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Said Sebti
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71
Hamilton, Andrew
31
Blaskovich, Michelle
21
Qian, Yimin
16
Ohkanda, Junko
15
Lazo, John
12
Vogt, Andreas
10
Coppola, Domenico
8
Adnane, Jalila
8
Rosenbloom, Joel
7
Sun, Jiazhi
7
Favre, Gilles
7
Mcguire, Terence
6
Gelb, Michael
6
Carrico, Dora
6
Van Voorhis, Wesley
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All Publications
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2009: Hong David S; Sebti Said M; Newman Robert A; Blaskovich Michelle A; Ye Lei; Gagel Robert F; Moulder Stacy; Wheler Jennifer J; Naing Aung; Tannir Nizar M; Ng Chaan S; Sherman Steven I; El Naggar Adel K; Khan Rabia; Trent Jon; Wright John J; Kurzrock Razelle
Phase I trial of a combination of the multikinase inhibitor sorafenib and the farnesyltransferase inhibitor tipifarnib in advanced malignancies.
Clinical cancer research : an official journal of the American Association for Cancer Research 2009;15(22):7061-8.
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2009: Sparano Joseph A; Moulder Stacy; Kazi Aslamuzzaman; Coppola Domenico; Negassa Abdissa; Vahdat Linda; Li Tianhong; Pellegrino Christine; Fineberg Susan; Munster Pam; Malafa Mokenge; Lee David; Hoschander Shira; Hopkins Una; Hershman Dawn; Wright John J; Kleer Celina; Merajver Sofia; Sebti Said M
Phase II trial of tipifarnib plus neoadjuvant doxorubicin-cyclophosphamide in patients with clinical stage IIB-IIIC breast cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 2009;15(8):2942-8.
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2009: Kazi Aslamuzzaman; Carie Adam; Blaskovich Michelle A; Bucher Cynthia; Thai Van; Moulder Stacy; Peng Hairuo; Carrico Dora; Pusateri Erin; Pledger Warren J; Berndt Norbert; Hamilton Andrew; Sebti Saïd M
Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy.
Molecular and cellular biology 2009;29(8):2254-63.
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2009: Hast Michael A; Fletcher Steven; Cummings Christopher G; Pusateri Erin E; Blaskovich Michelle A; Rivas Kasey; Gelb Michael H; Van Voorhis Wesley C; Sebti Said M; Hamilton Andrew D; Beese Lorena S
Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Chemistry & biology 2009;16(2):181-92.
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2009: Kayser-Bricker Katherine J; Glenn Matthew P; Lee Sang Hoon; Sebti Said M; Cheng Jin Q; Hamilton Andrew D
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Bioorganic & medicinal chemistry 2009;17(4):1764-71.
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2008: Fletcher Steven; Cummings Christopher G; Rivas Kasey; Katt William P; Hornéy Carrie; Buckner Frederick S; Chakrabarti Debopam; Sebti Saïd M; Gelb Michael H; Van Voorhis Wesley C; Hamilton Andrew D
Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.
Journal of medicinal chemistry 2008;51(17):5176-97.
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2008: Gustafsdottir Sigrun M; Wennström Stefan; Fredriksson Simon; Schallmeiner Edith; Hamilton Andrew D; Sebti Said M; Landegren Ulf
Use of proximity ligation to screen for inhibitors of interactions between vascular endothelial growth factor A and its receptors.
Clinical chemistry 2008;54(7):1218-25.
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2008: Kinkade Rebecca; Dasgupta Piyali; Carie Adam; Pernazza Daniele; Carless Melanie; Pillai Smitha; Lawrence Nicholas; Sebti Said M; Chellappan Srikumar
A small molecule disruptor of Rb/Raf-1 interaction inhibits cell proliferation, angiogenesis, and growth of human tumor xenografts in nude mice.
Cancer research 2008;68(10):3810-8.
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2008: Kurzrock Razelle; Kantarjian Hagop M; Blascovich Michelle A; Bucher Cindy; Verstovsek Srdan; Wright John J; Pilat Susan R; Cortes Jorge E; Estey Elihu H; Giles Francis J; Beran Miloslav; Sebti Said M
Phase I study of alternate-week administration of tipifarnib in patients with myelodysplastic syndrome.
Clinical cancer research : an official journal of the American Association for Cancer Research 2008;14(2):509-14.
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2007: Siddiquee Khandaker A Z; Gunning Patrick T; Glenn Matthew; Katt William P; Zhang Shumin; Schrock Christopher; Sebti Said M; Jove Richard; Hamilton Andrew D; Turkson James
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.
ACS chemical biology 2007;2(12):787-98.
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2007: Falsetti Samuel C; Wang De-an; Peng Hairuo; Carrico Dora; Cox Adrienne D; Der Channing J; Hamilton Andrew D; Sebti Saïd M
Geranylgeranyltransferase I inhibitors target RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth.
Molecular and cellular biology 2007;27(22):8003-14.
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2007: Siddiquee Khandaker; Zhang Shumin; Guida Wayne C; Blaskovich Michelle A; Greedy Benjamin; Lawrence Harshani R; Yip M L Richard; Jove Richard; McLaughlin Mark M; Lawrence Nicholas J; Sebti Said M; Turkson James
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.
Proceedings of the National Academy of Sciences of the United States of America 2007;104(18):7391-6.
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2007: Epifano Francesco; Curini Massimo; Genovese Salvatore; Blaskovich Michelle; Hamilton Andrew; Sebti Said M
Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I.
Bioorganic & medicinal chemistry letters 2007;17(9):2639-42.
