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Page 1
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J. Mathieu S, et al. Among authors: hatzivassiliou g. J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29. J Med Chem. 2012. PMID: 22335519
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J. Wenglowsky S, et al. Among authors: hatzivassiliou g. ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900315 Free PMC article.
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. Hatzivassiliou G, et al. Nature. 2010 Mar 18;464(7287):431-5. doi: 10.1038/nature08833. Epub 2010 Feb 3. Nature. 2010. PMID: 20130576
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S. Romero FA, et al. Among authors: hatzivassiliou g. J Med Chem. 2017 Nov 22;60(22):9162-9183. doi: 10.1021/acs.jmedchem.7b00796. Epub 2017 Sep 21. J Med Chem. 2017. PMID: 28892380
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).
Pei Z, Mendonca R, Gazzard L, Pastor R, Goon L, Gustafson A, VanderPorten E, Hatzivassiliou G, Dement K, Cass R, Yuen PW, Zhang Y, Wu G, Lin X, Liu Y, Sellers BD. Pei Z, et al. Among authors: hatzivassiliou g. ACS Med Chem Lett. 2018 Apr 2;9(5):417-421. doi: 10.1021/acsmedchemlett.7b00427. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795752 Free PMC article.
The Hippo pathway effector TAZ induces TEAD-dependent liver inflammation and tumors.
Hagenbeek TJ, Webster JD, Kljavin NM, Chang MT, Pham T, Lee HJ, Klijn C, Cai AG, Totpal K, Ravishankar B, Yang N, Lee DH, Walsh KB, Hatzivassiliou G, de la Cruz CC, Gould SE, Wu X, Lee WP, Yang S, Zhang Z, Gu Q, Ji Q, Jackson EL, Lim DS, Dey A. Hagenbeek TJ, et al. Among authors: hatzivassiliou g. Sci Signal. 2018 Sep 11;11(547):eaaj1757. doi: 10.1126/scisignal.aaj1757. Sci Signal. 2018. PMID: 30206136
ERK inhibition overcomes acquired resistance to MEK inhibitors.
Hatzivassiliou G, Liu B, O'Brien C, Spoerke JM, Hoeflich KP, Haverty PM, Soriano R, Forrest WF, Heldens S, Chen H, Toy K, Ha C, Zhou W, Song K, Friedman LS, Amler LC, Hampton GM, Moffat J, Belvin M, Lackner MR. Hatzivassiliou G, et al. Mol Cancer Ther. 2012 May;11(5):1143-54. doi: 10.1158/1535-7163.MCT-11-1010. Epub 2012 Mar 8. Mol Cancer Ther. 2012. PMID: 22402123
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. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Nature. 2013. PMID: 23934108
Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2.
Foster SA, Whalen DM, Özen A, Wongchenko MJ, Yin J, Yen I, Schaefer G, Mayfield JD, Chmielecki J, Stephens PJ, Albacker LA, Yan Y, Song K, Hatzivassiliou G, Eigenbrot C, Yu C, Shaw AS, Manning G, Skelton NJ, Hymowitz SG, Malek S. Foster SA, et al. Among authors: hatzivassiliou g. Cancer Cell. 2016 Apr 11;29(4):477-493. doi: 10.1016/j.ccell.2016.02.010. Epub 2016 Mar 17. Cancer Cell. 2016. PMID: 26996308 Free article.
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition.
Ghosh S, Taylor A, Chin M, Huang HR, Conery AR, Mertz JA, Salmeron A, Dakle PJ, Mele D, Cote A, Jayaram H, Setser JW, Poy F, Hatzivassiliou G, DeAlmeida-Nagata D, Sandy P, Hatton C, Romero FA, Chiang E, Reimer T, Crawford T, Pardo E, Watson VG, Tsui V, Cochran AG, Zawadzke L, Harmange JC, Audia JE, Bryant BM, Cummings RT, Magnuson SR, Grogan JL, Bellon SF, Albrecht BK, Sims RJ 3rd, Lora JM. Ghosh S, et al. Among authors: hatzivassiliou g. J Biol Chem. 2016 Jun 17;291(25):13014-27. doi: 10.1074/jbc.M115.708560. Epub 2016 Apr 7. J Biol Chem. 2016. PMID: 27056325 Free PMC article.
43 results