 2005;48(25):7970-9.
2005: Jung Mira; Kozikowski Alan; Dritschilo Anatoly
Rational design and development of radiation-sensitizing histone deacetylase inhibitors.
Chemistry & biodiversity 2005;2(11):1452-61.
2005: Guilarte Tomás R; McGlothan Jennifer L; Foss Catherine A; Zhou Jia; Heston Warren D; Kozikowski Alan P; Pomper Martin G
Glutamate carboxypeptidase II levels in rodent brain using [125I]DCIT quantitative autoradiography.
Neuroscience letters 2005;387(3):141-4.
2005: Yu Meixiang; Tueckmantel Werner; Wang Xukui; Zhu Aijun; Kozikowski Alan P; Brownell Anna-Liisa
Methoxyphenylethynyl, methoxypyridylethynyl and phenylethynyl derivatives of pyridine: synthesis, radiolabeling and evaluation of new PET ligands for metabotropic glutamate subtype 5 receptors.
Nuclear medicine and biology 2005;32(6):631-40.
2005: Ukairo Okechukwu T; Bondi Corry D; Newman Amy Hauck; Kulkarni Santosh S; Kozikowski Alan P; Pan Stephen; Surratt Christopher K
Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue.
The Journal of pharmacology and experimental therapeutics 2005;314(2):575-83.
2005: Foss Catherine A; Mease Ronnie C; Fan Hong; Wang Yuchuan; Ravert Hayden T; Dannals Robert F; Olszewski Rafal T; Heston Warren D; Kozikowski Alan P; Pomper Martin G
Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 2005;11(11):4022-8.
2005: Yin Yuzhi; Russell Robert G; Dettin Luis E; Bai Renkui; Wei Zhi-Liang; Kozikowski Alan P; Kopelovich Levy; Glazer Robert I
Peroxisome proliferator-activated receptor delta and gamma agonists differentially alter tumor differentiation and progression during mammary carcinogenesis.
Cancer research 2005;65(9):3950-7.
2005: Zhou Jia; Kläss Thomas; Johnson Kenneth M; Giberson Kelly M; Kozikowski Alan P
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Bioorganic & medicinal chemistry letters 2005;15(10):2461-5.
2005: Jung Mira; Velena Alfredo; Chen Bin; Petukhov Pavel A; Kozikowski Alan P; Dritschilo Anatoly
Novel HDAC inhibitors with radiosensitizing properties.
Radiation research 2005;163(5):488-93.
2005: Wei Jingjun; Wu Chunying; Lankin David; Gulrati Anil; Valyi-Nagy Tibor; Cochran Elizabeth; Pike Victor W; Kozikowski Alan; Wang Yanming
Development of novel amyloid imaging agents based upon thioflavin S.
Current Alzheimer research 2005;2(2):109-14.
2005: Wei Zhi-Liang; Xiao Yingxian; Yuan Hongbin; Baydyuk Maryna; Petukhov Pavel A; Musachio John L; Kellar Kenneth J; Kozikowski Alan P
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
Journal of medicinal chemistry 2005;48(6):1721-4.
2005: Chen Bin; Petukhov Pavel A; Jung Mira; Velena Alfredo; Eliseeva Elena; Dritschilo Anatoly; Kozikowski Alan P
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(5):1389-92.
2005: Zhong Chunlong; Zhao Xueren; Sarva Jayaprakash; Kozikowski Alan; Neale Joseph H; Lyeth Bruce G
NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats.
Journal of neurotrauma 2005;22(2):266-76.
2005: Carón Rubén W; Yacoub Adly; Li Min; Zhu Xiaoyu; Mitchell Clint; Hong Young; Hawkins William; Sasazuki Takehiko; Shirasawa Senji; Kozikowski Alan P; Dennis Philip A; Hagan Michael P; Grant Steven; Dent Paul
Activated forms of H-RAS and K-RAS differentially regulate membrane association of PI3K, PDK-1, and AKT and the effect of therapeutic kinase inhibitors on cell survival.
Molecular cancer therapeutics 2005;4(2):257-70.
2004: Wei Zhi-Liang; Petukhov Pavel A; Bizik Fero; Teixeira Joaquim Cabral; Mercola Mark; Volpe Eugene A; Glazer Robert I; Willson Timothy M; Kozikowski Alan P
Isoxazolyl-serine-based agonists of peroxisome proliferator-activated receptor: design, synthesis, and effects on cardiomyocyte differentiation.
Journal of the American Chemical Society 2004;126(51):16714-5.
2004: Micale Nicola; Vairagoundar Rajendran; Yakovlev Alexander G; Kozikowski Alan P
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
Journal of medicinal chemistry 2004;47(26):6455-8.