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2007: Carie A E; Sebti S M
A chemical biology approach identifies a beta-2 adrenergic receptor agonist that causes human tumor regression by blocking the Raf-1/Mek-1/Erk1/2 pathway.
Oncogene 2007;26(26):3777-88.
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2007: Gunning Patrick T; Katt William P; Glenn Matthew; Siddiquee Khandaker; Kim Joon S; Jove Richard; Sebti Saïd M; Turkson James; Hamilton Andrew D
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
Bioorganic & medicinal chemistry letters 2007;17(7):1875-8.
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2007: Kayser Katherine J; Glenn Matthew P; Sebti Said M; Cheng Jin Q; Hamilton Andrew D
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.
Bioorganic & medicinal chemistry letters 2007;17(7):2068-73.
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2007: Delarue F L; Adnane J; Joshi B; Blaskovich M A; Wang D-A; Hawker J; Bizouarn F; Ohkanda J; Zhu K; Hamilton A D; Chellappan S; Sebti S M
Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter.
Oncogene 2007;26(5):633-40.
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2006: Hu Baoli; Gilkes Daniele M; Farooqi Bilal; Sebti Said M; Chen Jiandong
MDMX overexpression prevents p53 activation by the MDM2 inhibitor Nutlin.
The Journal of biological chemistry 2006;281(44):33030-5.
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2006: Glenn Matthew P; Chang Sung-Youn; Hornéy Carrie; Rivas Kasey; Yokoyama Kohei; Pusateri Erin E; Fletcher Steven; Cummings Christopher G; Buckner Frederick S; Pendyala Prakash R; Chakrabarti Debopam; Sebti Saïd M; Gelb Michael; Van Voorhis Wesley C; Hamilton Andrew D
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.
Journal of medicinal chemistry 2006;49(19):5710-27.
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2006: Tang Dongjiang; Park Ho-Jin; Georgescu Serban P; Sebti Saïd M; Hamilton Andrew D; Galper Jonas B
Simvastatin potentiates tumor necrosis factor alpha-mediated apoptosis of human vascular endothelial cells via the inhibition of the geranylgeranylation of RhoA.
Life sciences 2006;79(15):1484-92.
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2006: Chen Liwei; Sung Shen-Shu; Yip M L Richard; Lawrence Harshani R; Ren Yuan; Guida Wayne C; Sebti Said M; Lawrence Nicholas J; Wu Jie
Discovery of a novel shp2 protein tyrosine phosphatase inhibitor.
Molecular pharmacology 2006;70(2):562-70.
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2006: Sparano Joseph A; Moulder Stacy; Kazi Aslamuzzaman; Vahdat Linda; Li Tianhong; Pellegrino Christine; Munster Pam; Malafa Mokenge; Lee David; Hoschander Shira; Hopkins Una; Hershman Dawn; Wright John J; Sebti Said M
Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2006;24(19):3013-8.
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2006: Zhou Huchen; Wang De-an; Baldini Laura; Ennis Eileen; Jain Rishi; Carie Adam; Sebti Saïd M; Hamilton Andrew D
Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation.
Organic & biomolecular chemistry 2006;4(12):2376-86.
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2006: Peng Hairuo; Carrico Dora; Thai Van; Blaskovich Michelle; Bucher Cynthia; Pusateri Erin E; Sebti Said M; Hamilton Andrew D
Synthesis and evaluation of potent, highly-selective, 3-aryl-piperazinone inhibitors of protein geranylgeranyltransferase-I.
Organic & biomolecular chemistry 2006;4(9):1768-84.
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2006: Donapaty Sreenivasa; Louis Somaja; Horvath Elizabeth; Kun Jiang; Sebti Said M; Malafa Mokenge P
RRR-alpha-tocopherol succinate down-regulates oncogenic Ras signaling.
Molecular cancer therapeutics 2006;5(2):309-16.
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2006: Ohkanda Junko; Strickland Corey L; Blaskovich Michelle A; Carrico Dora; Lockman Jeffrey W; Vogt Andreas; Bucher Cynthia J; Sun Jiazhi; Qian Yimin; Knowles David; Pusateri Erin E; Sebti Saïd M; Hamilton Andrew D
Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.
Organic & biomolecular chemistry 2006;4(3):482-92.
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2005: Guida Wayne C; Hamilton Andrew D; Crotty Justin W; Sebti Saïd M
Protein farnesyltransferase: flexible docking studies on inhibitors using computational modeling.
Journal of computer-aided molecular design 2005;19(12):871-85.
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2005: Takahashi Yoshinori; Karbowski Mariusz; Yamaguchi Hirohito; Kazi Aslamuzzaman; Wu Jie; Sebti Saïd M; Youle Richard J; Wang Hong-Gang
Loss of Bif-1 suppresses Bax/Bak conformational change and mitochondrial apoptosis.
Molecular and cellular biology 2005;25(21):9369-82.
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2005: Nefedova Yulia; Nagaraj Srinivas; Rosenbauer Amsler; Muro-Cacho Carlos; Sebti Said M; Gabrilovich Dmitry I
Regulation of dendritic cell differentiation and antitumor immune response in cancer by pharmacologic-selective inhibition of the janus-activated kinase 2/signal transducers and activators of transcription 3 pathway.
Cancer research 2005;65(20):9525-35.
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2005: Nefedova Yulia; Cheng Pingyan; Gilkes Daniele; Blaskovich Michelle; Beg Amer A; Sebti Said M; Gabrilovich Dmitry I
Activation of dendritic cells via inhibition of Jak2/STAT3 signaling.
