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Page 1
Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.
Diaz D, Ford KA, Hartley DP, Harstad EB, Cain GR, Achilles-Poon K, Nguyen T, Peng J, Zheng Z, Merchant M, Sutherlin DP, Gaudino JJ, Kaus R, Lewin-Koh SC, Choo EF, Liederer BM, Dambach DM. Diaz D, et al. Among authors: merchant m. Toxicol Appl Pharmacol. 2013 Jan 1;266(1):86-94. doi: 10.1016/j.taap.2012.10.026. Epub 2012 Nov 7. Toxicol Appl Pharmacol. 2013. PMID: 23142475
A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.
Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M. Lau T, et al. Among authors: merchant m. Cancer Res. 2013 May 15;73(10):3132-44. doi: 10.1158/0008-5472.CAN-12-4562. Epub 2013 Mar 28. Cancer Res. 2013. PMID: 23539443
PAK1 mediates pancreatic cancer cell migration and resistance to MET inhibition.
Zhou W, Jubb AM, Lyle K, Xiao Q, Ong CC, Desai R, Fu L, Gnad F, Song Q, Haverty PM, Aust D, Grützmann R, Romero M, Totpal K, Neve RM, Yan Y, Forrest WF, Wang Y, Raja R, Pilarsky C, de Jesus-Acosta A, Belvin M, Friedman LS, Merchant M, Jaffee EM, Zheng L, Koeppen H, Hoeflich KP. Zhou W, et al. Among authors: merchant m. J Pathol. 2014 Dec;234(4):502-13. doi: 10.1002/path.4412. Epub 2014 Oct 6. J Pathol. 2014. PMID: 25074413 Free PMC article.
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.
Blake JF, Burkard M, Chan J, Chen H, Chou KJ, Diaz D, Dudley DA, Gaudino JJ, Gould SE, Grina J, Hunsaker T, Liu L, Martinson M, Moreno D, Mueller L, Orr C, Pacheco P, Qin A, Rasor K, Ren L, Robarge K, Shahidi-Latham S, Stults J, Sullivan F, Wang W, Yin J, Zhou A, Belvin M, Merchant M, Moffat J, Schwarz JB. Blake JF, et al. Among authors: merchant m. J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7. J Med Chem. 2016. PMID: 27227380
Disruption of IRE1α through its kinase domain attenuates multiple myeloma.
Harnoss JM, Le Thomas A, Shemorry A, Marsters SA, Lawrence DA, Lu M, Chen YA, Qing J, Totpal K, Kan D, Segal E, Merchant M, Reichelt M, Ackerly Wallweber H, Wang W, Clark K, Kaufman S, Beresini MH, Laing ST, Sandoval W, Lorenzo M, Wu J, Ly J, De Bruyn T, Heidersbach A, Haley B, Gogineni A, Weimer RM, Lee D, Braun MG, Rudolph J, VanWyngarden MJ, Sherbenou DW, Gomez-Bougie P, Amiot M, Acosta-Alvear D, Walter P, Ashkenazi A. Harnoss JM, et al. Among authors: merchant m. Proc Natl Acad Sci U S A. 2019 Aug 13;116(33):16420-16429. doi: 10.1073/pnas.1906999116. Epub 2019 Aug 1. Proc Natl Acad Sci U S A. 2019. PMID: 31371506 Free PMC article.
ERBB3 and IGF1R Signaling Are Required for Nrf2-Dependent Growth in KEAP1-Mutant Lung Cancer.
Vartanian S, Lee J, Klijn C, Gnad F, Bagniewska M, Schaefer G, Zhang D, Tan J, Watson SA, Liu L, Chen H, Liang Y, Watanabe C, Cuellar T, Kan D, Hartmaier RJ, Lau T, Costa MR, Martin SE, Merchant M, Haley B, Stokoe D. Vartanian S, et al. Among authors: merchant m. Cancer Res. 2019 Oct 1;79(19):4828-4839. doi: 10.1158/0008-5472.CAN-18-2086. Epub 2019 Aug 15. Cancer Res. 2019. PMID: 31416841
IRE1α Disruption in Triple-Negative Breast Cancer Cooperates with Antiangiogenic Therapy by Reversing ER Stress Adaptation and Remodeling the Tumor Microenvironment.
Harnoss JM, Le Thomas A, Reichelt M, Guttman O, Wu TD, Marsters SA, Shemorry A, Lawrence DA, Kan D, Segal E, Merchant M, Totpal K, Crocker LM, Mesh K, Dohse M, Solon M, Modrusan Z, Rudolph J, Koeppen H, Walter P, Ashkenazi A. Harnoss JM, et al. Among authors: merchant m. Cancer Res. 2020 Jun 1;80(11):2368-2379. doi: 10.1158/0008-5472.CAN-19-3108. Epub 2020 Apr 7. Cancer Res. 2020. PMID: 32265225 Free PMC article.
CRAF dimerization with ARAF regulates KRAS-driven tumor growth.
Venkatanarayan A, Liang J, Yen I, Shanahan F, Haley B, Phu L, Verschueren E, Hinkle TB, Kan D, Segal E, Long JE, Lima T, Liau NPD, Sudhamsu J, Li J, Klijn C, Piskol R, Junttila MR, Shaw AS, Merchant M, Chang MT, Kirkpatrick DS, Malek S. Venkatanarayan A, et al. Among authors: merchant m. Cell Rep. 2022 Feb 8;38(6):110351. doi: 10.1016/j.celrep.2022.110351. Cell Rep. 2022. PMID: 35139374 Free article.
573 results