2004: Yuan Hongbin; Kozikowski Alan P; Petukhov Pavel A
CoMFA study of piperidine analogues of cocaine at the dopamine transporter: exploring the binding mode of the 3 alpha-substituent of the piperidine ring using pharmacophore-based flexible alignment.
Journal of medicinal chemistry 2004;47(25):6137-43.
2004: Zhou Jia; He Rong; Johnson Kenneth M; Ye Yanping; Kozikowski Alan P
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Journal of medicinal chemistry 2004;47(24):5821-4.
2004: Pearce Larry V; Petukhov Pavel A; Szabo Tamas; Kedei Noemi; Bizik Fero; Kozikowski Alan P; Blumberg Peter M
Evodiamine functions as an agonist for the vanilloid receptor TRPV1.
Organic & biomolecular chemistry 2004;2(16):2281-6.
2004: Etcheberrigaray René; Tan Mathew; Dewachter Ilse; Kuipéri Cuno; Van der Auwera Ingrid; Wera Stefaan; Qiao Lixin; Bank Barry; Nelson Thomas J; Kozikowski Alan P; Van Leuven Fred; Alkon Daniel L
Therapeutic effects of PKC activators in Alzheimer's disease transgenic mice.
Proceedings of the National Academy of Sciences of the United States of America 2004;101(30):11141-6.
2004: Yamamoto Tatsuo; Hirasawa Serabi; Wroblewska Barbara; Grajkowska Ewa; Zhou Jia; Kozikowski Alan; Wroblewski Jarda; Neale Joseph H
Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model.
The European journal of neuroscience 2004;20(2):483-94.
2004: Petukhov Pavel A; Zhang Jianrong; Wang Cheng Z; Ye Yan Ping; Johnson Kenneth M; Kozikowski Alan P
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring.
Journal of medicinal chemistry 2004;47(12):3009-18.
2004: Olszewski Rafal T; Bukhari Noreen; Zhou Jia; Kozikowski Alan P; Wroblewski Jarda T; Shamimi-Noori Susan; Wroblewska Barbara; Bzdega Tomasz; Vicini Stefano; Barton Franca B; Neale Joseph H
NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR.
Journal of neurochemistry 2004;89(4):876-85.
2004: Castillo S Sianna; Brognard John; Petukhov Pavel A; Zhang Chunyu; Tsurutani Junji; Granville Courtney A; Li Min; Jung Michael; West Kip A; Gills Joell G; Kozikowski Alan P; Dennis Phillip A
Preferential inhibition of Akt and killing of Akt-dependent cancer cells by rationally designed phosphatidylinositol ether lipid analogues.
Cancer research 2004;64(8):2782-92.
2004: Wei Zhi-Liang; Xiao Yingxian; Kellar Kenneth J; Kozikowski Alan P
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
Bioorganic & medicinal chemistry letters 2004;14(8):1855-8.
2004: Kozikowski Alan P; Zhang Jiazhong; Nan Fajun; Petukhov Pavel A; Grajkowska Ewa; Wroblewski Jarda T; Yamamoto Tatsuo; Bzdega Tomasz; Wroblewska Barbara; Neale Joseph H
Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.
Journal of medicinal chemistry 2004;47(7):1729-38.
2004: Quirante Josefina; Vila Xavier; Bonjoch Josep; Kozikowski Alan P; Johnson Kenneth M
2,3-disubstituted 6-azabicyclo[3.2.1]octanes as novel dopamine transporter inhibitors.
Bioorganic & medicinal chemistry 2004;12(6):1383-91.
2004: Komander David; Kular Gursant S; Schüttelkopf Alexander W; Deak Maria; Prakash K R C; Bain Jennifer; Elliott Matthew; Garrido-Franco Marta; Kozikowski Alan P; Alessi Dario R; van Aalten Daan M F
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.
Structure (London, England : 1993) 2004;12(2):215-26.
2004: Tóth Attila; Blumberg Peter M; Chen Zili; Kozikowski Alan P
Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.
Molecular pharmacology 2004;65(2):282-91.
2003: Wei Zhi-Liang; Xiao Yingxian; George Clifford; Kellar Kenneth J; Kozikowski Alan P
Functionalization of the alicyclic skeleton of epibatidine: synthesis and nicotinic acetylcholine receptor binding affinities of epibatidine analogues.
Organic & biomolecular chemistry 2003;1(22):3878-81.
2003: Wei Zhi-Liang; Kozikowski Alan P
A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta.
The Journal of organic chemistry 2003;68(23):9116-8.
2003: Zhou Jia; Kläss Thomas; Zhang Ao; Johnson Kenneth M; Wang Cheng Z; Ye Yanping; Kozikowski Alan P
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2003;13(20):3565-9.
