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Page 1
Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor.
Koblish HK, Wu L, Wang LS, Liu PCC, Wynn R, Rios-Doria J, Spitz S, Liu H, Volgina A, Zolotarjova N, Kapilashrami K, Behshad E, Covington M, Yang YO, Li J, Diamond S, Soloviev M, O'Hayer K, Rubin S, Kanellopoulou C, Yang G, Rupar M, DiMatteo D, Lin L, Stevens C, Zhang Y, Thekkat P, Geschwindt R, Marando C, Yeleswaram S, Jackson J, Scherle P, Huber R, Yao W, Hollis G. Koblish HK, et al. Among authors: covington m. Cancer Discov. 2022 Jun 2;12(6):1482-1499. doi: 10.1158/2159-8290.CD-21-1156. Cancer Discov. 2022. PMID: 35254416 Free PMC article. Clinical Trial.
Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K. Brodmerkel CM, et al. Among authors: covington m. J Immunol. 2005 Oct 15;175(8):5370-8. doi: 10.4049/jimmunol.175.8.5370. J Immunol. 2005. PMID: 16210643
Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab.
Liu X, Fridman JS, Wang Q, Caulder E, Yang G, Covington M, Liu C, Marando C, Zhuo J, Li Y, Yao W, Vaddi K, Newton RC, Scherle PA, Friedman SM. Liu X, et al. Among authors: covington m. Cancer Biol Ther. 2006 Jun;5(6):648-56. doi: 10.4161/cbt.5.6.2707. Epub 2006 Jun 14. Cancer Biol Ther. 2006. PMID: 16627988 Free article.
Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells.
Liu PC, Liu X, Li Y, Covington M, Wynn R, Huber R, Hillman M, Yang G, Ellis D, Marando C, Katiyar K, Bradley J, Abremski K, Stow M, Rupar M, Zhuo J, Li YL, Lin Q, Burns D, Xu M, Zhang C, Qian DQ, He C, Sharief V, Weng L, Agrios C, Shi E, Metcalf B, Newton R, Friedman S, Yao W, Scherle P, Hollis G, Burn TC. Liu PC, et al. Among authors: covington m. Cancer Biol Ther. 2006 Jun;5(6):657-64. doi: 10.4161/cbt.5.6.2708. Epub 2006 Jun 14. Cancer Biol Ther. 2006. PMID: 16627989 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: covington mb. J Med Chem. 2007 Feb 22;50(4):603-6. doi: 10.1021/jm061344o. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256836
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Yao W, Zhuo J, Burns DM, Li YL, Qian DQ, Zhang C, He C, Xu M, Shi E, Li Y, Marando CA, Covington MB, Yang G, Liu X, Pan M, Fridman JS, Scherle P, Wasserman ZR, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B. Yao W, et al. Among authors: covington mb. Bioorg Med Chem Lett. 2008 Jan 1;18(1):159-63. doi: 10.1016/j.bmcl.2007.10.108. Epub 2007 Nov 4. Bioorg Med Chem Lett. 2008. PMID: 18036818
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Burns DM, Li YL, Shi E, He C, Xu M, Zhuo J, Zhang C, Qian DQ, Li Y, Wynn R, Covington MB, Katiyar K, Marando CA, Fridman JS, Scherle P, Friedman S, Metcalf B, Yao W. Burns DM, et al. Among authors: covington mb. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3525-30. doi: 10.1016/j.bmcl.2009.04.143. Epub 2009 May 5. Bioorg Med Chem Lett. 2009. PMID: 19457660
Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.
Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA. Shin N, et al. Among authors: covington mb. Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5. doi: 10.1016/j.bbrc.2009.06.135. Epub 2009 Jul 1. Biochem Biophys Res Commun. 2009. PMID: 19576173
Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K. Fridman JS, et al. Among authors: covington mb. J Immunol. 2010 May 1;184(9):5298-307. doi: 10.4049/jimmunol.0902819. Epub 2010 Apr 2. J Immunol. 2010. PMID: 20363976
255 results