Journal of immunology (Baltimore, Md. : 1950) 2005;175(7):4338-46.
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2005: Cloughesy Timothy F; Kuhn John; Robins H Ian; Abrey Lauren; Wen Patrick; Fink Karen; Lieberman Frank S; Mehta Minesh; Chang Susan; Yung Alfred; DeAngelis Lisa; Schiff David; Junck Larry; Groves Morris; Paquette Steve; Wright John; Lamborn Kathleen; Sebti Said M; Prados Michael
Phase I trial of tipifarnib in patients with recurrent malignant glioma taking enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2005;23(27):6647-56.
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2005: Glenn Matthew P; Chang Sung-Youn; Hucke Oliver; Verlinde Christophe L M J; Rivas Kasey; Hornéy Carrie; Yokoyama Kohei; Buckner Frederick S; Pendyala Prakash R; Chakrabarti Debopam; Gelb Michael; Van Voorhis Wesley C; Sebti Saïd M; Hamilton Andrew D
Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites.
Angewandte Chemie (International ed. in English) 2005;44(31):4903-6.
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2005: Yin Hang; Lee Gui-In; Sedey Kristine A; Kutzki Olaf; Park Hyung Soon; Orner Brendan P; Ernst Justin T; Wang Hong-Gang; Sebti Said M; Hamilton Andrew D
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL.
Journal of the American Chemical Society 2005;127(29):10191-6.
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2005: Sun Jiazhi; Wang De-An; Jain Rishi K; Carie Adam; Paquette Steve; Ennis Eileen; Blaskovich Michelle A; Baldini Laura; Coppola Domenico; Hamilton Andrew D; Sebti Saïd M
Inhibiting angiogenesis and tumorigenesis by a synthetic molecule that blocks binding of both VEGF and PDGF to their receptors.
Oncogene 2005;24(29):4701-9.
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2005: Zhu Kuichun; Gerbino Elvira; Beaupre Darrin M; Mackley Paul A; Muro-Cacho Carlos; Beam Craig; Hamilton Andrew D; Lichtenheld Mathias G; Kerr William G; Dalton William; Alsina Melissa; Sebti Saïd M
Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.
Blood 2005;105(12):4759-66.
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2005: Sun Jiazhi; Blaskovich Michelle A; Jove Richard; Livingston Sandra K; Coppola Domenico; Sebti Saïd M
Cucurbitacin Q: a selective STAT3 activation inhibitor with potent antitumor activity.
Oncogene 2005;24(20):3236-45.
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2005: Wang De-An; Sebti Said M
Palmitoylated cysteine 192 is required for RhoB tumor-suppressive and apoptotic activities.
The Journal of biological chemistry 2005;280(19):19243-9.
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2005: Sebti Saïd M
Protein farnesylation: implications for normal physiology, malignant transformation, and cancer therapy.
Cancer cell 2005;7(4):297-300.
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2005: Yin Hang; Lee Gui-In; Sedey Kristine A; Rodriguez Johanna M; Wang Hong-Gang; Sebti Said M; Hamilton Andrew D
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
Journal of the American Chemical Society 2005;127(15):5463-8.
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2005: Yin Hang; Lee Gui-in; Park Hyung Soon; Payne Gregory A; Rodriguez Johanna M; Sebti Said M; Hamilton Andrew D
Terphenyl-based helical mimetics that disrupt the p53/HDM2 interaction.
Angewandte Chemie (International ed. in English) 2005;44(18):2704-7.
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2005: Mazières Julien; Tillement Vanessa; Allal Cuider; Clanet Carine; Bobin Lisbeth; Chen Zhi; Sebti Said M; Favre Gilles; Pradines Anne
Geranylgeranylated, but not farnesylated, RhoB suppresses Ras transformation of NIH-3T3 cells.
Experimental cell research 2005;304(2):354-64.
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2005: Carrico Dora; Blaskovich Michelle A; Bucher Cynthia J; Sebti Saïd M; Hamilton Andrew D
Design, synthesis, and evaluation of potent and selective benzoyleneurea-based inhibitors of protein geranylgeranyltransferase-I.
Bioorganic & medicinal chemistry 2005;13(3):677-88.
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2005: Woo Je-Tae; Nakagawa Hiroshi; Krecic Annette M; Nagai Kazuo; Hamilton Andrew D; Sebti Said M; Stern Paula H
Inhibitory effects of mevastatin and a geranylgeranyl transferase I inhibitor (GGTI-2166) on mononuclear osteoclast formation induced by receptor activator of NF kappa B ligand (RANKL) or tumor necrosis factor-alpha (TNF-alpha).
Biochemical pharmacology 2005;69(1):87-95.
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2004: Carrico Dora; Ohkanda Junko; Kendrick Howard; Yokoyama Kohei; Blaskovich Michelle A; Bucher Cynthia J; Buckner Frederick S; Van Voorhis Wesley C; Chakrabarti Debopam; Croft Simon L; Gelb Michael H; Sebti Saïd M; Hamilton Andrew D
In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability.
Bioorganic & medicinal chemistry 2004;12(24):6517-26.
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2004: Dasgupta Piyali; Sun Jiazhi; Wang Sheng; Fusaro Gina; Betts Vicki; Padmanabhan Jaya; Sebti Saïd M; Chellappan Srikumar P
Disruption of the Rb--Raf-1 interaction inhibits tumor growth and angiogenesis.
Molecular and cellular biology 2004;24(21):9527-41.
