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Preclinical absorption, distribution, metabolism, excretion, and pharmacokinetic-pharmacodynamic modelling of N-(4-(3-((3S,4R)-1-ethyl-3-fluoropiperidine-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide, a novel MET kinase inhibitor.
Liederer BM, Berezhkovskiy LM, Dean BJ, Dinkel V, Peng J, Merchant M, Plise EG, Wong H, Liu X. Liederer BM, et al. Among authors: merchant m. Xenobiotica. 2011 Apr;41(4):327-39. doi: 10.3109/00498254.2010.542500. Epub 2010 Dec 23. Xenobiotica. 2011. PMID: 21182395
Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.
Heald RA, Jackson P, Savy P, Jones M, Gancia E, Burton B, Newman R, Boggs J, Chan E, Chan J, Choo E, Merchant M, Rudewicz P, Ultsch M, Wiesmann C, Yue Q, Belvin M, Price S. Heald RA, et al. Among authors: merchant m. J Med Chem. 2012 May 24;55(10):4594-604. doi: 10.1021/jm2017094. Epub 2012 May 3. J Med Chem. 2012. PMID: 22506516
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
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Hatzivassiliou G, et al. Among authors: merchant m. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Nature. 2013. PMID: 23934108
Nonclinical evaluation of the serum pharmacodynamic biomarkers HGF and shed MET following dosing with the anti-MET monovalent monoclonal antibody onartuzumab.
Mai E, Zheng Z, Chen Y, Peng J, Severin C, Filvaroff E, Romero M, Mallet W, Kaur S, Gelzleichter T, Nijem I, Merchant M, Young JC. Mai E, et al. Among authors: merchant m. Mol Cancer Ther. 2014 Feb;13(2):540-52. doi: 10.1158/1535-7163.MCT-13-0494. Epub 2013 Nov 20. Mol Cancer Ther. 2014. PMID: 24258345
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.
571 results