2003: Quinlivan Mitchell; Mattner Filomena; Papazian Vahan; Zhou Jia; Katsifis Andrew; Emond Patrick; Chalon Sylvie; Kozikowski Alan; Guilloteau Denis; Kassiou Michael
Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter.
Nuclear medicine and biology 2003;30(7):741-6.
2003: Sridhar Jayalakshmi; Wei Zhi-Liang; Nowak Ireneusz; Lewin Nancy E; Ayres Jolene A; Pearce Larry V; Blumberg Peter M; Kozikowski Alan P
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Journal of medicinal chemistry 2003;46(19):4196-204.
2003: Yu Meixiang; Någren Kjell; Chen Y Iris; Livni Elijahu; Elmaleh David; Kozikowski Alan; Wang Xukui; Jokivarsi Kimmo; Brownell Anna-Liisa
Radiolabeling and biodistribution of methyl 2-(methoxycarbonyl)-2-(methylamino) bicyclo[2.1.1] -hexane -5-carboxylate, a potential neuroprotective drug.
Life sciences 2003;73(12):1577-85.
2003: Zhou Jia; Zhang Ao; Kläss Thomas; Johnson Kenneth M; Wang Cheng Z; Ye Yan Ping; Kozikowski Alan P
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.
Journal of medicinal chemistry 2003;46(10):1997-2007.
2003: Meuillet Emmanuelle J; Mahadevan Daruka; Vankayalapati Hariprasad; Berggren Margareta; Williams Ryan; Coon Amy; Kozikowski Alan P; Powis Garth
Specific inhibition of the Akt1 pleckstrin homology domain by D-3-deoxy-phosphatidyl-myo-inositol analogues.
Molecular cancer therapeutics 2003;2(4):389-99.
2003: Kozikowski Alan P; Johnson Kenneth M; Deschaux Olivier; Bandyopadhyay Bidhan C; Araldi Gian Luca; Carmona Gilberto; Munzar Patrik; Smith Miles P; Balster Robert L; Beardsley Patrick M; Tella Srihari R
Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine.
The Journal of pharmacology and experimental therapeutics 2003;305(1):143-50.
2003: Faden Alan I; Fox Gerard B; Di Xiao; Knoblach Susan M; Cernak Ibolja; Mullins Paul; Nikolaeva Maria; Kozikowski Alan P
Neuroprotective and nootropic actions of a novel cyclized dipeptide after controlled cortical impact injury in mice.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 2003;23(3):355-63.
2003: Faden Alan I; Knoblach Susan M; Cernak Ibolja; Fan Lei; Vink Robert; Araldi Gian Luca; Fricke Stanley T; Roth Bryan L; Kozikowski Alan P
Novel diketopiperazine enhances motor and cognitive recovery after traumatic brain injury in rats and shows neuroprotection in vitro and in vivo.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 2003;23(3):342-54.
2003: Wei Zhi-Liang; Petukhov Pavel A; Xiao Yingxian; Tückmantel Werner; George Clifford; Kellar Kenneth J; Kozikowski Alan P
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Journal of medicinal chemistry 2003;46(6):921-4.
2003: Sakamuri Sukumar; Enyedy Istvan J; Zaman Wahiduz A; Tella Srihari R; Kozikowski Alan P; Flippen-Anderson Judith L; Farkas Tivadar; Johnson Kenneth M; Wang Shaomeng
2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors.
Bioorganic & medicinal chemistry 2003;11(6):1123-36.
2003: Kozikowski Alan P; Tückmantel Werner; Böttcher Gesine; Romanczyk Leo J
Studies in polyphenol chemistry and bioactivity. 4.(1) Synthesis of trimeric, tetrameric, pentameric, and higher oligomeric epicatechin-derived procyanidins having all-4beta,8-interflavan connectivity and their inhibition of cancer cell growth through cell cycle arrest.
The Journal of organic chemistry 2003;68(5):1641-58.
2003: Kozikowski Alan P; Sun Haiying; Brognard John; Dennis Phillip A
Novel PI analogues selectively block activation of the pro-survival serine/threonine kinase Akt.
Journal of the American Chemical Society 2003;125(5):1144-5.
2003: Kozikowski Alan P; Nowak Ireneusz; Petukhov Pavel A; Etcheberrigaray Rene; Mohamed Ali; Tan Mathew; Lewin Nancy; Hennings Henry; Pearce Larry L; Blumberg Peter M
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.
Journal of medicinal chemistry 2003;46(3):364-73.