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2004: Yang Lin; Dan Han C; Sun Mei; Liu Qiyuan; Sun Xia-meng; Feldman Richard I; Hamilton Andrew D; Polokoff Mark; Nicosia Santo V; Herlyn Meenhard; Sebti Said M; Cheng Jin Q
Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt.
Cancer research 2004;64(13):4394-9.
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2004: Sun Jiazhi; Blaskovich Michelle A; Jain Rishi K; Delarue Frederic; Paris Daniel; Brem Steven; Wotoczek-Obadia Marguerite; Lin Qing; Coppola Domenico; Choi Kihang; Mullan Michael; Hamilton Andrew D; Sebti Saïd M
Blocking angiogenesis and tumorigenesis with GFA-116, a synthetic molecule that inhibits binding of vascular endothelial growth factor to its receptor.
Cancer research 2004;64(10):3586-92.
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2004: Alsina Melissa; Fonseca Rafael; Wilson Edward F; Belle A Nelida; Gerbino Elvira; Price-Troska Tammy; Overton Rose M; Ahmann Gregory; Bruzek Laura M; Adjei Alex A; Kaufmann Scott H; Wright John J; Sullivan Daniel; Djulbegovic Benjamin; Cantor Alan B; Greipp Philip R; Dalton William S; Sebti Saïd M
Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.
Blood 2004;103(9):3271-7.
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2004: Sebti Said M; Adjei Alex A
Farnesyltransferase inhibitors.
Seminars in oncology 2004;31(1 Suppl 1):28-39.
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2004: Jiang Kun; Delarue Frederic L; Sebti Saïd M
EGFR, ErbB2 and Ras but not Src suppress RhoB expression while ectopic expression of RhoB antagonizes oncogene-mediated transformation.
Oncogene 2004;23(5):1136-45.
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2004: Dan Han C; Jiang Kun; Coppola Domenico; Hamilton Andrew; Nicosia Santo V; Sebti Said M; Cheng Jin Q
Phosphatidylinositol-3-OH kinase/AKT and survivin pathways as critical targets for geranylgeranyltransferase I inhibitor-induced apoptosis.
Oncogene 2004;23(3):706-15.
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2004: Ohkanda Junko; Buckner Frederick S; Lockman Jeffrey W; Yokoyama Kohei; Carrico Dora; Eastman Richard; de Luca-Fradley Kate; Davies Wendy; Croft Simon L; Van Voorhis Wesley C; Gelb Michael H; Sebti Saïd M; Hamilton Andrew D
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.
Journal of medicinal chemistry 2004;47(2):432-45.
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2004: Paris Daniel; Townsend Kirk; Quadros Amita; Humphrey James; Sun Jiazhi; Brem Steven; Wotoczek-Obadia Marguerite; DelleDonne Anthony; Patel Nikunj; Obregon Demian F; Crescentini Robert; Abdullah Laila; Coppola Domenico; Rojiani Amyn M; Crawford Fiona; Sebti Saïd M; Mullan Michael
Inhibition of angiogenesis by Abeta peptides.
Angiogenesis 2004;7(1):75-85.
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2003: Zhu Kuichun; Hamilton Andrew D; Sebti Saïd M
Farnesyltransferase inhibitors as anticancer agents: current status.
Current opinion in investigational drugs (London, England : 2000) 2003;4(12):1428-35.
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2003: Sebti Saïd M; Der Channing J
Opinion: Searching for the elusive targets of farnesyltransferase inhibitors.
Nature reviews. Cancer 2003;3(12):945-51.
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2003: Sun Jiazhi; Ohkanda Junko; Coppola Domenico; Yin Hang; Kothare Mohit; Busciglio Brian; Hamilton Andrew D; Sebti Saïd M
Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.
Cancer research 2003;63(24):8922-9.
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2003: Kurzrock Razelle; Kantarjian Hagop M; Cortes Jorge E; Singhania Neil; Thomas Deborah A; Wilson Edward F; Wright John J; Freireich Emil J; Talpaz Moshe; Sebti Saïd M
Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting.
Blood 2003;102(13):4527-34.
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2003: Forsberg Maria; Blomgran Robert; Lerm Maria; Särndahl Eva; Sebti Said M; Hamilton Andrew; Stendahl Olle; Zheng Limin
Differential effects of invasion by and phagocytosis of Salmonella typhimurium on apoptosis in human macrophages: potential role of Rho-GTPases and Akt.
Journal of leukocyte biology 2003;74(4):620-9.
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2003: Zhang Zhongqiu; Wang Yian; Lantry Laura E; Kastens Elizabeth; Liu Gongjie; Hamilton Andrew D; Sebti Said M; Lubet Ronald A; You Ming
Farnesyltransferase inhibitors are potent lung cancer chemopreventive agents in A/J mice with a dominant-negative p53 and/or heterozygous deletion of Ink4a/Arf.
Oncogene 2003;22(40):6257-65.
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2003: Bordier Bruno B; Ohkanda Junko; Liu Ping; Lee So-Young; Salazar F H; Marion Patricia L; Ohashi Kazuo; Meuse Leonard; Kay Mark A; Casey John L; Sebti Said M; Hamilton Andrew D; Glenn Jeffrey S
In vivo antiviral efficacy of prenylation inhibitors against hepatitis delta virus.
The Journal of clinical investigation 2003;112(3):407-14.
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2003: Blaskovich Michelle A; Sun Jiazhi; Cantor Alan; Turkson James; Jove Richard; Sebti Saïd M
Discovery of JSI-124 (cucurbitacin I), a selective Janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine cancer cells in mice.
