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23,435 results

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Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy.
Shin N, Stubbs M, Koblish H, Yue EW, Soloviev M, Douty B, Wang KH, Wang Q, Gao M, Feldman P, Yang G, Hall L, Hansbury M, O'Connor S, Leffet L, Collins R, Katiyar K, He X, Waeltz P, Collier P, Lu J, Li YL, Li Y, Liu PCC, Burn T, Covington M, Diamond S, Shuey D, Roberts A, Yeleswaram S, Hollis G, Metcalf B, Yao W, Huber R, Combs A, Newton R, Scherle P. Shin N, et al. Among authors: yang g. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222. doi: 10.1124/jpet.120.265538. Epub 2020 Apr 28. J Pharmacol Exp Ther. 2020. PMID: 32345620
INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies.
Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P. Shin N, et al. Among authors: yang g. J Pharmacol Exp Ther. 2018 Jan;364(1):120-130. doi: 10.1124/jpet.117.244947. Epub 2017 Nov 10. J Pharmacol Exp Ther. 2018. PMID: 29127109
Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.
Koblish HK, Hansbury MJ, Bowman KJ, Yang G, Neilan CL, Haley PJ, Burn TC, Waeltz P, Sparks RB, Yue EW, Combs AP, Scherle PA, Vaddi K, Fridman JS. Koblish HK, et al. Among authors: yang g. Mol Cancer Ther. 2010 Feb;9(2):489-98. doi: 10.1158/1535-7163.MCT-09-0628. Epub 2010 Feb 2. Mol Cancer Ther. 2010. PMID: 20124451
Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.
Liu X, Shin N, Koblish HK, Yang G, Wang Q, Wang K, Leffet L, Hansbury MJ, Thomas B, Rupar M, Waeltz P, Bowman KJ, Polam P, Sparks RB, Yue EW, Li Y, Wynn R, Fridman JS, Burn TC, Combs AP, Newton RC, Scherle PA. Liu X, et al. Among authors: yang g. Blood. 2010 Apr 29;115(17):3520-30. doi: 10.1182/blood-2009-09-246124. Epub 2010 Mar 2. Blood. 2010. PMID: 20197554 Free article.
A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.
Liu X, Wang Q, Yang G, Marando C, Koblish HK, Hall LM, Fridman JS, Behshad E, Wynn R, Li Y, Boer J, Diamond S, He C, Xu M, Zhuo J, Yao W, Newton RC, Scherle PA. Liu X, et al. Among authors: yang g. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. doi: 10.1158/1078-0432.CCR-11-1157. Epub 2011 Sep 14. Clin Cancer Res. 2011. PMID: 21918175
A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity.
Rios-Doria J, Favata M, Lasky K, Feldman P, Lo Y, Yang G, Stevens C, Wen X, Sehra S, Katiyar K, Liu K, Wynn R, Harris JJ, Ye M, Spitz S, Wang X, He C, Li YL, Yao W, Covington M, Scherle P, Koblish H. Rios-Doria J, et al. Among authors: yang g. Front Oncol. 2020 Dec 7;10:598477. doi: 10.3389/fonc.2020.598477. eCollection 2020. Front Oncol. 2020. PMID: 33425754 Free PMC article.
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: yang yo, yang g. 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.
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: yang g. 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: yang g. 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.
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W. Burns DM, et al. Among authors: yang g. Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. doi: 10.1016/j.bmcl.2007.11.086. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18068976
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