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Craig Lindsley

Research Profile

Physiology

Allosteric Regulation

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Publications

TOP 3
Darren W Engers; Audrey Y Frist; Charles C Hong; Craig W Lindsley; Corey R Hopkins
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Patrick R Gentry; Peter S Hodder; P Jeffrey Conn; Atin Lamsal; Colleen M Niswender; J Scott Daniels; Emery Smith; Paige N Vinson; Michael R Wood; Thomas M Bridges; Peter Chase; Julie L Engers; Craig W Lindsley
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Karen J Gregory; Craig W Lindsley; Jens Meiler; Elizabeth D Nguyen; Sean D Reiff; Emma F Squire; Shaun R Stauffer; P Jeffrey Conn
Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a "Molecular Switch" in PAM Pharmacology.

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All Publications

2013: Darren W Engers; Audrey Y Frist; Charles C Hong; Craig W Lindsley; Corey R Hopkins
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Bioorganic & medicinal chemistry letters 2013;23(11):3248-52.
2013: Patrick R Gentry; Peter S Hodder; P Jeffrey Conn; Atin Lamsal; Colleen M Niswender; J Scott Daniels; Emery Smith; Paige N Vinson; Michael R Wood; Thomas M Bridges; Peter Chase; Julie L Engers; Craig W Lindsley
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Bioorganic & medicinal chemistry letters 2013;23(10):2996-3000.
2013: Karen J Gregory; Craig W Lindsley; Jens Meiler; Elizabeth D Nguyen; Sean D Reiff; Emma F Squire; Shaun R Stauffer; P Jeffrey Conn
Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a "Molecular Switch" in PAM Pharmacology.
Molecular pharmacology 2013;83(5):991-1006.
2013: M J Noetzel; S R Stauffer; P N Vinson; Zixiu Xiang; K J Gregory; Craig W Lindsley; J T Manka; Colleen M Niswender; P Jeffrey Conn
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.
Molecular pharmacology 2013;83(4):835-47.
2013: Matthew C O'Reilly; Sarah A Scott; Paul G Thomas; Ryan Morrison; Thomas H Oguin; H Alex Brown; Kyle A Brown; J Scott Daniels; Craig W Lindsley
Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
Journal of medicinal chemistry 2013;56(6):2695-9.
2013: Michael S Poslusney; Douglas J Sheffler; Thomas J Utley; Thomas M Bridges; P Jeffrey Conn; J Scott Daniels; Patrick R Gentry; Craig W Lindsley; Bruce J Melancon; Colleen M Niswender; Michael R Wood
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.
Bioorganic & medicinal chemistry letters 2013;23(6):1860-4.
2013: Jerri M Rook; Shaun R Stauffer; Paige N Vinson; Zixiu Xiang; Ya Zhou; Thomas M Bridges; Hyekyung P Cho; J Scott Daniels; F Edward Dudek; Rocco D Gogliotti; Karen J Gregory; Carrie K Jones; Craig W Lindsley; Jason T Manka; Colleen M Niswender; Meredith J Noetzel; Wendy A Pouliot; P Jeffrey Conn
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
Biological psychiatry 2013;73(6):501-9.
2013: Jon Jacobs; Craig W Lindsley; Andrew D Mesecar; Anna M Mielech; S Adrian Saldanha; Yahira M Baez-Santos; Susan C Baker; Peter Chase; Eric S Dawson; Aimee Eggler; Valerie Grum-Tokars; Peter Hodder; Sakshi Tomar; Mark Turlington; Ya Zhou; Shaun R Stauffer
Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease.
Journal of medicinal chemistry 2013;56(2):534-46.
2013: Bruce J Melancon; Colleen M Niswender; Michael S Poslusney; Douglas J Sheffler; James C Tarr; Thomas J Utley; Thomas M Bridges; P Jeffrey Conn; J Scott Daniels; Patrick R Gentry; Craig W Lindsley; Margrith E Mattmann; Michael R Wood
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.
Bioorganic & medicinal chemistry letters 2013;23(2):412-6.
2013: Jason D Downey; Craig W Lindsley; Ryan D Morrison; Sam A Saleh; J Scott Daniels; Thomas M Bridges; Richard M Breyer
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.
Bioorganic & medicinal chemistry letters 2013;23(1):37-41.
2013: Douglas J Sheffler; James C Tarr; Michael R Wood; Kimberly M Lovell; Colleen M Niswender; Christian Sevel; Sheridan J S Carrington; Hyekyung P Cho; P Jeffrey Conn; Gregory J Digby; Corey R Hopkins; Uyen M Le; Craig W Lindsley
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
Bioorganic & medicinal chemistry letters 2013;23(1):223-7.
2013: Uyen M Le; Craig W Lindsley; Bruce J Melancon; Colleen M Niswender; Alice L Rodriguez; Douglas J Sheffler; Thomas J Utley; Daryl Venable; Paige N Vinson; Michael R Wood; Anna L Blobaum; Thomas M Bridges; P Jeffrey Conn; J Scott Daniels; Carrie K Jones; Atin Lamsal; Corey R Hopkins
Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.
Bioorganic & medicinal chemistry letters 2013;23(1):346-50.
2012: Gregory J Digby; Atin Lamsal; Evan P Lebois; Craig W Lindsley; Colleen M Niswender; Christian Sevel; Douglas J Sheffler; Thomas J Utley; Michael R Wood; Thomas M Bridges; P Jeffrey Conn
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
ACS chemical neuroscience 2012;3(12):1025-36.
2012: Alice L Rodriguez; J Scott Daniels; Thomas Steckler; Paige N Vinson; Richard Williams; Ya Zhou; José M Bartolomé; C David Weaver; Eric S Dawson; P Jeffrey Conn; Carrie K Jones; Hilde Lavreysen; Craig W Lindsley; Gregor J Macdonald; Claire Mackie; Colleen M Niswender; Shaun R Stauffer
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
Bioorganic & medicinal chemistry letters 2012;22(24):7388-92.
2012: James C Tarr; Mark L Turlington; Thomas J Utley; Michael R Wood; Zixui Xiang; Ryan D Morrison; Colleen M Niswender; Tristano Pancani; Paul R Reid; Douglas J Sheffler; Anna L Blobaum; Thomas M Bridges; Hyekyung P Cho; P Jeffrey Conn; J Scott Daniels; Rebecca Klar; Michael T Klein; Craig W Lindsley
Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.