Cancer research 2003;63(6):1270-9.
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2003: Doisneau-Sixou Sophie F; Cestac Philippe; Chouini Sarah; Carroll Jason S; Hamilton Andrew D; Sebti Said M; Poirot Marc; Balaguer Patrick; Faye Jean-Charles; Sutherland Robert L; Favre Gilles
Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells.
Endocrinology 2003;144(3):989-98.
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2003: Mazzocca Antonio; Giusti Sabrina; Hamilton Andrew D; Sebti Said M; Pantaleo Pietro; Carloni Vinicio
Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines.
Molecular pharmacology 2003;63(1):159-66.
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2003: Sebti Saïd M
Blocked pathways: FTIs shut down oncogene signals.
The oncologist 2003;8 Suppl 3():30-8.
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2003: Ohkanda Junko; Blaskovich Michelle A; Sebti Saïd M; Hamilton Andrew D
The development of protein farnesyltransferase inhibitors as signaling-based anticancer agents.
Progress in cell cycle research 2003;5():211-7.
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2002: Jackson Rosalind J; Adnane Jalila; Coppola Domenico; Cantor Alan; Sebti Saïd M; Pledger W Jock
Loss of the cell cycle inhibitors p21(Cip1) and p27(Kip1) enhances tumorigenesis in knockout mouse models.
Oncogene 2002;21(55):8486-97.
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2002: Allal Cuider; Pradines Anne; Hamilton Andrew D; Sebti Said M; Favre Gilles
Farnesylated RhoB prevents cell cycle arrest and actin cytoskeleton disruption caused by the geranylgeranyltransferase I inhibitor GGTI-298.
Cell cycle (Georgetown, Tex.) 2002;1(6):430-7.
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2002: Adnane Jalila; Muro-Cacho Carlos; Mathews Linda; Sebti Said M; Muñoz-Antonia Teresita
Suppression of rho B expression in invasive carcinoma from head and neck cancer patients.
Clinical cancer research : an official journal of the American Association for Cancer Research 2002;8(7):2225-32.
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2002: Crespo N C; Delarue F; Ohkanda J; Carrico D; Hamilton A D; Sebti S M
The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status.
Cell death and differentiation 2002;9(7):702-9.
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2002: Li Xianwu; Liu Li; Tupper Joan C; Bannerman Douglas D; Winn Robert K; Sebti Said M; Hamilton Andrew D; Harlan John M
Inhibition of protein geranylgeranylation and RhoA/RhoA kinase pathway induces apoptosis in human endothelial cells.
The Journal of biological chemistry 2002;277(18):15309-16.
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2002: Walters Claire E; Pryce Gareth; Hankey Deborah J R; Sebti Said M; Hamilton Andrew D; Baker David; Greenwood John; Adamson Peter
Inhibition of Rho GTPases with protein prenyltransferase inhibitors prevents leukocyte recruitment to the central nervous system and attenuates clinical signs of disease in an animal model of multiple sclerosis.
Journal of immunology (Baltimore, Md. : 1950) 2002;168(8):4087-94.
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2002: Ohkanda Junko; Knowles David B; Blaskovich Michelle A; Sebti Said M; Hamilton Andrew D
Inhibitors of protein farnesyltransferase as novel anticancer agents.
Current topics in medicinal chemistry 2002;2(3):303-23.
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2002: Adnane Jalila; Seijo Edward; Chen Zhi; Bizouarn Francisco; Leal Martha; Sebti Said M; Muñoz-Antonia Teresita
RhoB, not RhoA, represses the transcription of the transforming growth factor beta type II receptor by a mechanism involving activator protein 1.
The Journal of biological chemistry 2002;277(10):8500-7.
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2002: Ohkanda Junko; Lockman Jeffrey W; Kothare Mohit A; Qian Yimin; Blaskovich Michelle A; Sebti Said M; Hamilton Andrew D
Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.
Journal of medicinal chemistry 2002;45(1):177-88.
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2001: Kucich U; Rosenbloom J C; Herrick D J; Abrams W R; Hamilton A D; Sebti S M; Rosenbloom J
Signaling events required for transforming growth factor-beta stimulation of connective tissue growth factor expression by cultured human lung fibroblasts.
Archives of biochemistry and biophysics 2001;395(1):103-12.
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2001: Delarue F L; Taylor B S; Sebti S M
Ras and RhoA suppress whereas RhoB enhances cytokine-induced transcription of nitric oxide synthase-2 in human normal liver AKN-1 cells and lung cancer A-549 cells.
Oncogene 2001;20(45):6531-7.
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2001: Finder J D; Petrus J L; Hamilton A; Villavicencio R T; Pitt B R; Sebti S M
Signal transduction pathways of IL-1beta-mediated iNOS in pulmonary vascular smooth muscle cells.
American journal of physiology. Lung cellular and molecular physiology 2001;281(4):L816-23.
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2001: Crespo N C; Ohkanda J; Yen T J; Hamilton A D; Sebti S M
The farnesyltransferase inhibitor, FTI-2153, blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells.
The Journal of biological chemistry 2001;276(19):16161-7.
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2001: Ohkanda J; Lockman J W; Yokoyama K; Gelb M H; Croft S L; Kendrick H; Harrell M I; Feagin J E; Blaskovich M A; Sebti S M; Hamilton A D
Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.
Bioorganic & medicinal chemistry letters 2001;11(6):761-4.
