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Page 1
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
Du X, Moore J, Blank BR, Eksterowicz J, Sutimantanapi D, Yuen N, Metzger T, Chan B, Huang T, Chen X, Chen Y, Duong F, Kong W, Chang JH, Sun J, Zavorotinskaya T, Ye Q, Junttila MR, Ndubaku C, Friedman LS, Fantin VR, Sun D. Du X, et al. Among authors: fantin vr. J Med Chem. 2020 Sep 24;63(18):10433-10459. doi: 10.1021/acs.jmedchem.0c01086. Epub 2020 Sep 9. J Med Chem. 2020. PMID: 32865411
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D. Rew Y, et al. Among authors: fantin vr. J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23. J Med Chem. 2018. PMID: 30091920
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Du X, Eksterowicz J, Zhou H, Rew Y, Zhu L, Yan X, Medina JC, Huang T, Chen X, Sutimantanapi D, Jahchan N, Kong W, Sun J, Zavorotinskaya T, Ye Q, Fantin VR, Sun D. Du X, et al. Among authors: fantin vr. J Med Chem. 2019 Jul 25;62(14):6751-6764. doi: 10.1021/acs.jmedchem.9b00711. Epub 2019 Jul 5. J Med Chem. 2019. PMID: 31274313
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M. Kung PP, et al. Among authors: fantin vr. J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6. J Med Chem. 2016. PMID: 27512831
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.
Popovici-Muller J, Saunders JO, Salituro FG, Travins JM, Yan S, Zhao F, Gross S, Dang L, Yen KE, Yang H, Straley KS, Jin S, Kunii K, Fantin VR, Zhang S, Pan Q, Shi D, Biller SA, Su SM. Popovici-Muller J, et al. Among authors: fantin vr. ACS Med Chem Lett. 2012 Sep 17;3(10):850-5. doi: 10.1021/ml300225h. eCollection 2012 Oct 11. ACS Med Chem Lett. 2012. PMID: 24900389 Free PMC article.
Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A.
Quinlan CL, Kaiser SE, Bolaños B, Nowlin D, Grantner R, Karlicek-Bryant S, Feng JL, Jenkinson S, Freeman-Cook K, Dann SG, Wang X, Wells PA, Fantin VR, Stewart AE, Grant SK. Quinlan CL, et al. Among authors: fantin vr. Nat Chem Biol. 2017 Jul;13(7):785-792. doi: 10.1038/nchembio.2384. Epub 2017 May 29. Nat Chem Biol. 2017. PMID: 28553945
Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.
Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M. Gomes B, et al. Among authors: fantin vr. Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19. Mol Cancer Ther. 2018. PMID: 30232146
Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia.
Kashyap MK, Amaya-Chanaga CI, Kumar D, Simmons B, Huser N, Gu Y, Hallin M, Lindquist K, Yafawi R, Choi MY, Amine AA, Rassenti LZ, Zhang C, Liu SH, Smeal T, Fantin VR, Kipps TJ, Pernasetti F, Castro JE. Kashyap MK, et al. Among authors: fantin vr. J Hematol Oncol. 2017 May 19;10(1):112. doi: 10.1186/s13045-017-0435-x. J Hematol Oncol. 2017. PMID: 28526063 Free PMC article.
Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M. Kung PP, et al. Among authors: fantin vr. J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. J Med Chem. 2016. PMID: 27936698 No abstract available.
51 results