ACS chemical neuroscience 2012;3(11):884-95.
2012: Joseph D Panarese; Craig W Lindsley
Biomimetic synthesis and biological evaluation of Aplidiopsamine A.
Organic letters 2012;14(22):5808-10.
2012: Michael S Poslusney; Christian Sevel; Douglas J Sheffler; Thomas J Utley; Thomas M Bridges; P Jeffrey Conn; J S Daniels; Nathan R Kett; Craig W Lindsley; Ryan D Morrison; Colleen M Niswender; Michael R Wood
Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.
Bioorganic & medicinal chemistry letters 2012;22(22):6923-8.
2012: Karen J Gregory; Craig W Lindsley; Colleen M Niswender; Meredith J Noetzel; Alice L Rodriguez; Jerri M Rook; Shaun R Stauffer; Paige N Vinson; Ya Zhou; Brian A Chauder; Aspen C Chun; Kyle A Emmitte; Andrew S Felts; P Jeffrey Conn
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.
Molecular pharmacology 2012;82(5):860-75.
2012: Jason T Manka; Colleen M Niswender; Thomas Steckler; Paige N Vinson; C David Weaver; Richard Williams; Ya Zhou; José M Bartolomé; P Jeffrey Conn; J Scott Daniels; Emily Days; Kiran Gogi; Karen J Gregory; Elizabeth J Herman; Satya Jadhav; Carrie K Jones; Hilde Lavreysen; Craig W Lindsley; Gregor J Macdonald; Claire Mackie; Shaun R Stauffer
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Bioorganic & medicinal chemistry letters 2012;22(20):6481-5.
2012: Margrith E Mattmann; Owen B McManus; Meng Wu; Kaiping Xu; Haibo Yu; Xiaofang Huang; Uyen M Le; Min Li; Zhihong Lin; Craig W Lindsley; Shunyou Long; Darren W Engers; Corey R Hopkins
Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Bioorganic & medicinal chemistry letters 2012;22(18):5936-41.
2012: Ryan D Morrison; Colleen M Niswender; Alice L Rodriguez; Roger Rush; Raymundo Sanchez-Ponce; Tammy S Santomango; Donald Stec; Daryl F Venable; Brittney S Bates; Anna L Blobaum; Katrina A Brewer; Thomas M Bridges; Frank W Byers; P Jeffrey Conn; Melany M Corlew; Kyle A Emmitte; Andrew S Felts; Carrie K Jones; Craig W Lindsley; Jason Manka; J Scott Daniels
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
Drug metabolism and disposition: the biological fate of chemicals 2012;40(9):1834-45.
2012: Ralf Mueller; Colleen M Niswender; C David Weaver; Mariusz Butkiewicz; P Jeffrey Conn; Eric S Dawson; Corey R Hopkins; Craig W Lindsley; Jens Meiler
Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.
Journal of molecular modeling 2012;18(9):4437-46.
2012: Yiu-Yin Cheung; Min Li; Craig W Lindsley; Owen B McManus; Meng Wu; Kaiping Xu; Haibo Yu; Beiyan Zou; Corey R Hopkins
Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Journal of medicinal chemistry 2012;55(15):6975-9.
2012: Bruce J Melancon; Ryan D Morrison; Colleen M Niswender; Christian Sevel; Douglas J Sheffler; Thomas J Utley; Thomas M Bridges; Yiu-Yin Cheung; Craig W Lindsley; Margrith E Mattmann; P Jeffrey Conn; J Scott Daniels; Michael R Wood
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.
Bioorganic & medicinal chemistry letters 2012;22(15):5035-40.
2012: James M Salovich; Douglas J Sheffler; Thomas J Utley; Paige N Vinson; Michael R Wood; P Jeffrey Conn; J Scott Daniels; Carrie K Jones; Atin Lamsal; Uyen Le; Craig W Lindsley; Colleen M Niswender; Anna L Blobaum; Thomas M Bridges; Corey R Hopkins
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.
Bioorganic & medicinal chemistry letters 2012;22(15):5084-8.
2012: Eric Delpire; Nathan Kett; Kwangho Kim; Ryan D Morrison; Alex G Waterson; J Scott Daniels; C David Weaver; Aleksandra Baranczak; Craig W Lindsley
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.
Bioorganic & medicinal chemistry letters 2012;22(14):4532-5.
2012: Gregory J Digby; Kimberly Italiano; Carrie K Jones; Evan P Lebois; Craig W Lindsley; Sarah E Mennenga; Ryan Morrison; Natali E Nemirovsky; Colleen M Niswender; Meredith J Noetzel; M Foster Olive; Douglas J Sheffler; Thomas J Utley; Adam G Walker; Zixiu Xiang; Heather A Bimonte-Nelson; Jacob Bode; Michael Bubser; Nellie E Byun; Bryan W Camp; Hyekyung P Cho; J Scott Daniels; Albert A Davis; P Jeffrey Conn
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2012;32(25):8532-44.
2012: Douglas J Sheffler; Shaun R Stauffer; Mitchell Vamos; Paige N Vinson; Cody J Wenthur; P Jeffrey Conn; J Scott Daniels; Anna L Blobaum; Joshua A Bruner; Sheridan J S Carrington; Nicholas D P Cosford; Kiran K Gogi; Ryan D Morrison; Colleen M Niswender; Craig W Lindsley
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Bioorganic & medicinal chemistry letters 2012;22(12):3921-5.
2012: Matthew C O'Reilly; Craig W Lindsley
A general, enantioselective synthesis of protected morpholines and piperazines.
Organic letters 2012;14(11):2910-3.
2012: Bruce J Melancon; Ryan D Morrison; Colleen M Niswender; Sam A Saleh; Douglas J Sheffler; James C Tarr; Thomas J Utley; Thomas M Bridges; Brian A Chauder; Hyekyung P Cho; P Jeffrey Conn; J Scott Daniels; Rocco D Gogliotti; Evan P Lebois; Craig W Lindsley; Michael R Wood
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
Bioorganic & medicinal chemistry letters 2012;22(10):3467-72.
2012: Olugbeminiyi O Fadeyi; Kristopher N Hahn; Timothy J Senter; Craig W Lindsley
A versatile enantioselective synthesis of azabicyclic ring systems: a concise total synthesis of (+)-grandisine D and unnatural analogues.
Chemistry (Weinheim an der Bergstrasse, Germany) 2012;18(19):5826-31.