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2001: Sun J; Nam S; Lee C S; Li B; Coppola D; Hamilton A D; Dou Q P; Sebti S M
CEP1612, a dipeptidyl proteasome inhibitor, induces p21WAF1 and p27KIP1 expression and apoptosis and inhibits the growth of the human lung adenocarcinoma A-549 in nude mice.
Cancer research 2001;61(4):1280-4.
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2000: Sebti S M; Hamilton A D
Farnesyltransferase and geranylgeranyltransferase I inhibitors in cancer therapy: important mechanistic and bench to bedside issues.
Expert opinion on investigational drugs 2000;9(12):2767-82.
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2000: Adnane J; Bizouarn F A; Chen Z; Ohkanda J; Hamilton A D; Munoz-Antonia T; Sebti S M
Inhibition of farnesyltransferase increases TGFbeta type II receptor expression and enhances the responsiveness of human cancer cells to TGFbeta.
Oncogene 2000;19(48):5525-33.
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2000: Adnane J; Jackson R J; Nicosia S V; Cantor A B; Pledger W J; Sebti S M
Loss of p21WAF1/CIP1 accelerates Ras oncogenesis in a transgenic/knockout mammary cancer model.
Oncogene 2000;19(47):5338-47.
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2000: Blaskovich M A; Lin Q; Delarue F L; Sun J; Park H S; Coppola D; Hamilton A D; Sebti S M
Design of GFB-111, a platelet-derived growth factor binding molecule with antiangiogenic and anticancer activity against human tumors in mice.
Nature biotechnology 2000;18(10):1065-70.
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2000: Allal C; Favre G; Couderc B; Salicio S; Sixou S; Hamilton A D; Sebti S M; Lajoie-Mazenc I; Pradines A
RhoA prenylation is required for promotion of cell growth and transformation and cytoskeleton organization but not for induction of serum response element transcription.
The Journal of biological chemistry 2000;275(40):31001-8.
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2000: Cohen-Jonathan E; Muschel R J; Gillies McKenna W; Evans S M; Cerniglia G; Mick R; Kusewitt D; Sebti S M; Hamilton A D; Oliff A; Kohl N; Gibbs J B; Bernhard E J
Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS.
Radiation research 2000;154(2):125-32.
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2000: Rosenbloom J; Saitta B; Gaidarova S; Sandorfi N; Rosenbloom J C; Abrams W R; Hamilton A D; Sebti S M; Kucich U; Jimenez S A
Inhibition of type I collagen gene expression in normal and systemic sclerosis fibroblasts by a specific inhibitor of geranylgeranyl transferase I.
Arthritis and rheumatism 2000;43(7):1624-32.
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2000: Chen Z; Sun J; Pradines A; Favre G; Adnane J; Sebti S M
Both farnesylated and geranylgeranylated RhoB inhibit malignant transformation and suppress human tumor growth in nude mice.
The Journal of biological chemistry 2000;275(24):17974-8.
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2000: Kucich U; Rosenbloom J C; Shen G; Abrams W R; Hamilton A D; Sebti S M; Rosenbloom J
TGF-beta1 stimulation of fibronectin transcription in cultured human lung fibroblasts requires active geranylgeranyl transferase I, phosphatidylcholine-specific phospholipase C, protein kinase C-delta, and p38, but not erk1/erk2.
Archives of biochemistry and biophysics 2000;374(2):313-24.
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2000: Boota A; Johnson B; Lee K L; Blaskovich M A; Liu S X; Kagan V E; Hamilton A; Pitt B; Sebti S M; Davies P
Prenyltransferase inhibitors block superoxide production by pulmonary vascular smooth muscle.
American journal of physiology. Lung cellular and molecular physiology 2000;278(2):L329-34.
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2000: Carloni V; Pinzani M; Giusti S; Romanelli R G; Parola M; Bellomo G; Failli P; Hamilton A D; Sebti S M; Laffi G; Gentilini P
Tyrosine phosphorylation of focal adhesion kinase by PDGF is dependent on ras in human hepatic stellate cells.
Hepatology (Baltimore, Md.) 2000;31(1):131-40.
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2000: Lantry L E; Zhang Z; Yao R; Crist K A; Wang Y; Ohkanda J; Hamilton A D; Sebti S M; Lubet R A; You M
Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.
Carcinogenesis 2000;21(1):113-6.
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2000: Sebti S M; Hamilton A D
Inhibition of Rho GTPases using protein geranylgeranyltransferase I inhibitors.
Methods in enzymology 2000;325():381-8.
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1999: Qian Y; Marugan J J; Fossum R D; Vogt A; Sebti S M; Hamilton A D
Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors.
Bioorganic & medicinal chemistry 1999;7(12):3011-24.
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1999: Sun J; Blaskovich M A; Knowles D; Qian Y; Ohkanda J; Bailey R D; Hamilton A D; Sebti S M
Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.
Cancer research 1999;59(19):4919-26.
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1999: Cohen-Jonathan E; Toulas C; Ader I; Monteil S; Allal C; Bonnet J; Hamilton A D; Sebti S M; Daly-Schveitzer N; Favre G
The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS.
Radiation research 1999;152(4):404-11.
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1999: Vasudevan A; Qian Y; Vogt A; Blaskovich M A; Ohkanda J; Sebti S M; Hamilton A D
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
Journal of medicinal chemistry 1999;42(8):1333-40.
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1999: Sun J; Qian Y; Chen Z; Marfurt J; Hamilton A D; Sebti S M
The geranylgeranyltransferase I inhibitor GGTI-298 induces hypophosphorylation of retinoblastoma and partner switching of cyclin-dependent kinase inhibitors. A potential mechanism for GGTI-298 antitumor activity.