2002: Woolverton W L; Ranaldi R; Wang Z; Ordway G A; Paul I A; Petukhov P; Kozikowski A
Reinforcing strength of a novel dopamine transporter ligand: pharmacodynamic and pharmacokinetic mechanisms.
The Journal of pharmacology and experimental therapeutics 2002;303(1):211-7.
2002: Rong Suo-Bao; Zhang Jiazhong; Neale Joseph H; Wroblewski Jarda T; Wang Shaomeng; Kozikowski Alan P
Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors.
Journal of medicinal chemistry 2002;45(19):4140-52.
2002: Prakash K R C; Tang Y; Kozikowski Alan P; Flippen-Anderson Judith L; Knoblach Susan M; Faden Alan I
Synthesis and biological activity of novel neuroprotective diketopiperazines.
Bioorganic & medicinal chemistry 2002;10(9):3043-8.
2002: Riedel Gernot; Harrington Nicholas R; Kozikowski Alan P; Sandager-Nielsen Karin; Macphail Euan M
Variation of CS salience reveals group II mGluR-dependent and -independent forms of conditioning in the rat.
Neuropharmacology 2002;43(2):205-14.
2002: Petukhov Pavel A; Zhang Jianrong; Kozikowski Alan P; Wang Cheng Z; Ye Yan Ping; Johnson Kenneth M; Tella Srihari R
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.
Journal of medicinal chemistry 2002;45(15):3161-70.
2002: Ma Dawei; Tang Guozhi; Kozikowski Alan P
Synthesis of 7-substituted benzolactam-V8s and their selectivity for protein kinase C isozymes.
Organic letters 2002;4(14):2377-80.
2002: Wei Zhi-Liang; Sakamuri Sukumar; Petukhov Pavel A; George Clifford; Lewin Nancy E; Blumberg Peter M; Kozikowski Alan P
Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators.
Organic letters 2002;4(13):2169-72.
2002: Rajendran V; Saxena Ashima; Doctor Bhupendra P; Kozikowski Alan P
Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B.
Bioorganic & medicinal chemistry letters 2002;12(11):1521-3.
2002: Pomper Martin G; Musachio John L; Zhang Jiazhong; Scheffel Ursula; Zhou Yun; Hilton John; Maini Atul; Dannals Robert F; Wong Dean F; Kozikowski Alan P
11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase).
Molecular imaging : official journal of the Society for Molecular Imaging 2002;1(2):96-101.
2002: Zhang Ao; Zhou Guochun; Hoepping Alexander; Mukhopadhyaya Jayanta; Johnson Kenneth M; Zhang Mei; Kozikowski Alan P
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors.
Journal of medicinal chemistry 2002;45(9):1930-41.
2002: Zhang Ao; Zhou Guochun; Rong Suo-Bao; Johnson Kenneth M; Zhang Mei; Kozikowski Alan P
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Bioorganic & medicinal chemistry letters 2002;12(7):993-5.
2002: Rong Suo-Bao; Enyedy Istvan J; Qiao Lixin; Zhao Lianyun; Ma Dawei; Pearce Larry L; Lorenzo Patricia S; Stone James C; Blumberg Peter M; Wang Shaomeng; Kozikowski Alan P
Structural basis of RasGRP binding to high-affinity PKC ligands.
Journal of medicinal chemistry 2002;45(4):853-60.
2001: Zhang J; Flippen-Anderson J L; Kozikowski A P
A tandem Michael addition ring-closure route to the metabotropic receptor ligand alpha-(hydroxymethyl)glutamic acid and its gamma-alkylated derivatives.
The Journal of organic chemistry 2001;66(22):7555-9.
2001: Petukhov P A; Zhang M; Johnson K J; Tella S R; Kozikowski A P
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.
Bioorganic & medicinal chemistry letters 2001;11(16):2079-83.
2001: Mukhopadhyaya J K; Kozikowski A P; Grajkowska E; Pshenichkin S; Wroblewski J T
Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors.
Bioorganic & medicinal chemistry letters 2001;11(14):1919-24.
2001: Wang S; Sakamuri S; Enyedy I J; Kozikowski A P; Zaman W A; Johnson K M
Molecular modeling, structure--activity relationships and functional antagonism studies of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketones as a novel class of dopamine transporter inhibitors.
Bioorganic & medicinal chemistry 2001;9(7):1753-64.
2001: Enyedy I J; Zaman W A; Sakamuri S; Kozikowski A P; Johnson K M; Wang S
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(9):1113-8.
2001: Tamiz A P; Bandyopadhyay B C; Zhang J; Flippen-Anderson J L; Zhang M; Wang C Z; Johnson K M; Tella S; Kozikowski A P
Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors.
Journal of medicinal chemistry 2001;44(10):1615-22.
