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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM. Wehn PM, et al. Among authors: czerwinski rm. J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18. J Med Chem. 2018. PMID: 30289716
3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM. Xu R, et al. Among authors: czerwinski rm. J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31282155 Clinical Trial.
A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA. Wallace EM, et al. Among authors: czerwinski rm. Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6. Cancer Res. 2016. PMID: 27635045
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A. Casimiro-Garcia A, et al. J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30. J Med Chem. 2018. PMID: 30423248
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB. Thorarensen A, et al. Among authors: czerwinski rm. J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16. J Med Chem. 2017. PMID: 28139931
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Thorarensen A, Balbo P, Banker ME, Czerwinski RM, Kuhn M, Maurer TS, Telliez JB, Vincent F, Wittwer AJ. Thorarensen A, et al. Among authors: czerwinski rm. Bioorg Med Chem. 2021 Jan 1;29:115865. doi: 10.1016/j.bmc.2020.115865. Epub 2020 Nov 18. Bioorg Med Chem. 2021. PMID: 33285410
Identification and characterization of acidic mammalian chitinase inhibitors.
Cole DC, Olland AM, Jacob J, Brooks J, Bursavich MG, Czerwinski R, DeClercq C, Johnson M, Joseph-McCarthy D, Ellingboe JW, Lin L, Nowak P, Presman E, Strand J, Tam A, Williams CM, Yao S, Tsao DH, Fitz LJ. Cole DC, et al. J Med Chem. 2010 Aug 26;53(16):6122-8. doi: 10.1021/jm100533p. J Med Chem. 2010. PMID: 20666458
41 results