The Journal of biological chemistry 1999;274(11):6930-4.
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1998: Adnane J; Bizouarn F A; Qian Y; Hamilton A D; Sebti S M
p21(WAF1/CIP1) is upregulated by the geranylgeranyltransferase I inhibitor GGTI-298 through a transforming growth factor beta- and Sp1-responsive element: involvement of the small GTPase rhoA.
Molecular and cellular biology 1998;18(12):6962-70.
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1998: Kucich U; Rosenbloom J C; Shen G; Abrams W R; Blaskovich M A; Hamilton A D; Ohkanda J; Sebti S M; Rosenbloom J
Requirement for geranylgeranyl transferase I and acyl transferase in the TGF-beta-stimulated pathway leading to elastin mRNA stabilization.
Biochemical and biophysical research communications 1998;252(1):111-6.
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1998: Stark W W; Blaskovich M A; Johnson B A; Qian Y; Vasudevan A; Pitt B; Hamilton A D; Sebti S M; Davies P
Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells.
The American journal of physiology 1998;275(1 Pt 1):L55-63.
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1998: Bernhard E J; McKenna W G; Hamilton A D; Sebti S M; Qian Y; Wu J M; Muschel R J
Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes.
Cancer research 1998;58(8):1754-61.
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1998: Qian Y; Vogt A; Vasudevan A; Sebti S M; Hamilton A D
Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics.
Bioorganic & medicinal chemistry 1998;6(3):293-9.
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1997: Sebti S M; Hamilton A D
Anticancer activity of farnesyltransferase and geranylgeranyltransferase I inhibitors: prospects for drug development.
Expert opinion on investigational drugs 1997;6(11):1711-4.
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1997: Vogt A; Sun J; Qian Y; Hamilton A D; Sebti S M
The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner.
The Journal of biological chemistry 1997;272(43):27224-9.
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1997: Lerner E C; Zhang T T; Knowles D B; Qian Y; Hamilton A D; Sebti S M
Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines.
Oncogene 1997;15(11):1283-8.
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1997: Miquel K; Pradines A; Sun J; Qian Y; Hamilton A D; Sebti S M; Favre G
GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.
Cancer research 1997;57(10):1846-50.
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1997: Finder J D; Litz J L; Blaskovich M A; McGuire T F; Qian Y; Hamilton A D; Davies P; Sebti S M
Inhibition of protein geranylgeranylation causes a superinduction of nitric-oxide synthase-2 by interleukin-1beta in vascular smooth muscle cells.
The Journal of biological chemistry 1997;272(21):13484-8.
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1997: McGuire T F; Sebti S M
Geranylgeraniol potentiates lovastatin inhibition of oncogenic H-Ras processing and signaling while preventing cytotoxicity.
Oncogene 1997;14(3):305-12.
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1997: Sebti S M; Hamilton A D
Inhibition of Ras prenylation: a novel approach to cancer chemotherapy.
Pharmacology & therapeutics 1997;74(1):103-14.
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1997: Qian Y; Sebti S M; Hamilton A D
Farnesyltransferase as a target for anticancer drug design.
Biopolymers 1997;43(1):25-41.
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1996: Vogt A; Qian Y; McGuire T F; Hamilton A D; Sebti S M
Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts.
Oncogene 1996;13(9):1991-9.
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1996: McGuire T F; Qian Y; Vogt A; Hamilton A D; Sebti S M
Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation.
The Journal of biological chemistry 1996;271(44):27402-7.
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1996: Sebti S M; Hamilton A D
Rational design of Ras prenyltransferase inhibitors as potential anticancer drugs.
Biochemical Society transactions 1996;24(3):692-9.
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1996: Pei Z; Sebti S M
Cys102 and His398 are required for bleomycin-inactivating activity but not for hexamer formation of yeast bleomycin hydrolase.
Biochemistry 1996;35(33):10751-6.
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1996: Bernhard E J; Kao G; Cox A D; Sebti S M; Hamilton A D; Muschel R J; McKenna W G
The farnesyltransferase inhibitor FTI-277 radiosensitizes H-ras-transformed rat embryo fibroblasts.
Cancer research 1996;56(8):1727-30.
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1996: Xu X Q; McGuire T F; Blaskovich M A; Sebti S M; Romero G
Lovastatin inhibits the stimulation of mitogen-activated protein kinase by insulin in HIRcB fibroblasts.
Archives of biochemistry and biophysics 1996;326(2):233-7.
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1996: Qian Y; Vogt A; Sebti S M; Hamilton A D
Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors.
Journal of medicinal chemistry 1996;39(1):217-23.
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1996: Lazo J S; Sebti S M; Schellens J H
Bleomycin.
Cancer chemotherapy and biological response modifiers 1996;16():39-47.
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1995: Lerner E C; Qian Y; Blaskovich M A; Fossum R D; Vogt A; Sun J; Cox A D; Der C J; Hamilton A D; Sebti S M
Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes.
The Journal of biological chemistry 1995;270(45):26802-6.
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1995: Lerner E C; Qian Y; Hamilton A D; Sebti S M
Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor.
The Journal of biological chemistry 1995;270(45):26770-3.
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1995: Kauffmann R C; Qian Y; Vogt A; Sebti S M; Hamilton A D; Carthew R W
Activated Drosophila Ras1 is selectively suppressed by isoprenyl transferase inhibitors.
Proceedings of the National Academy of Sciences of the United States of America 1995;92(24):10919-23.
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1995: Sun J; Qian Y; Hamilton A D; Sebti S M
Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.
