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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: wu l. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. PLoS One. 2020. PMID: 32315352 Free PMC article.
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. 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
Inhibition of ALK2 with bicyclic pyridyllactams.
Witten MR, Wu L, Lai CT, Kapilashrami K, Pusey M, Gallagher K, Chen Y, Yao W. Witten MR, et al. Among authors: wu l. Bioorg Med Chem Lett. 2022 Jan 1;55:128452. doi: 10.1016/j.bmcl.2021.128452. Epub 2021 Nov 13. Bioorg Med Chem Lett. 2022. PMID: 34780900
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: wu l. 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 of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Nguyen MH, Atasoylu O, Wu L, Kapilashrami K, Pusey M, Gallagher K, Lai CT, Zhao P, Barbosa J, Liu K, He C, Zhang C, Styduhar ED, Witten MR, Chen Y, Lin L, Yang YO, Covington M, Diamond S, Yeleswaram S, Yao W. Nguyen MH, et al. Among authors: wu l. ACS Med Chem Lett. 2022 Jun 22;13(7):1159-1164. doi: 10.1021/acsmedchemlett.2c00206. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859885 Free PMC article.
Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors.
Sokolsky A, Winterton S, Kennedy K, Drake K, Stump K, Huo L, Lo Y, Ye M, Covington M, Diamond S, Yang YO, Kim S, Yeleswaram S, Wu L, Yao W. Sokolsky A, et al. Among authors: wu l. ACS Med Chem Lett. 2022 Oct 6;13(11):1797-1804. doi: 10.1021/acsmedchemlett.2c00408. eCollection 2022 Nov 10. ACS Med Chem Lett. 2022. PMID: 36385925 Free PMC article.
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
Hummel JR, Xiao KJ, Yang JC, Epling LB, Mukai K, Ye Q, Xu M, Qian D, Huo L, Weber M, Roman V, Lo Y, Drake K, Stump K, Covington M, Kapilashrami K, Zhang G, Ye M, Diamond S, Yeleswaram S, Macarron R, Deller MC, Wee S, Kim S, Wang X, Wu L, Yao W. Hummel JR, et al. Among authors: wu l. J Med Chem. 2024 Feb 22;67(4):3112-3126. doi: 10.1021/acs.jmedchem.3c02287. Epub 2024 Feb 7. J Med Chem. 2024. PMID: 38325398
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