2012: Craig W Lindsley; Corey R Hopkins
Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature.
Expert opinion on therapeutic patents 2012;22(5):461-81.
2012: Timothy J Senter; Olugbeminiyi O Fadeyi; Craig W Lindsley
Enantioselective total synthesis of (+)-amabiline.
Organic letters 2012;14(7):1869-71.
2012: Morgane Thomsen; Jürgen Wess; Jeffrey E Wessell; P Jeffrey Conn; Brian S Fulton; Craig W Lindsley; S Barak Caine
Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice.
Psychopharmacology 2012;220(4):673-85.
2012: Ralf Mueller; Colleen M Niswender; Christopher M Olsen; Alice L Rodriguez; Danny G Winder; Jens Meiler; Usha N Menon; Brittney S Bates; Brian A Chauder; P Jeffrey Conn; Eric S Dawson; Kyle A Emmitte; Andrew S Felts; Karen J Gregory; Sataywan B Jadhav; Carrie K Jones; Alexander S Kane; Jeffrey P Lamb; Craig W Lindsley
Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.
ChemMedChem 2012;7(3):406-14.
2012: Zixiu Xiang; Carrie K Jones; Craig W Lindsley; Analisa D Thompson; P Jeffrey Conn
Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease.
The Journal of pharmacology and experimental therapeutics 2012;340(3):595-603.
2012: Bruce J Melancon; Colleen M Niswender; Michael R Wood; Arthur Christopoulos; P Jeffrey Conn; Kyle A Emmitte; Corey R Hopkins; Craig W Lindsley
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
Journal of medicinal chemistry 2012;55(4):1445-64.
2012: Carrie K Jones; Craig W Lindsley; Ryan D Morrison; Analisa D Thompson; Nathalie Turle-Lorenzo; Marianne Amalric; Anna L Blobaum; Jacob Bode; Thomas M Bridges; Michael Bubser; P Jeffrey Conn; J Scott Daniels; Jonathan W Dickerson; Darren W Engers; Corey R Hopkins; Kimberly Italiano; Satyawan Jadhav; Colleen M Niswender
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
The Journal of pharmacology and experimental therapeutics 2012;340(2):404-21.
2012: Meredith J Noetzel; Alice L Rodriguez; Jerri M Rook; Shaun R Stauffer; Paige N Vinson; C David Weaver; Zixiu Xiang; Y Zhou; J Scott Daniels; Emily Days; Carrie K Jones; Hilde Lavreysen; Craig W Lindsley; Colleen M Niswender; Hyekyung P Cho; P Jeffrey Conn
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Molecular pharmacology 2012;81(2):120-33.
2011: Thomas Utley; Paige N Vinson; Rocio Zamorano; James M Salovich; Dustin Haddenham; Corey R Hopkins; Craig W Lindsley; Colleen M Niswender
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.
Bioorganic & medicinal chemistry letters 2011;21(23):6955-9.
2011: Carrie K Jones; Craig W Lindsley; Stacey R Lindsley; Ryan Morrison; Colleen M Niswender; Yoland Smith; Analisa D Thompson; C David Weaver; Rocio Zamorano; Ya Zhou; Anna L Blobaum; Jim Bogenpohl; P Jeffrey Conn; J Scott Daniels; Darren W Engers; Julie R Field; Rocco D Gogliotti; Satyawan Jadhav; Corey R Hopkins
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.
Journal of medicinal chemistry 2011;54(21):7639-47.
2011: Evan P Lebois; Thomas M Bridges; Hyekyung P Cho; Gregory J Digby; Bruce J Melancon; Nicole R Miller; Ryan Morrison; Douglas J Sheffler; James C Tarr; Michael R Wood; Zixiu Xiang; P Jeffrey Conn; J Scott Daniels; Craig W Lindsley
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.
Bioorganic & medicinal chemistry letters 2011;21(21):6451-5.
2011: Michael L Schulte; Craig W Lindsley
Highly diastereoselective and general synthesis of primary β-fluoroamines.
Organic letters 2011;13(20):5684-7.
2011: Paige E Selvy; Robert R Lavieri; Craig W Lindsley; H Alex Brown
Phospholipase D: enzymology, functionality, and chemical modulation.
Chemical reviews 2011;111(10):6064-119.
2011: Sydney L Stoops; A Scott Pearson; Connie Weaver; Alex G Waterson; Emily Days; Chris Farmer; Suzanne Brady; C David Weaver; R Daniel Beauchamp; Craig W Lindsley
Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells.
ACS chemical biology 2011;6(5):452-65.
2011: Jeffrey P Lamb; Darren W Engers; Colleen M Niswender; Alice L Rodriguez; Daryl F Venable; P Jeffrey Conn; Craig W Lindsley
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
Bioorganic & medicinal chemistry letters 2011;21(9):2711-4.
2011: Scott E Wolkenberg; Zhijian Zhao; Catherine Thut; Jill W Maxwell; Terrence P McDonald; Fumi Kinose; Michael Reilly; Craig W Lindsley; George D Hartman
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Journal of medicinal chemistry 2011;54(7):2351-8.
2011: Michael R Wood; Corey R Hopkins; John T Brogan; P Jeffrey Conn; Craig W Lindsley
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
Biochemistry 2011;50(13):2403-10.
2011: Terence G Hamill; Waisi Eng; Andrew Jennings; Richard Lewis; Steven Thomas; Suzanne Wood; Leslie Street; David D Wisnoski; Scott Wolkenberg; Craig W Lindsley; Sandra Sanabria; Shil Patel; Kerry Riffel; Christine Ryan; Jacquelynn Cook; Cyrille Sur; H Donald Burns; Richard Hargreaves
The synthesis and preclinical evaluation in rhesus monkey of [¹⁸F]MK-6577 and [¹¹C]CMPyPB glycine transporter 1 positron emission tomography radiotracers.
Synapse (New York, N.Y.) 2011;65(4):261-70.
2011: Yiu-Yin Cheung; Rocio Zamorano; Anna L Blobaum; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.
ACS combinatorial science 2011;13(2):159-65.
2011: Richard Williams; Jason T Manka; Alice L Rodriguez; Paige N Vinson; Colleen M Niswender; C David Weaver; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.
Bioorganic & medicinal chemistry letters 2011;21(5):1350-3.