Cancer research 1995;55(19):4243-7.
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1995: Pei Z; Calmels T P; Creutz C E; Sebti S M
Yeast cysteine proteinase gene ycp1 induces resistance to bleomycin in mammalian cells.
Molecular pharmacology 1995;48(4):676-81.
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1995: Vogt A; Sun J; Qian Y; Tan-Chiu E; Hamilton A D; Sebti S M
Burkitt lymphoma Daudi cells contain two distinct farnesyltransferases with different divalent cation requirements.
Biochemistry 1995;34(38):12398-403.
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1995: Vogt A; Qian Y; Blaskovich M A; Fossum R D; Hamilton A D; Sebti S M
A non-peptide mimetic of Ras-CAAX: selective inhibition of farnesyltransferase and Ras processing.
The Journal of biological chemistry 1995;270(2):660-4.
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1994: McGuire T F; Xu X Q; Corey S J; Romero G G; Sebti S M
Lovastatin disrupts early events in insulin signaling: a potential mechanism of lovastatin's anti-mitogenic activity.
Biochemical and biophysical research communications 1994;204(1):399-406.
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1994: Weng W; Reynolds I J; Jani J P; Blaskovich M; Sebti S M; Davies P; Pitt B R
Desensitization of 5HT2 receptors by protein kinase C activation in distal pulmonary vascular smooth muscle cells in culture.
Microcirculation (New York, N.Y. : 1994) 1994;1(2):129-35.
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1994: Qian Y; Blaskovich M A; Saleem M; Seong C M; Wathen S P; Hamilton A D; Sebti S M
Design and structural requirements of potent peptidomimetic inhibitors of p21ras farnesyltransferase.
The Journal of biological chemistry 1994;269(17):12410-3.
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1994: Lazo J S; Sebti S M
Bleomycin.
Cancer chemotherapy and biological response modifiers 1994;15():44-50.
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1993: Nigam M; Seong C M; Qian Y; Hamilton A D; Sebti S M
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
The Journal of biological chemistry 1993;268(28):20695-8.
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1993: McGuire T F; Corey S J; Sebti S M
Lovastatin inhibits platelet-derived growth factor (PDGF) stimulation of phosphatidylinositol 3-kinase activity as well as association of p85 subunit to tyrosine-phosphorylated PDGF receptor.
The Journal of biological chemistry 1993;268(30):22227-30.
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1993: Lazo J S; Sebti S M
Bleomycins.
Cancer chemotherapy and biological response modifiers 1993;14():37-44.
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1992: Morris G; Mistry J S; Jani J P; Mignano J E; Sebti S M; Lazo J S
Neutralization of bleomycin hydrolase by an epitope-specific antibody.
Molecular pharmacology 1992;42(1):57-62.
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1992: Jani J P; Mistry J S; Morris G; Davies P; Lazo J S; Sebti S M
In vivo circumvention of human colon carcinoma resistance to bleomycin.
Cancer research 1992;52(10):2931-7.
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1992: Mistry J S; Jani J P; Morris G; Mujumdar R B; Reynolds I J; Sebti S M; Lazo J S
Synthesis and evaluation of fluoromycin: a novel fluorescence-labeled derivative of talisomycin S10b.
Cancer research 1992;52(3):709-18.
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1992: Jani J P; Mistry J S; Morris G; Lazo J S; Sebti S M
In vivo sensitization of human lung carcinoma to bleomycin by the cysteine proteinase inhibitor E-64.
Oncology research 1992;4(2):59-63.
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1991: Morris G; Mistry J S; Jani J P; Sebti S M; Lazo J S
Cysteine proteinase inhibitors and bleomycin-sensitive and -resistant cells.
Biochemical pharmacology 1991;41(11):1559-66.
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1991: Sebti S M; Tkalcevic G T; Jani J P
Lovastatin, a cholesterol biosynthesis inhibitor, inhibits the growth of human H-ras oncogene transformed cells in nude mice.
Cancer communications 1991;3(5):141-7.
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1991: Sebti S M; Jani J P; Mistry J S; Gorelik E; Lazo J S
Metabolic inactivation: a mechanism of human tumor resistance to bleomycin.
Cancer research 1991;51(1):227-32.
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1990: Mistry J S; Sebti S M; Lazo J S
Separation of bleomycins and their deamido metabolites by high-performance cation-exchange chromatography.
Journal of chromatography 1990;514(1):86-90.
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1990: Lazo J S; Hoyt D G; Sebti S M; Pitt B R
Bleomycin: a pharmacologic tool in the study of the pathogenesis of interstitial pulmonary fibrosis.
Pharmacology & therapeutics 1990;47(3):347-58.
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1989: Sebti S M; Mignano J E; Jani J P; Srimatkandada S; Lazo J S
Bleomycin hydrolase: molecular cloning, sequencing, and biochemical studies reveal membership in the cysteine proteinase family.
Biochemistry 1989;28(16):6544-8.
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1989: Sebti S M; DeLeon J C; Ma L T; Hecht S M; Lazo J S
Substrate specificity of bleomycin hydrolase.
Biochemical pharmacology 1989;38(1):141-7.
-
1988: Sebti S M; Lazo J S
Metabolic inactivation of bleomycin analogs by bleomycin hydrolase.
Pharmacology & therapeutics 1988;38(3):321-9.
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1987: Sebti S M; DeLeon J C; Lazo J S
Purification, characterization, and amino acid composition of rabbit pulmonary bleomycin hydrolase.
Biochemistry 1987;26(14):4213-9.
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