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208 results

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Page 1
Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors.
Yen I, Shanahan F, Merchant M, Orr C, Hunsaker T, Durk M, La H, Zhang X, Martin SE, Lin E, Chan J, Yu Y, Amin D, Neve RM, Gustafson A, Venkatanarayan A, Foster SA, Rudolph J, Klijn C, Malek S. Yen I, et al. Among authors: la h. Cancer Cell. 2018 Oct 8;34(4):611-625.e7. doi: 10.1016/j.ccell.2018.09.002. Cancer Cell. 2018. PMID: 30300582 Free article.
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Huestis MP, Dela Cruz D, DiPasquale AG, Durk MR, Eigenbrot C, Gibbons P, Gobbi A, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Siu M, Rudolph J. Huestis MP, et al. Among authors: la h. J Med Chem. 2021 Apr 8;64(7):3940-3955. doi: 10.1021/acs.jmedchem.0c02085. Epub 2021 Mar 29. J Med Chem. 2021. PMID: 33780623
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Huestis MP, Durk MR, Eigenbrot C, Gibbons P, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Rudolph J, Siu M. Huestis MP, et al. Among authors: la h. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797. doi: 10.1021/acsmedchemlett.1c00063. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055227 Free PMC article.
Noncovalent wild-type-sparing inhibitors of EGFR T790M.
Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Lee HJ, et al. Among authors: la h. Cancer Discov. 2013 Feb;3(2):168-81. doi: 10.1158/2159-8290.CD-12-0357. Epub 2012 Dec 10. Cancer Discov. 2013. PMID: 23229345 Free PMC article.
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP. Hanan EJ, et al. Among authors: la h. J Med Chem. 2014 Dec 11;57(23):10176-91. doi: 10.1021/jm501578n. Epub 2014 Nov 20. J Med Chem. 2014. PMID: 25383627 Free PMC article.
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP. Hanan EJ, et al. Among authors: la h. Bioorg Med Chem Lett. 2016 Jan 15;26(2):534-539. doi: 10.1016/j.bmcl.2015.11.078. Epub 2015 Nov 22. Bioorg Med Chem Lett. 2016. PMID: 26639762
Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat.
Fan PW, Chen JZ, Allan Jaochico M, La H, Liu N, Mulder T, Cass RT, Durk M, Messick K, Valle N, Liu S, Lee W, Crawford JJ, Rudolf J, Murray LJ, Cyrus Khojasteh S, Wright M. Fan PW, et al. Among authors: la h. Drug Metab Lett. 2016;10(2):91-100. doi: 10.2174/1872312810666160411144358. Drug Metab Lett. 2016. PMID: 27063863 Free PMC article.
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.
Chan BK, Hanan EJ, Bowman KK, Bryan MC, Burdick D, Chan E, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Shao L, Wang S, Yeap SK, Yen I, Yu C, Heffron TP. Chan BK, et al. Among authors: la h. J Med Chem. 2016 Oct 13;59(19):9080-9093. doi: 10.1021/acs.jmedchem.6b00995. Epub 2016 Sep 12. J Med Chem. 2016. PMID: 27564586
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP. Heald R, et al. Among authors: la h. J Med Chem. 2015 Nov 25;58(22):8877-95. doi: 10.1021/acs.jmedchem.5b01412. Epub 2015 Nov 12. J Med Chem. 2015. PMID: 26455919
208 results