亓爽,中国科学院合肥物质科学研究院健康与医学技术研究所创新药物研究中心副研究员。2006年本科毕业于南京大学;2011年博士毕业于香港大学;2011-2014年在中国科学技术大学生命科学院从事博士后研究;2014年底加入中国科学院合肥物质科学研究院工作至今。
重点关注肿瘤药理机制研究、激酶靶向药物的药效评价。
1.肿瘤药理研究:包括小分子药物的药理机制、肿瘤耐药机制与干预策略研究;
2.激酶靶向药物的药效评价:以转化应用为导向,开展激酶靶向药物的体内体外药效评价。
代表性论文
BMX inhibition overcomes small cell lung cancer chemoresistance by stabilizing E2F1 via ERK1/2-Cyclin D1/CDK4/6 axis, Signal Transduction and Targeted Therapy, 2026 Apr 8;11(1):125.
Discovery of IHMT-15130 as a Highly Potent Irreversible BMX Inhibitor for the Treatment of Myocardial Hypertrophy and Remodeling. ACS Chem Biol, 2025 20 (6), 1181-1194.
Hypocrellin A from an ethnic medicinal fungus protects against NLRP3-driven gout in mice by suppressing inflammasome activation, Acta Pharmacologica Sinica, 2025, 46(4): 1016-1029.
CHMFL-26 is a highly potent irreversible HER2 inhibitor for use in the treatment of HER2-positive and HER2-mutant cancers. Acta Pharmacol Sin., 2022, 43, pages2678–2686.
Inhibition of the deubiquitinating enzyme USP47 as a novel targeted therapy for hematologic malignancies expressing mutant EZH2. Leukemia, 2022, 36, pages1048–1057.
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas. J. Med.Chem., 2021, 64, 20, 15170–15188.
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J. Med. Chem. 2019, 62 (13), 6083-6101.
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. Eur. J. Med. Chem. 2018 Mar 12;150:366-384.
专利
吡唑衍生物及其用途,2020-08-14,202010816805.9
MST1激酶抑制剂及其用途,2019-09-25,201910914334.2
MST1激酶抑制剂及其用途,2018-10-15,201811190756.1
吲唑类激酶抑制剂及其用途,2018-11-02,201811299323.X
一类新型的苯氧基哌啶衍生物及其用途,2018-03-19,201810224206.0
一种新型的PDGFR激酶抑制剂及其用途,2016-09-08,201610811854.7
一种选择性的C-KIT激酶抑制剂,2016-04-01,201610210424.X
一种新型布鲁顿酪氨酸激酶不可逆抑制剂,2016-02-04,201610084082.1
承担项目
mTOR/MNK双重抑制剂CYF-1-56克服mTOR抑制剂诱导的eIF4E活化导致的 耐药机制初探,国家自然科学基金青年项目,2020.01-2022.12,结题,主持
新型高活性高选择性FGF2/FGFR1配体陷阱蛋白抑制剂的理性设计和构效,安徽省自然科学基金面上项目,2019.07-2022.06,结题,主持
高选择性FGF1/FGFR信号通路配体陷阱大分子蛋白抑制剂的发现以及作用机制研究,院长基金青年“火花”项目,2018.06-2020.05,结题,主持