2011: Rene Raphemot; Thomas Utley; C David Weaver; Rocco Gogliotti; Corey Hopkins; Rishin Kadakia; L Michelle Lewis; Craig W Lindsley; Daniel F Lonergan; Thuy T Nguyen; Jerod S Denton
Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1.
Frontiers in pharmacology 2011;2():75.
2011: Nicole Speed; Roxanne A Vaughan; Adeola R Davis; Lynette Daws; Jack P Kennedy; Craig W Lindsley; Heinrich J G Matthies; Rachael L Neve; Kevin D Niswender; W Anthony Owens; Scott J Russo; Sanaz Saadat; Christine Saunders; Aurelio Galli
Impaired striatal Akt signaling disrupts dopamine homeostasis and increases feeding.
PloS one 2011;6(9):e25169.
2011: Evan P Lebois; Carrie K Jones; Craig W Lindsley
The evolution of histamine H₃ antagonists/inverse agonists.
Current topics in medicinal chemistry 2011;11(6):648-60.
2011: Gautam Bhave; Brian A Chauder; Wen Liu; Eric S Dawson; Rishin Kadakia; Thuy T Nguyen; L Michelle Lewis; Jens Meiler; C David Weaver; Lisa M Satlin; Craig W Lindsley; Jerod S Denton
Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel.
Molecular pharmacology 2011;79(1):42-50.
2010: Alice L Rodriguez; Mark D Grier; Carrie K Jones; Elizabeth J Herman; Alexander S Kane; Randy L Smith; Richard Williams; Ya Zhou; Joy E Marlo; Emily L Days; Tasha N Blatt; Satyawan Jadhav; Usha N Menon; Paige N Vinson; Jerri M Rook; Shaun R Stauffer; Colleen M Niswender; Craig W Lindsley; C David Weaver; P Jeffrey Conn
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Molecular pharmacology 2010;78(6):1105-23.
2010: Thomas M Bridges; J Phillip Kennedy; Corey R Hopkins; P Jeffrey Conn; Craig W Lindsley
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(19):5617-22.
2010: Gregory J Digby; P Jeffrey Conn; Craig W Lindsley
Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.
Current opinion in drug discovery & development 2010;13(5):587-94.
2010: Darren W Engers; Patrick R Gentry; Richard Williams; Julie D Bolinger; C David Weaver; Usha N Menon; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Bioorganic & medicinal chemistry letters 2010;20(17):5175-8.
2010: Leslie N Aldrich; Sydney L Stoops; Brenda C Crews; Lawrence J Marnett; Craig W Lindsley
Total synthesis and biological evaluation of tambjamine K and a library of unnatural analogs.
Bioorganic & medicinal chemistry letters 2010;20(17):5207-11.
2010: Andrew S Felts; Stacey R Lindsley; Jeffrey P Lamb; Alice L Rodriguez; Usha N Menon; Satyawan Jadhav; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Bioorganic & medicinal chemistry letters 2010;20(15):4390-4.
2010: Olugbeminiyi O Fadeyi; Michael L Schulte; Craig W Lindsley
General access to chiral N-alkyl terminal aziridines via organocatalysis.
Organic letters 2010;12(14):3276-8.
2010: Thomas M Bridges; Evan P LeBois; Corey R Hopkins; Michael R Wood; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley
The antipsychotic potential of muscarinic allosteric modulation.
Drug news & perspectives 2010;23(4):229-40.
2010: Nicole R Miller; R Nathan Daniels; David Lee; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
Bioorganic & medicinal chemistry letters 2010;20(7):2174-7.
2010: Thomas M Bridges; J Phillip Kennedy; Meredith J Noetzel; Micah L Breininger; Patrick R Gentry; P Jeffrey Conn; Craig W Lindsley
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
Bioorganic & medicinal chemistry letters 2010;20(6):1972-5.
2010: Leslie N Aldrich; Eric S Dawson; Craig W Lindsley
Evaluation of the biosynthetic proposal for the synthesis of marineosins A and B.
Organic letters 2010;12(5):1048-51.
2010: Thomas M Bridges; J Phillip Kennedy; Hyekyung P Cho; Micah L Breininger; Patrick R Gentry; Corey R Hopkins; P Jeffrey Conn; Craig W Lindsley
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.
Bioorganic & medicinal chemistry letters 2010;20(2):558-62.
2010: Feng V Yang; William D Shipe; Jaime L Bunda; M Brad Nolt; David D Wisnoski; Zhijian Zhao; James C Barrow; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; George D Hartman; Craig W Lindsley
Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(2):531-6.
2010: Craig W Lindsley
The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update.
Current topics in medicinal chemistry 2010;10(4):458-77.
2009: Todd W Miller; James T Forbes; Chirayu Shah; Shelby K Wyatt; H Charles Manning; Maria G Olivares; Violeta Sanchez; Teresa C Dugger; Nara de Matos Granja; Archana Narasanna; Rebecca Cook; J Phillip Kennedy; Craig W Lindsley; Carlos L Arteaga
Inhibition of mammalian target of rapamycin is required for optimal antitumor effect of HER2 inhibitors against HER2-overexpressing cancer cells.
Clinical cancer research : an official journal of the American Association for Cancer Research 2009;15(23):7266-76.
2009: Ya Zhou; Alice L Rodriguez; Richard Williams; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Bioorganic & medicinal chemistry letters 2009;19(23):6502-6.
2009: Andrew S Felts; Sam A Saleh; Uyen Le; Alice L Rodriguez; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Bioorganic & medicinal chemistry letters 2009;19(23):6623-6.
2009: R Nathan Daniels; Bruce J Melancon; Emily A Wang; Brenda C Crews; Lawrence J Marnett; Gary A Sulikowski; Craig W Lindsley
Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A.
The Journal of organic chemistry 2009;74(22):8852-5.
2009: Jana K Shirey; Ashley E Brady; Paulianda J Jones; Albert A Davis; Thomas M Bridges; J Phillip Kennedy; Satyawan B Jadhav; Usha N Menon; Zixiu Xiang; Mona L Watson; Edward P Christian; James J Doherty; Michael C Quirk; Dean H Snyder; James J Lah; Allan Levey; Michelle M Nicolle; Craig W Lindsley; P Jeffrey Conn
A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2009;29(45):14271-86.
2009: J Phillip Kennedy; Thomas M Bridges; Patrick R Gentry; John T Brogan; Alexander S Kane; Carrie K Jones; Ashley E Brady; Jana K Shirey; P Jeffrey Conn; Craig W Lindsley
Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor.
