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Page 1
Emergence and Targeting of Acquired and Hereditary Resistance to Multikinase RET Inhibition in Patients With RET-Altered Cancer.
Wirth LJ, Kohno T, Udagawa H, Matsumoto S, Ishii G, Ebata K, Tuch BB, Zhu EY, Nguyen M, Smith S, Hanson LM, Burkard MR, Cable L, Blake JF, Condroski KR, Brandhuber BJ, Andrews S, Rothenberg SM, Goto K. Wirth LJ, et al. Among authors: burkard mr. JCO Precis Oncol. 2019 Sep 11;3:PO.19.00189. doi: 10.1200/PO.19.00189. eCollection 2019. JCO Precis Oncol. 2019. PMID: 32923848 Free PMC article. No abstract available.
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG. Fell JB, et al. Among authors: burkard mr. ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613331 Free PMC article.
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
Fell JB, Fischer JP, Baer BR, Blake JF, Bouhana K, Briere DM, Brown KD, Burgess LE, Burns AC, Burkard MR, Chiang H, Chicarelli MJ, Cook AW, Gaudino JJ, Hallin J, Hanson L, Hartley DP, Hicken EJ, Hingorani GP, Hinklin RJ, Mejia MJ, Olson P, Otten JN, Rhodes SP, Rodriguez ME, Savechenkov P, Smith DJ, Sudhakar N, Sullivan FX, Tang TP, Vigers GP, Wollenberg L, Christensen JG, Marx MA. Fell JB, et al. Among authors: burkard mr. J Med Chem. 2020 Jul 9;63(13):6679-6693. doi: 10.1021/acs.jmedchem.9b02052. Epub 2020 Apr 6. J Med Chem. 2020. PMID: 32250617 Free article.
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.
Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB. Ren L, et al. J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25603482
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.
Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB. Blake JF, et al. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29. Bioorg Med Chem Lett. 2014. PMID: 24813737
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. 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
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue Y, Gatto S, Fernandez-Banet J, Pavlicek A, Velastagui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF 3rd, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Jänne PA, Olson P, Christensen JG. Hallin J, et al. Among authors: burkard mr. Cancer Discov. 2020 Jan;10(1):54-71. doi: 10.1158/2159-8290.CD-19-1167. Epub 2019 Oct 28. Cancer Discov. 2020. PMID: 31658955 Free PMC article.
Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP. Hunt KW, et al. J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16. J Med Chem. 2013. PMID: 23537249
Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP, Gunawardana IW. Thomas AA, et al. J Med Chem. 2014 Feb 13;57(3):878-902. doi: 10.1021/jm401635n. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24397738
22 results