2001: Rong S B; Hu Y; Enyedy I; Powis G; Meuillet E J; Wu X; Wang R; Wang S; Kozikowski A P
Molecular modeling studies of the Akt PH domain and its interaction with phosphoinositides.
Journal of medicinal chemistry 2001;44(6):898-908.
2001: Kozikowski A P; Nan F; Conti P; Zhang J; Ramadan E; Bzdega T; Wroblewska B; Neale J H; Pshenichkin S; Wroblewski J T
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
Journal of medicinal chemistry 2001;44(3):298-301.
2001: Kozikowski A P; Tückmantel W; Hu Y
Studies in polyphenol chemistry and bioactivity. 3.(1,2) stereocontrolled synthesis of epicatechin-4alpha,8-epicatechin, an unnatural isomer of the B-type procyanidins.
The Journal of organic chemistry 2001;66(4):1287-96.
2001: Sakamuri S; Enyedy I J; Kozikowski A P; Zaman W A; Johnson K M; Wang S
Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(4):495-500.
2001: Trzcinska M; Pimentel P; Stellar J R; Hanson R N; Choi S W; Elmaleh D R; Zhang J; Prakash K R; Tamiz A P; Kozikowski A P; Johnson K M; Smith M P; Babich J W
Novel monoamine transporter ligands reduce cocaine-induced enhancement of brain stimulation reward.
Pharmacology, biochemistry, and behavior 2001;68(1):171-80.
2001: Ma D; Zhang T; Wang G; Kozikowski A P; Lewin N E; Blumberg P M
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Bioorganic & medicinal chemistry letters 2001;11(2):99-101.
2001: Hu Y; Meuillet E J; Berggren M; Powis G; Kozikowski A P
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.
Bioorganic & medicinal chemistry letters 2001;11(2):173-6.
2000: Tamiz A P; Conti P; Zhang M; Johnson K M; Kozikowski A P
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents.
Bioorganic & medicinal chemistry letters 2000;10(24):2741-3.
2000: Rajendran V; Prakash K R; Ved H S; Saxena A; Doctor B P; Kozikowski A P
Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A.
Bioorganic & medicinal chemistry letters 2000;10(21):2467-9.
2000: Kozikowski A P; Tückmantel W; George C
Studies in polyphenol chemistry and bioactivity. 2. Establishment of interflavan linkage regio- and stereochemistry by oxidative degradation of an O-alkylated derivative of procyanidin B2 to (R)-(-)-2,4-diphenylbutyric acid.
The Journal of organic chemistry 2000;65(17):5371-81.
2000: Zhao L; Johnson K M; Zhang M; Flippen-Anderson J; Kozikowski A P
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.
Journal of medicinal chemistry 2000;43(17):3283-94.
2000: Hu Y; Qiao L; Wang S; Rong S B; Meuillet E J; Berggren M; Gallegos A; Powis G; Kozikowski A P
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.
Journal of medicinal chemistry 2000;43(16):3045-51.
2000: Tamiz A P; Smith M P; Enyedy I; Flippen-Anderson J; Zhang M; Johnson K M; Kozikowski A P
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2000;10(15):1681-6.
2000: Prakash K R; Trzcinska M; Johnson K M; Kozikowski A P
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.
Bioorganic & medicinal chemistry letters 2000;10(13):1443-6.
2000: Hoepping A; Johnson K M; George C; Flippen-Anderson J; Kozikowski A P
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.
Journal of medicinal chemistry 2000;43(10):2064-71.
2000: Tamiz A P; Zhang J; Flippen-Anderson J L; Zhang M; Johnson K M; Deschaux O; Tella S; Kozikowski A P
Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.
Journal of medicinal chemistry 2000;43(6):1215-22.
2000: Nan F; Bzdega T; Pshenichkin S; Wroblewski J T; Wroblewska B; Neale J H; Kozikowski A P
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.
Journal of medicinal chemistry 2000;43(5):772-4.
2000: Tamiz A P; Smith M P; Kozikowski A P
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.
Bioorganic & medicinal chemistry letters 2000;10(3):297-300.
2000: Wang S; Sakamuri S; Enyedy I J; Kozikowski A P; Deschaux O; Bandyopadhyay B C; Tella S R; Zaman W A; Johnson K M
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.
Journal of medicinal chemistry 2000;43(3):351-60.
2000: Qiao L; Hu Y; Nan F; Powis G; Kozikowski A P
A versatile approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from L-(-)-quebrachitol.
Organic letters 2000;2(2):115-7.
1999: Prakash K R; Tamiz A P; Araldi G L; Zhang M; Johnson K M; Kozikowski A P
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.
Bioorganic & medicinal chemistry letters 1999;9(23):3325-8.
