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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP. Yue EW, et al. Among authors: wynn r. ACS Med Chem Lett. 2017 Mar 6;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523098 Free PMC article.
Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP. Yue EW, et al. Among authors: wynn r. J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f. J Med Chem. 2009. PMID: 19507862
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Wu L, Zhang C, He C, Qian D, Lu L, Sun Y, Xu M, Zhuo J, Liu PCC, Klabe R, Wynn R, Covington M, Gallagher K, Leffet L, Bowman K, Diamond S, Koblish H, Zhang Y, Soloviev M, Hollis G, Burn TC, Scherle P, Yeleswaram S, Huber R, Yao W. Wu L, et al. Among authors: wynn r. J Med Chem. 2021 Aug 12;64(15):10666-10679. doi: 10.1021/acs.jmedchem.1c00713. Epub 2021 Jul 16. J Med Chem. 2021. PMID: 34269576
Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
Combs AP, Yue EW, Bower M, Ala PJ, Wayland B, Douty B, Takvorian A, Polam P, Wasserman Z, Zhu W, Crawley ML, Pruitt J, Sparks R, Glass B, Modi D, McLaughlin E, Bostrom L, Li M, Galya L, Blom K, Hillman M, Gonneville L, Reid BG, Wei M, Becker-Pasha M, Klabe R, Huber R, Li Y, Hollis G, Burn TC, Wynn R, Liu P, Metcalf B. Combs AP, et al. Among authors: wynn r. J Med Chem. 2005 Oct 20;48(21):6544-8. doi: 10.1021/jm0504555. J Med Chem. 2005. PMID: 16220970
Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: synthesis and structure-activity relationships of a peptide scaffold.
Yue EW, Wayland B, Douty B, Crawley ML, McLaughlin E, Takvorian A, Wasserman Z, Bower MJ, Wei M, Li Y, Ala PJ, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP. Yue EW, et al. Among authors: wynn r. Bioorg Med Chem. 2006 Sep 1;14(17):5833-49. doi: 10.1016/j.bmc.2006.05.032. Bioorg Med Chem. 2006. PMID: 16769216
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B. Combs AP, et al. Among authors: wynn r. J Med Chem. 2006 Jun 29;49(13):3774-89. doi: 10.1021/jm0600904. J Med Chem. 2006. PMID: 16789735
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.
Ala PJ, Gonneville L, Hillman M, Becker-Pasha M, Yue EW, Douty B, Wayland B, Polam P, Crawley ML, McLaughlin E, Sparks RB, Glass B, Takvorian A, Combs AP, Burn TC, Hollis GF, Wynn R. Ala PJ, et al. Among authors: wynn r. J Biol Chem. 2006 Dec 8;281(49):38013-21. doi: 10.1074/jbc.M607913200. Epub 2006 Oct 6. J Biol Chem. 2006. PMID: 17028182 Free article.
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B. Yao W, et al. Among authors: wynn r. J Med Chem. 2007 Feb 22;50(4):603-6. doi: 10.1021/jm061344o. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256836
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.
Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW. Douty B, et al. Among authors: wynn r. Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. doi: 10.1016/j.bmcl.2007.11.012. Epub 2007 Nov 9. Bioorg Med Chem Lett. 2008. PMID: 18037290
875 results