ChemMedChem 2009;4(10):1600-7.
2009: Lei Ma; Matthew A Seager; Matthew Seager; Marion Wittmann; Marlene Jacobson; Denise Bickel; Maryann Burno; Keith Jones; Valerie Kuzmick Graufelds; Guangping Xu; Michelle Pearson; Alexander McCampbell; Renee Gaspar; Paul J Shughrue; Andrew Danziger; Christopher Regan; Rose Flick; Danette Pascarella; Susan Garson; Scott Doran; Constantine Kreatsoulas; Lone Veng; Craig W Lindsley; William Shipe; Scott Kuduk; Cyrille Sur; Gene G Kinney; Guy R Seabrook; William Ray
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(37):15950-5.
2009: Olugbeminiyi O Fadeyi; Craig W Lindsley
Total synthesis of brevisamide.
Organic letters 2009;11(17):3950-2.
2009: Richard Williams; Kari A Johnson; Patrick R Gentry; Colleen M Niswender; Charles D Weaver; P Jeffrey Conn; Craig W Lindsley; Corey R Hopkins
Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).
Bioorganic & medicinal chemistry letters 2009;19(17):4967-70.
2009: Douglas J Sheffler; Richard Williams; Thomas M Bridges; Zixiu Xiang; Alexander S Kane; Nellie E Byun; Satyawan Jadhav; Mathew M Mock; Fang Zheng; L Michelle Lewis; Carrie K Jones; Colleen M Niswender; Charles D Weaver; Craig W Lindsley; P Jeffrey Conn
A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Molecular pharmacology 2009;76(2):356-68.
2009: Jennifer E Ayala; Yelin Chen; Jessica L Banko; Douglas J Sheffler; Richard Williams; Alexandra N Telk; Noreen L Watson; Zixiu Xiang; Yongqin Zhang; Paulianda J Jones; Craig W Lindsley; M Foster Olive; P Jeffrey Conn
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 2009;34(9):2057-71.
2009: Sameer Sharma; Jeffrey Kedrowski; Jerri M Rook; Randy L Smith; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Craig W Lindsley
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
Journal of medicinal chemistry 2009;52(14):4103-6.
2009: Darren W Engers; Colleen M Niswender; C David Weaver; Satyawan Jadhav; Usha N Menon; Rocio Zamorano; P Jeffrey Conn; Craig W Lindsley; Corey R Hopkins
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
Journal of medicinal chemistry 2009;52(14):4115-8.
2009: Craig W Lindsley; Kyle A Emmitte
Recent progress in the discovery and development of negative allosteric modulators of mGluR5.
Current opinion in drug discovery & development 2009;12(4):446-57.
2009: Alice L Rodriguez; Richard Williams; Ya Zhou; Stacey R Lindsley; Uyen Le; Mark D Grier; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.
Bioorganic & medicinal chemistry letters 2009;19(12):3209-13.
2009: J Phillip Kennedy; P Jeffrey Conn; Craig W Lindsley
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.
Bioorganic & medicinal chemistry letters 2009;19(12):3204-8.
2009: Thomas M Bridges; Joy E Marlo; Colleen M Niswender; Carrie K Jones; Satyawan B Jadhav; Patrick R Gentry; Hyekyung C Plumley; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Journal of medicinal chemistry 2009;52(11):3445-8.
2009: Corey R Hopkins; Craig W Lindsley; Colleen M Niswender
mGluR4-positive allosteric modulation as potential treatment for Parkinson's disease.
Future medicinal chemistry 2009;1(3):501-13.
2009: Todd W Miller; Marianela Pérez-Torres; Archana Narasanna; Marta Guix; Olle Stål; Gizeh Pérez-Tenorio; Ana M Gonzalez-Angulo; Bryan T. J. Hennessy; Gordon B Mills; J Phillip Kennedy; Craig W Lindsley; Carlos L Arteaga
Loss of Phosphatase and Tensin homologue deleted on chromosome 10 engages ErbB3 and insulin-like growth factor-I receptor signaling to promote antiestrogen resistance in breast cancer.
Cancer research 2009;69(10):4192-201.
2009: Robert Lavieri; Sarah A Scott; Jana A Lewis; Paige E Selvy; Michelle D Armstrong; H Alex Brown; Craig W Lindsley
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
Bioorganic & medicinal chemistry letters 2009;19(8):2240-3.
2009: Jana A Lewis; Sarah A Scott; Robert Lavieri; Jason R Buck; Paige E Selvy; Sydney L Stoops; Michelle D Armstrong; H Alex Brown; Craig W Lindsley
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
Bioorganic & medicinal chemistry letters 2009;19(7):1916-20.
2009: Darren W Engers; Alice L Rodriguez; Richard Williams; Alexis S Hammond; Daryl Venable; Oluwatomi Oluwatola; Gary A Sulikowski; P Jeffrey Conn; Craig W Lindsley
Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273.
ChemMedChem 2009;4(4):505-11.
2009: Eric Delpire; Emily Days; L Michelle Lewis; Dehui Mi; Kwangho Kim; Craig W Lindsley; C David Weaver
Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(13):5383-8.
2009: P Jeffrey Conn; Carrie K Jones; Craig W Lindsley
Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.
Trends in pharmacological sciences 2009;30(3):148-55.
2009: Scott E Wolkenberg; Zhijian Zhao; David D Wisnoski; William H Leister; Julie O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Christopher Gibson; Bennett K Ma; Stacey L Polsky-Fisher; Craig W Lindsley; George D Hartman
Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 2009;19(5):1492-5.
2009: Zhijian Zhao; William H Leister; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; George D Hartman; Craig W Lindsley; Scott E Wolkenberg
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(5):1488-91.
2009: Joy E Marlo; Colleen M Niswender; Emily L Days; Thomas M Bridges; Yun Xiang; Alice L Rodriguez; Jana K Shirey; Ashley E Brady; Tasha Nalywajko; Qingwei Luo; Cheryl A Austin; Michael Baxter Williams; Kwangho Kim; Richard Williams; Darren Orton; H Alex Brown; Craig W Lindsley; C David Weaver; P Jeffrey Conn
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Molecular pharmacology 2009;75(3):577-88.
2009: Olugbeminiyi O Fadeyi; Craig W Lindsley
Rapid, general access to chiral beta-fluoroamines and beta,beta-difluoroamines via organocatalysis.