1999: Hoepping A; Babich J; Zubieta J A; Johnson K M; Machill S; Kozikowski A P
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
Bioorganic & medicinal chemistry letters 1999;9(22):3211-6.
1999: Faden A I; Fox G B; Fan L; Araldi G L; Qiao L; Wang S; Kozikowski A P
Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents.
The American journal of physiology 1999;277(4 Pt 2):R1196-204.
1999: Wang S; Liu M; Lewin N E; Lorenzo P S; Bhattacharrya D; Qiao L; Kozikowski A P; Blumberg P M
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.
Journal of medicinal chemistry 1999;42(18):3436-46.
1999: Kozikowski A P; Simoni D; Roberti M; Rondanin R; Wang S; Du P; Johnson K M
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.
Bioorganic & medicinal chemistry letters 1999;9(13):1831-6.
1999: Kozikowski A P; Araldi G L; Tückmantel W; Pshenichkin S; Surina E; Wroblewski J T
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.
Bioorganic & medicinal chemistry letters 1999;9(12):1721-6.
1999: Ma D; Wang G; Wang S; Kozikowski A P; Lewin N E; Blumberg P M
Synthesis and protein kinase C binding activity of benzolactam-V7.
Bioorganic & medicinal chemistry letters 1999;9(10):1371-4.
1999: Ibarreta D; Duchén M; Ma D; Qiao L; Kozikowski A P; Etcheberrigaray R
Benzolactam (BL) enhances sAPP secretion in fibroblasts and in PC12 cells.
Neuroreport 1999;10(5):1035-40.
1999: Faden A I; Fox G; Fan L; Knoblach S; Araldi G L; Kozikowski A P
Neuroprotective and cognitive enhancing effects of novel small peptides.
Annals of the New York Academy of Sciences 1999;890():120.
1998: Kozikowski A P; Araldi G L; Prakash K R; Zhang M; Johnson K M
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.
Journal of medicinal chemistry 1998;41(25):4973-82.
1998: Ma D; Ma Z; Kozikowski A P; Pshenichkin S; Wroblewski J T
Synthesis and biological evaluation of two analogues of (S)-alpha-methyl-3-carboxyphenylalanine.
Bioorganic & medicinal chemistry letters 1998;8(18):2447-50.
1998: Bhagavan S; Ibarreta D; Ma D; Kozikowski A P; Etcheberrigaray R
Restoration of TEA-induced calcium responses in fibroblasts from Alzheimer's disease patients by a PKC activator.
Neurobiology of disease 1998;5(3):177-87.
1998: Qiao L; Nan F; Kunkel M; Gallegos A; Powis G; Kozikowski A P
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.
Journal of medicinal chemistry 1998;41(18):3303-6.
1998: Kozikowski A P; Araldi G L; Boja J; Meil W M; Johnson K M; Flippen-Anderson J L; George C; Saiah E
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.
Journal of medicinal chemistry 1998;41(11):1962-9.
1998: Kozikowski A P; Steensma D; Araldi G L; Tückmantel W; Wang S; Pshenichkin S; Surina E; Wroblewski J T
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
Journal of medicinal chemistry 1998;41(10):1641-50.
1998: Qiao L; Kozikowski A P; Olivera A; Spiegel S
Synthesis and evaluation of a photolyzable derivative of sphingosine 1-phosphate--caged SPP.
Bioorganic & medicinal chemistry letters 1998;8(7):711-4.
1998: Kozikowski A P; Araldi G L; Flippen-Anderson J; George C; Pshenichkin S; Surina E; Wroblewski J
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.
Bioorganic & medicinal chemistry letters 1998;8(8):925-30.
1998: Kozikowski A P; Steensma D; Varasi M; Pshenichkin S; Surina E; Wroblewski J T
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.
Bioorganic & medicinal chemistry letters 1998;8(5):447-52.
1997: Kozikowski A P; Kotoula M; Ma D; Boujrad N; Tückmantel W; Papadopoulos V
Synthesis and biology of a 7-nitro-2,1,3-benzoxadiazol-4-yl derivative of 2-phenylindole-3-acetamide: a fluorescent probe for the peripheral-type benzodiazepine receptor.
Journal of medicinal chemistry 1997;40(16):2435-9.
1997: Kozikowski A P; Wang S; Ma D; Yao J; Ahmad S; Glazer R I; Bogi K; Acs P; Modarres S; Lewin N E; Blumberg P M
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Journal of medicinal chemistry 1997;40(9):1316-26.
1995: Kozikowski A P; Eddine Saiah M K; Johnson K M; Bergmann J S
Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position.
Journal of medicinal chemistry 1995;38(16):3086-93.
