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The 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor INCB13739 improves hyperglycemia in patients with type 2 diabetes inadequately controlled by metformin monotherapy.
Rosenstock J, Banarer S, Fonseca VA, Inzucchi SE, Sun W, Yao W, Hollis G, Flores R, Levy R, Williams WV, Seckl JR, Huber R; INCB13739-202 Principal Investigators. Rosenstock J, et al. Among authors: huber r. Diabetes Care. 2010 Jul;33(7):1516-22. doi: 10.2337/dc09-2315. Epub 2010 Apr 22. Diabetes Care. 2010. PMID: 20413513 Free PMC article. Clinical Trial.
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
Zhang C, Xu M, He C, Zhuo J, Burns DM, Qian DQ, Lin Q, Li YL, Chen L, Shi E, Agrios C, Weng L, Sharief V, Jalluri R, Li Y, Scherle P, Diamond S, Hunter D, Covington M, Marando C, Wynn R, Katiyar K, Contel N, Vaddi K, Yeleswaram S, Hollis G, Huber R, Friedman S, Metcalf B, Yao W. Zhang C, et al. Among authors: huber r. Bioorg Med Chem Lett. 2022 Aug 1;69:128782. doi: 10.1016/j.bmcl.2022.128782. Epub 2022 May 7. Bioorg Med Chem Lett. 2022. PMID: 35537608
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: huber 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
INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models.
Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G. Liu PCC, et al. Among authors: huber r. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. PLoS One. 2020. PMID: 32315352 Free PMC article.
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: huber r. 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
The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.
Stubbs MC, Burn TC, Sparks R, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue CB, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu PCC. Stubbs MC, et al. Among authors: huber r. Clin Cancer Res. 2019 Jan 1;25(1):300-311. doi: 10.1158/1078-0432.CCR-18-0098. Epub 2018 Sep 11. Clin Cancer Res. 2019. PMID: 30206163
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: huber r. 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.
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: huber r. 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
2,394 results