Organic letters 2009;11(4):943-6.
2009: Sarah A Scott; Paige E Selvy; Jason R Buck; Hyekyung P Cho; Tracy Criswell; Ashley L Thomas; Michelle D Armstrong; Carlos L Arteaga; Craig W Lindsley; H Alex Brown
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
Nature chemical biology 2009;5(2):108-17.
2009: Richard Williams; Colleen M Niswender; Qingwei Luo; Uyen Le; P Jeffrey Conn; Craig W Lindsley
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead.
Bioorganic & medicinal chemistry letters 2009;19(3):962-6.
2009: C David Weaver; Douglas J Sheffler; L Michelle Lewis; Thomas M Bridges; Richard Williams; Natalia T Nalywajko; J Phillip Kennedy; Matthew M Mulder; Satyawan Jadhav; Leslie A Aldrich; Carrie K Jones; Joy E Marlo; Colleen M Niswender; Matthew M Mock; Fang Zheng; P Jeffrey Conn; Craig W Lindsley
Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe.
Current topics in medicinal chemistry 2009;9(13):1217-26.
2009: Craig W Lindsley; Colleen M Niswender; Darren W Engers; Corey R Hopkins
Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease.
Current topics in medicinal chemistry 2009;9(10):949-63.
2009: Craig W Lindsley
Molecule of the month. FDA approves new treatment for fibromyalgia.
Current topics in medicinal chemistry 2009;9(2):225.
2009: P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.
Nature reviews. Drug discovery 2009;8(1):41-54.
2009: P Jeffrey Conn; Craig W Lindsley; Carrie K Jones
Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia.
Trends in pharmacological sciences 2009;30(1):25-31.
2008: Thomas M Bridges; Richard Williams; Craig W Lindsley
Design of potent GlyT1 inhibitors: in vitro and in vivo profiles.
Current opinion in molecular therapeutics 2008;10(6):591-601.
2008: Ashley E Brady; Carrie K Jones; Thomas M Bridges; J Phillip Kennedy; Analisa D Thompson; Justin U Heiman; Micah L Breininger; Patrick R Gentry; Huiyong Yin; Satyawan B Jadhav; Jana K Shirey; P Jeffrey Conn; Craig W Lindsley
Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats.
The Journal of pharmacology and experimental therapeutics 2008;327(3):941-53.
2008: Colleen M Niswender; Kari A Johnson; C David Weaver; Carrie K Jones; Zixiu Xiang; Qingwei Luo; Alice L Rodriguez; Joy E Marlo; Tomas de Paulis; Analisa D Thompson; Emily L Days; Tasha Nalywajko; Cheryl A Austin; Michael Baxter Williams; Jennifer E Ayala; Richard Williams; Craig W Lindsley; P Jeffrey Conn
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
Molecular pharmacology 2008;74(5):1345-58.
2008: Zhi-Qiang Yang; James C Barrow; William D Shipe; Kelly-Ann S Schlegel; Youheng Shu; F Vivien Yang; Craig W Lindsley; Kenneth E Rittle; Mark G Bock; George D Hartman; Victor N Uebele; Cindy E Nuss; Steve V Fox; Richard L Kraus; Scott M Doran; Thomas M Connolly; Cuyue Tang; Jeanine E Ballard; Yuhsin Kuo; Emily D Adarayan; Thomayant Prueksaritanont; Matthew M Zrada; Michael J Marino; Valerie Kuzmick Graufelds; Anthony G DiLella; Ian J Reynolds; Hugo M Vargas; Patricia B Bunting; Richard F Woltmann; Michael M Magee; Kenneth S Koblan; John J Renger
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Journal of medicinal chemistry 2008;51(20):6471-7.
2008: Jana A Lewis; R Nathan Daniels; Craig W Lindsley
Total synthesis of Ciliatamides A-C: stereochemical revision and the natural product-guided synthesis of unnatural analogs.
Organic letters 2008;10(20):4545-8.
2008: Nicole R Miller; R Nathan Daniels; Thomas M Bridges; Ashley E Brady; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
Bioorganic & medicinal chemistry letters 2008;18(20):5443-7.
2008: Thomas M Bridges; Ashley E Brady; J Phillip Kennedy; R Nathan Daniels; Nicole R Miller; Kwango Kim; Micah L Breininger; Patrick R Gentry; John T Brogan; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
Bioorganic & medicinal chemistry letters 2008;18(20):5439-42.
2008: Colleen M Niswender; Evan P Lebois; Qingwei Luo; Kwangho Kim; Hubert Muchalski; Huiyong Yin; P Jeffrey Conn; Craig W Lindsley
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2008;18(20):5626-30.
2008: Carrie K Jones; Ashley E Brady; Albert A Davis; Zixiu Xiang; Michael Bubser; Mohammed Noor Tantawy; Alexander S Kane; Thomas M Bridges; J Phillip Kennedy; Stefania R Bradley; Todd E Peterson; M Sib Ansari; Ronald M Baldwin; Robert M Kessler; Ariel Deutch; James J Lah; Allan Levey; Craig W Lindsley; P Jeffrey Conn
Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2008;28(41):10422-33.
2008: J Phillip Kennedy; John T Brogan; Craig W Lindsley
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.
Journal of natural products 2008;71(10):1783-6.
2008: Thomas M Bridges; Craig W Lindsley
G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms.
ACS chemical biology 2008;3(9):530-41.
2008: R Nathan Daniels; Olugbeminiyi O Fadeyi; Craig W Lindsley
A new catalytic Cu(II)/sparteine oxidant system for beta,beta-phenolic couplings of styrenyl phenols: synthesis of carpanone and unnatural analogs.
Organic letters 2008;10(18):4097-100.
2008: Kwangho Kim; Nicole R Miller; Gary A Sulikowski; Craig W Lindsley
A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.
Bioorganic & medicinal chemistry letters 2008;18(16):4467-9.
2008: Sameer Sharma; Alice L Rodriguez; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Bioorganic & medicinal chemistry letters 2008;18(14):4098-101.
