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584 results

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Page 1
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: sullivan f. 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
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: sullivan fx. 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.
A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.
Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM. Drilon A, et al. Among authors: sullivan fx. Cancer Discov. 2017 Sep;7(9):963-972. doi: 10.1158/2159-8290.CD-17-0507. Epub 2017 Jun 3. Cancer Discov. 2017. PMID: 28578312 Free PMC article. Clinical Trial.
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.
Hinklin RJ, Baer BR, Boyd SA, Chicarelli MD, Condroski KR, DeWolf WE Jr, Fischer J, Frank M, Hingorani GP, Lee PA, Neitzel NA, Pratt SA, Singh A, Sullivan FX, Turner T, Voegtli WC, Wallace EM, Williams L, Aicher TD. Hinklin RJ, et al. Bioorg Med Chem. 2020 Jan 1;28(1):115232. doi: 10.1016/j.bmc.2019.115232. Epub 2019 Dec 2. Bioorg Med Chem. 2020. PMID: 31818630
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.
Thomas AA, Le Huerou Y, De Meese J, Gunawardana I, Kaplan T, Romoff TT, Gonzales SS, Condroski K, Boyd SA, Ballard J, Bernat B, DeWolf W, Han M, Lee P, Lemieux C, Pedersen R, Pheneger J, Poch G, Smith D, Sullivan F, Weiler S, Wright SK, Lin J, Brandhuber B, Vigers G. Thomas AA, et al. Among authors: sullivan f. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. doi: 10.1016/j.bmcl.2007.11.101. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18267359
Non-charged thiamine analogs as inhibitors of enzyme transketolase.
Thomas AA, De Meese J, Le Huerou Y, Boyd SA, Romoff TT, Gonzales SS, Gunawardana I, Kaplan T, Sullivan F, Condroski K, Lyssikatos JP, Aicher TD, Ballard J, Bernat B, DeWolf W, Han M, Lemieux C, Smith D, Weiler S, Wright SK, Vigers G, Brandhuber B. Thomas AA, et al. Among authors: sullivan f. Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12. doi: 10.1016/j.bmcl.2007.11.098. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18182286
Prodrug thiamine analogs as inhibitors of the enzyme transketolase.
Le Huerou Y, Gunawardana I, Thomas AA, Boyd SA, de Meese J, Dewolf W, Gonzales SS, Han M, Hayter L, Kaplan T, Lemieux C, Lee P, Pheneger J, Poch G, Romoff TT, Sullivan F, Weiler S, Wright SK, Lin J. Le Huerou Y, et al. Among authors: sullivan f. Bioorg Med Chem Lett. 2008 Jan 15;18(2):505-8. doi: 10.1016/j.bmcl.2007.11.100. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18083562
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor.
Hallin J, Bowcut V, Calinisan A, Briere DM, Hargis L, Engstrom LD, Laguer J, Medwid J, Vanderpool D, Lifset E, Trinh D, Hoffman N, Wang X, David Lawson J, Gunn RJ, Smith CR, Thomas NC, Martinson M, Bergstrom A, Sullivan F, Bouhana K, Winski S, He L, Fernandez-Banet J, Pavlicek A, Haling JR, Rahbaek L, Marx MA, Olson P, Christensen JG. Hallin J, et al. Among authors: sullivan f. Nat Med. 2022 Oct;28(10):2171-2182. doi: 10.1038/s41591-022-02007-7. Epub 2022 Oct 10. Nat Med. 2022. PMID: 36216931
584 results