1995: Kozikowski A P; Ma D; Du L; Lewin N E; Bumberg P M
Effect of alteration of the heterocyclic nucleus of ILV on its isoform selectivity for PKC. Palladium catalyzed route to benzofuran analogues of ILV.
Farmaco (Società chimica italiana : 1989) 1995;50(6):425-30.
1995: Kozikowski A P; Kiddle J J; Frew T; Berggren M; Powis G
Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation.
Journal of medicinal chemistry 1995;38(7):1053-6.
1995: Powis G; Berggren M; Gallegos A; Frew T; Hill S; Kozikowski A; Bonjouklian R; Zalkow L; Abraham R; Ashendel C
Advances with phospholipid signalling as a target for anticancer drug development.
Acta biochimica Polonica 1995;42(4):395-403.
1994: Pang Y P; Kozikowski A P
Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program.
Journal of computer-aided molecular design 1994;8(6):683-93.
1994: Pang Y P; Kozikowski A P
Prediction of the binding sites of huperzine A in acetylcholinesterase by docking studies.
Journal of computer-aided molecular design 1994;8(6):669-81.
1994: Wilcox R A; Challiss R A; Traynor J R; Fauq A H; Ognayanov V I; Kozikowski A P; Nahorski S R
Molecular recognition at the myo-inositol 1,4,5-trisphosphate receptor. 3-position substituted myo-inositol 1,4,5-trisphosphate analogues reveal the binding and Ca2+ release requirements for high affinity interaction with the myo-inositol 1,4,5-trisphosphate receptor.
The Journal of biological chemistry 1994;269(43):26815-21.
1994: Kozikowski A P; Saiah M K; Bergmann J S; Johnson K M
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding.
Journal of medicinal chemistry 1994;37(20):3440-2.
1994: Pang Y P; Zaidi J; Kozikowski A P; Cusack B; Richelson E
Rational design of novel neurotensin mimetics: discovery of a pharmacologically unprecedented agent exhibiting concentration-dependent dual effects as antagonist and full agonist.
Journal of computer-aided molecular design 1994;8(4):433-40.
1994: Kozikowski A P; Fauq A H; Wilcox R A; Challiss R A; Nahorski S R
The novel Ins(1,4,5)P3 analogue 3-amino-3-deoxy-Ins(1,4,5)P3: a pH-dependent Ins(1,4,5)P3 receptor partial agonist in SH-SY5Y neuroblastoma cells.
Journal of medicinal chemistry 1994;37(6):868-72.
1994: Brunn G; Fauq A H; Chow S; Kozikowski A P; Gallegos A; Powis G
Cellular pharmacology of D-3-azido-3-deoxy-myo-inositol, an inhibitor of phosphatidylinositol signaling having antiproliferative activity.
Cancer chemotherapy and pharmacology 1994;35(1):71-9.
1993: Simoni D; Stoelwinder J; Kozikowski A P; Johnson K M; Bergmann J S; Ball R G
Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist".
Journal of medicinal chemistry 1993;36(24):3975-77.
1993: Cusack B; Richelson E; Pang Y P; Zaidi J; Kozikowski A P
Pharmacological studies on novel neurotensin mimetics: discovery of a pharmacologically unique agent exhibiting concentration-dependent dual effects as antagonist and agonist.
Molecular pharmacology 1993;44(5):1036-40.
1993: Kozikowski A P; Ognyanov V I; Chen C; Fauq A H; Safrany S T; Wilcox R A; Nahorski S R
Deoxygenated inositol 1,4,5-trisphosphate analogues and their interaction with metabolic enzymes. (1R,2R,4R)-cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor.
Journal of medicinal chemistry 1993;36(20):3035-8.
1993: Kozikowski A P; Ma D; Brewer J; Sun S; Costa E; Romeo E; Guidotti A
Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Journal of medicinal chemistry 1993;36(20):2908-20.
1993: Casalotti S O; Kozikowski A P; Fauq A; Tückemantel W; Krueger K E
Monoclonal antibodies against a phencyclidine derivative are used to investigate protein-ligand interactions.
European journal of pharmacology 1993;247(2):209-13.
1993: Romeo E; Cavallaro S; Korneyev A; Kozikowski A P; Ma D; Polo A; Costa E; Guidotti A
Stimulation of brain steroidogenesis by 2-aryl-indole-3-acetamide derivatives acting at the mitochondrial diazepam-binding inhibitor receptor complex.
The Journal of pharmacology and experimental therapeutics 1993;267(1):462-71.
1993: Kozikowski A P; Tückmantel W; Liao Y; Manev H; Ikonomovic S; Wroblewski J T
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives.
Journal of medicinal chemistry 1993;36(18):2706-8.