2008: William D Shipe; James C Barrow; Zhi-Qiang Yang; Craig W Lindsley; F Vivien Yang; Kelly-Ann S Schlegel; Youheng Shu; Kenneth E Rittle; Mark G Bock; George D Hartman; Cuyue Tang; Jeanine E Ballard; Yuhsin Kuo; Emily D Adarayan; Thomayant Prueksaritanont; Matthew M Zrada; Victor N Uebele; Cindy E Nuss; Thomas M Connolly; Scott M Doran; Steven V Fox; Richard L Kraus; Michael J Marino; Valerie Kuzmick Graufelds; Hugo M Vargas; Patricia B Bunting; Martha Hasbun-Manning; Rose M Evans; Kenneth S Koblan; John Renger
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Journal of medicinal chemistry 2008;51(13):3692-5.
2008: Jana A Lewis; Evan P Lebois; Craig W Lindsley
Allosteric modulation of kinases and GPCRs: design principles and structural diversity.
Current opinion in chemical biology 2008;12(3):269-80.
2008: J Phillip Kennedy; Lyndsey Williams; Thomas M Bridges; R Nathan Daniels; David Weaver; Craig W Lindsley
Application of combinatorial chemistry science on modern drug discovery.
Journal of combinatorial chemistry 2008;10(3):345-54.
2008: P Jeffrey Conn; Carol A Tamminga; Darryle D Schoepp; Craig W Lindsley
Schizophrenia: moving beyond monoamine antagonists.
Molecular interventions 2008;8(2):99-107.
2008: Zhizhen Zeng; Julie A O'Brien; Wei Lemaire; Stacy S O'Malley; Patricia J Miller; Zhijian Zhao; Michael A Wallace; Conrad Raab; Craig W Lindsley; Cyrille Sur; David L Williams
A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies.
Nuclear medicine and biology 2008;35(3):315-25.
2008: Craig W Lindsley; Stanley Barnett; Mark E Layton; Mark T Bilodeau
The PI3K/Akt pathway: recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors.
Current cancer drug targets 2008;8(1):7-18.
2008: L Michelle Lewis; Douglas Sheffler; Richard Williams; Thomas M Bridges; J Phillip Kennedy; J T Brogan; Matthew J Mulder; Lyndsey Williams; Natalia T Nalywajko; Colleen M Niswender; Charles D Weaver; P Jeffrey Conn; Craig W Lindsley
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Bioorganic & medicinal chemistry letters 2008;18(3):885-90.
2008: Zhijian Zhao; Scott E Wolkenberg; Philip E J Sanderson; Meiqing Lu; Vandna Munshi; Gregory Moyer; Meizhen Feng; Anthony V Carella; Linda T Ecto; Lori Gabryelski; Ming-Tain Lai; Sridar G Prasad; Youwei Yan; Georgia B McGaughey; Michael D Miller; Craig W Lindsley; George D Hartman; Joseph P Vacca; Theresa M Williams
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Bioorganic & medicinal chemistry letters 2008;18(2):554-9.
2008: Craig W Lindsley
Molecule of the month. The 'skinny' on CB1 antagonists/inverse agonists: controversial obesity drugs will not go to FDA for approval.
Current topics in medicinal chemistry 2008;8(17):1553.
2008: Craig W Lindsley
Tumor necrosis factor (TNF) blockers ignite FDA inquiry over cancer concerns.
Current topics in medicinal chemistry 2008;8(13):1158.
2008: Craig W Lindsley
Molecule of the month.
Current topics in medicinal chemistry 2008;8(12):1100.
2008: Craig W Lindsley
Is Zetia a 'do nothing' drug?
Current topics in medicinal chemistry 2008;8(5):434.
2008: Ashley L Thomas; Craig W Lindsley
Molecule of the month. Overcoming resistance.
Current topics in medicinal chemistry 2008;8(1):62.
2008: Zhijian Zhao; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Hans E Huber; Mark E Duggan; Craig W Lindsley
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Bioorganic & medicinal chemistry letters 2008;18(1):49-53.
2007: Zhijian Zhao; David D Wisnoski; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Marion Wittman; Sookhee N Ha; Hervé Schaffhauser; Cyrille Sur; Douglas J Pettibone; Mark E Duggan; P Jeffrey Conn; George D Hartman; Craig W Lindsley
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Bioorganic & medicinal chemistry letters 2007;17(5):1386-91.
2007: Craig W Lindsley; David Weaver; Carrie Jones; Lawrence J Marnett; P Jeffrey Conn
Preclinical drug discovery research and training at Vanderbilt.
ACS chemical biology 2007;2(1):17-20.
2007: Craig W Lindsley; Stanley Barnett; Melissa Yaroschak; Mark T Bilodeau; Mark E Layton
Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors.
Current topics in medicinal chemistry 2007;7(14):1349-63.
2007: R Nathan Daniels; Craig W Lindsley
A new, non-SSRI mechanism of action for Prozac.
Current topics in medicinal chemistry 2007;7(10):1039.
2007: Anna S Dudkina; Craig W Lindsley
Small molecule protein-protein inhibitors for the p53-MDM2 interaction.
Current topics in medicinal chemistry 2007;7(10):952-60.
2007: Craig W Lindsley
Emerging from the shadow of Vioxx.
Current topics in medicinal chemistry 2007;7(7):739.
2006: Zhijian Zhao; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Douglas J Pettibone; Philip R Tiller; Sheri Smith; George D Hartman; Scott E Wolkenberg; Craig W Lindsley
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Bioorganic & medicinal chemistry letters 2006;16(23):5968-72.
2006: Kausik K Nanda; M Brad Nolt; Matthew J Cato; Stefanie A Kane; Laszlo Kiss; Robert H Spencer; Jixin Wang; Joseph J Lynch; christopher regan; Gary L Stump; Bing Li; Rebecca White; Suzie Yeh; Michael J Bogusky; Mark T Bilodeau; Christopher Dinsmore; Craig W Lindsley; George D Hartman; Scott E Wolkenberg; Wes Trotter
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Bioorganic & medicinal chemistry letters 2006;16(22):5897-901.
2006: Scott E Wolkenberg; Zhijian Zhao; Marianna Kapitskaya; Andrea L Webber; Konstantin Petrukhin; Yui S Tang; Dennis C Dean; George D Hartman; Craig W Lindsley
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Bioorganic & medicinal chemistry letters 2006;16(19):5001-4.
2006: Craig W Lindsley; Zhijian Zhao; William H Leister; Julie O'Brien; Wei Lemaire; David L Williams; Tsing-Bau Chen; Raymond S L Chang; Maryann Burno; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Nancy N Tsou; Mark E Duggan; P Jeffrey Conn; George D Hartman
Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides.
