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Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma.
Wu H, Wang W, Liu F, Weisberg EL, Tian B, Chen Y, Li B, Wang A, Wang B, Zhao Z, McMillin DW, Hu C, Li H, Wang J, Liang Y, Buhrlage SJ, Liang J, Liu J, Yang G, Brown JR, Treon SP, Mitsiades CS, Griffin JD, Liu Q, Gray NS. Wu H, et al. Among authors: hu c. ACS Chem Biol. 2014 May 16;9(5):1086-91. doi: 10.1021/cb4008524. Epub 2014 Mar 17. ACS Chem Biol. 2014. PMID: 24556163 Free PMC article.
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells.
Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, Zhao P, Wang J, Wang C, Weisberg EL, Gray NS, Yun CH, Liu J, Chen L, Liu Q. Wu H, et al. Among authors: hu c. Oncotarget. 2015 Oct 13;6(31):31313-22. doi: 10.18632/oncotarget.5182. Oncotarget. 2015. PMID: 26375053 Free PMC article.
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Li X, Wang A, Yu K, Qi Z, Chen C, Wang W, Hu C, Wu H, Wu J, Zhao Z, Liu J, Zou F, Wang L, Wang B, Wang W, Zhang S, Liu J, Liu Q. Li X, et al. Among authors: hu c. J Med Chem. 2015 Dec 24;58(24):9625-38. doi: 10.1021/acs.jmedchem.5b01611. Epub 2015 Dec 14. J Med Chem. 2015. PMID: 26630553
Discovery and characterization of a novel potent type II native and mutant BCR-ABL inhibitor (CHMFL-074) for Chronic Myeloid Leukemia (CML).
Liu F, Wang B, Wang Q, Qi Z, Chen C, Kong LL, Chen JY, Liu X, Wang A, Hu C, Wang W, Wang H, Wu F, Ruan Y, Qi S, Liu J, Zou F, Hu Z, Wang W, Wang L, Zhang S, Yun CH, Zhai Z, Liu J, Liu Q. Liu F, et al. Among authors: hu c, hu z. Oncotarget. 2016 Jul 19;7(29):45562-45574. doi: 10.18632/oncotarget.10037. Oncotarget. 2016. PMID: 27322145 Free PMC article.
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.
Li B, Wang A, Liu J, Qi Z, Liu X, Yu K, Wu H, Chen C, Hu C, Wang W, Wu J, Hu Z, Ye L, Zou F, Liu F, Wang B, Wang L, Ren T, Zhang S, Bai M, Zhang S, Liu J, Liu Q. Li B, et al. Among authors: hu c, hu z. J Med Chem. 2016 Sep 22;59(18):8456-72. doi: 10.1021/acs.jmedchem.6b00902. Epub 2016 Aug 30. J Med Chem. 2016. PMID: 27545040
Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.
Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, Gray NS, Weisberg EL, Chen L, Liu J, Yun CH, Liu Q. Wang A, et al. Among authors: hu c. Oncotarget. 2016 Oct 25;7(43):69760-69769. doi: 10.18632/oncotarget.11951. Oncotarget. 2016. PMID: 27626175 Free PMC article.
Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.
Wang Q, Liu F, Wang B, Zou F, Qi Z, Chen C, Yu K, Hu C, Qi S, Wang W, Hu Z, Liu J, Wang W, Wang L, Liang Q, Zhang S, Ren T, Liu Q, Liu J. Wang Q, et al. Among authors: hu c, hu z. J Med Chem. 2017 Jan 12;60(1):273-289. doi: 10.1021/acs.jmedchem.6b01290. Epub 2016 Dec 14. J Med Chem. 2017. PMID: 27966954
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