1993: Auta J; Romeo E; Kozikowski A; Ma D; Costa E; Guidotti A
Participation of mitochondrial diazepam binding inhibitor receptors in the anticonflict, antineophobic and anticonvulsant action of 2-aryl-3-indoleacetamide and imidazopyridine derivatives.
The Journal of pharmacology and experimental therapeutics 1993;265(2):649-56.
1992: Kozikowski A P; Roberti M; Xiang L; Bergmann J S; Callahan P M; Cunningham K A; Johnson K M
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.
Journal of medicinal chemistry 1992;35(25):4764-6.
1992: Johnson K M; Bergmann J S; Kozikowski A P
Cocaine and dopamine differentially protect [3H]mazindol binding sites from alkylation by N-ethylmaleimide.
European journal of pharmacology 1992;227(4):411-5.
1992: Romeo E; Auta J; Kozikowski A P; Ma D; Papadopoulos V; Puia G; Costa E; Guidotti A
2-Aryl-3-indoleacetamides (FGIN-1): a new class of potent and specific ligands for the mitochondrial DBI receptor (MDR).
The Journal of pharmacology and experimental therapeutics 1992;262(3):971-8.
1992: Reynolds I J; Rothermund K; Rajdev S; Fauq A H; Kozikowski A P
[125I]thienylphencyclidine, a novel ligand for the NMDA receptor.
European journal of pharmacology 1992;226(1):53-8.
1992: Chen C; Kozikowski A P; Wood P L; Reynolds I J; Ball R G; Pang Y P
Synthesis and biological activity of 8a-phenyldecahydroquinolines as probes of PCP's binding conformation. A new PCP-like compound with increased in vivo potency.
Journal of medicinal chemistry 1992;35(9):1634-8.
1992: Basu A; Kozikowski A P; Lazo J S
Structural requirements of lyngbyatoxin A for activation and downregulation of protein kinase C.
Biochemistry 1992;31(15):3824-30.
1992: Casalotti S O; Kozikowski A P; Fauq A; Tückmantel W; Krueger K E
Design of an irreversible affinity ligand for the phencyclidine recognition site on N-methyl-D-aspartate-type glutamate receptors.
The Journal of pharmacology and experimental therapeutics 1992;260(1):21-8.
1991: Kozikowski A P; Miller C P; Yamada F; Pang Y P; Miller J H; McKinney M; Ball R G
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity.
Journal of medicinal chemistry 1991;34(12):3399-402.
1991: McKinney M; Miller J H; Yamada F; Tuckmantel W; Kozikowski A P
Potencies and stereoselectivities of enantiomers of huperzine A for inhibition of rat cortical acetylcholinesterase.
European journal of pharmacology 1991;203(2):303-5.
1991: Kozikowski A P; Shum P W; Basu A; Lazo J S
Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C.
Journal of medicinal chemistry 1991;34(8):2420-30.
1991: Mistry J S; Abraham D J; Kozikowski A P; Hanin I
Neurochemistry of aging. 2. Design, synthesis, and biological evaluation of halomethyl analogues of choline with high affinity choline transport inhibitory activity.
Journal of medicinal chemistry 1991;34(7):2031-6.
1991: Basu A; Kozikowski A P; Sato K; Lazo J S
Cellular sensitization to cis-diamminedichloroplatinum(II) by novel analogues of the protein kinase C activator lyngbyatoxin A.
Cancer research 1991;51(10):2511-4.
1991: Geib S J; Tückmantel W; Kozikowski A P
Huperzine A--a potent acetylcholinesterase inhibitor of use in the treatment of Alzheimer's disease.
Acta crystallographica. Section C, Crystal structure communications 1991;47 ( Pt 4)():824-7.
1991: Powis G; Aksoy I A; Melder D C; Aksoy S; Eichinger H; Fauq A H; Kozikowski A P
D-3-deoxy-3-substituted myo-inositol analogues as inhibitors of cell growth.
Cancer chemotherapy and pharmacology 1991;29(2):95-104.
1990: Kozikowski A P; Tückmantel W; Reynolds I J; Wroblewski J T
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
Journal of medicinal chemistry 1990;33(6):1561-71.
1990: Kozikowski A P; Pang Y P
Structural determinants of affinity for the phencyclidine binding site of the N-methyl-D-aspartate receptor complex: discovery of a rigid phencyclidine analogue of high binding affinity.
Molecular pharmacology 1990;37(3):352-7.
1989: Kozikowski A P; Tueckmantel W; Maloneyhuss K
The discovery of new chemical modulators of the N-methyl-D-aspartate receptor.
Annals of the New York Academy of Sciences 1989;568():159-65.

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