ChemMedChem 2006;1(8):807-11.
2006: Cynthia D Jesudason; Lisa S Beavers; Jeffrey W Cramer; Joelle Dill; Don R Finley; Craig W Lindsley; F Craig Stevens; Robert A Gadski; Samuel W Oldham; Richard T Pickard; Christopher S Siedem; Dana K Sindelar; Ajay Singh; Brian M Watson; Philip A Hipskind
Synthesis and SAR of novel histamine H3 receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(13):3415-8.
2006: Craig W Lindsley; Scott E Wolkenberg; Gene G Kinney
Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors.
Current topics in medicinal chemistry 2006;6(17):1883-96.
2006: Craig W Lindsley; William D Shipe; Scott E Wolkenberg; Cory R Theberge; David L Williams; Cyrille Sur; Gene G Kinney
Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia.
Current topics in medicinal chemistry 2006;6(8):771-85.
2005: Donghwa Kim; George Z Cheng; Craig W Lindsley; Hua Yang; Jin Q Cheng
Targeting the phosphatidylinositol-3 kinase/Akt pathway for the treatment of cancer.
Current opinion in investigational drugs (London, England : 2000) 2005;6(12):1250-8.
2005: Jin Q Cheng; Craig W Lindsley; George Z Cheng; Hua Yang; Santo V Nicosia
The Akt/PKB pathway: molecular target for cancer drug discovery.
Oncogene 2005;24(50):7482-92.
2005: Scott E Wolkenberg; William D Shipe; Craig W Lindsley; James P Guare; Joseph M Pawluczyk
Applications of microwave-assisted organic synthesis on the multigram scale.
Current opinion in drug discovery & development 2005;8(6):701-8.
2005: William D Shipe; Scott E Wolkenberg; David L Williams; Craig W Lindsley
Recent advances in positive allosteric modulators of metabotropic glutamate receptors.
Current opinion in drug discovery & development 2005;8(4):449-57.
2005: Gene G Kinney; Julie A O'Brien; Wei Lemaire; Maryann Burno; Denise J Bickel; Michelle K Clements; Tsing-Bau Chen; David D Wisnoski; Craig W Lindsley; Philip R Tiller; Sheri Smith; Marlene A Jacobson; Cyrille Sur; Mark E Duggan; Douglas J Pettibone; P Jeffrey Conn; David L Williams
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.
The Journal of pharmacology and experimental therapeutics 2005;313(1):199-206.
2005: Zhijian Zhao; William H Leister; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Joel R Huff; Hans E Huber; Mark E Duggan; Craig W Lindsley
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(4):905-9.
2005: Deborah DeFeo-Jones; Stanley Barnett; Sheng Fu; Paula J Hancock; Kathleen M Haskell; Karen Leander; Elizabeth McAvoy; Ronald G Robinson; Mark E Duggan; Craig W Lindsley; Zhijian Zhao; Hans E Huber; Raymond E Jones
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.
Molecular cancer therapeutics 2005;4(2):271-9.
2005: Craig W Lindsley; Zhijian Zhao; William H Leister; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Joel R Huff; Hans E Huber; Mark E Duggan
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(3):761-4.
2005: David L Williams; Craig W Lindsley
Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).
Current topics in medicinal chemistry 2005;5(9):825-46.
2005: Bradley P Feuston; Subhas J Chakravorty; John F Conway; J Christopher Culberson; Joseph Forbes; Bryan Kraker; Patricia A Lennon; Craig W Lindsley; Georgia B McGaughey; Ralph T Mosley; Robert P Sheridan; Mario Valenciano; Simon K Kearsley
Web enabling technology for the design, enumeration, optimization and tracking of compound libraries.
Current topics in medicinal chemistry 2005;5(8):773-83.
2005: Stanley Barnett; Mark T Bilodeau; Craig W Lindsley
The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation.
Current topics in medicinal chemistry 2005;5(2):109-25.
2004: Craig W Lindsley; David D Wisnoski; William H Leister; Julie A O'Brien; Wei Lemaire; David L Williams; Maryann Burno; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Mark E Duggan; George D Hartman; P Jeffrey Conn; Joel R Huff
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Journal of medicinal chemistry 2004;47(24):5825-8.
2004: Craig W Lindsley
Mastering medicinal chemistry: strategies, issues and success stories.
Drug discovery today 2004;9(16):695-6.
2004: Julie A O'Brien; Wei Lemaire; Marion Wittmann; Marlene A Jacobson; Sookhee N Ha; David D Wisnoski; Craig W Lindsley; Hervé Schaffhauser; Blake Rowe; Cyrille Sur; Mark E Duggan; Douglas J Pettibone; P Jeffrey Conn; David L Williams
A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.
The Journal of pharmacology and experimental therapeutics 2004;309(2):568-77.
2004: Scott E Wolkenberg; David D Wisnoski; William H Leister; Yi Wang; Zhijian Zhao; Craig W Lindsley
Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation.
Organic letters 2004;6(9):1453-6.
2003: David L Williams; Julie A O'Brien; Wei Lemaire; Tsing-Bau Chen; Raymond S L Chang; Marlene A Jacobson; Sookhee N Ha; David D Wisnoski; Craig W Lindsley; Cyrille Sur; Mark E Duggan; Douglas J Pettibone; P Jeffrey Conn
Difference in mGluR5 interaction between positive allosteric modulators from two structural classes.
Annals of the New York Academy of Sciences 2003;1003():481-4.
2003: Julie A O'Brien; Wei Lemaire; Tsing-Bau Chen; Raymond S L Chang; Marlene A Jacobson; Sookhee N Ha; Craig W Lindsley; Hervé Schaffhauser; Cyrille Sur; Douglas J Pettibone; P Jeffrey Conn; David L Williams
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
Molecular pharmacology 2003;64(3):731-40.
2003: William Leister; Kimberly Strauss; David Wisnoski; Zhijian Zhao; Craig W Lindsley
Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries.
Journal of combinatorial chemistry 2003;5(3):322-9.
2001: John Tallarico; K M Depew; Henry E Pelish; Nick J Westwood; Craig W Lindsley; Matthew D Shair; Stuart L Schreiber; Michael A Foley
An alkylsilyl-tethered, high-capacity solid support amenable to diversity-oriented synthesis for one-bead, one-stock solution chemical genetics.
Journal of combinatorial chemistry 2001;3(3):312-8.