许恒，中国医学科学院药物研究所研究员，博士生导师。1998年本科毕业于南京大学化学系；2005年获得美国德克萨斯大学阿灵顿分校博士学位； 2005年至2008年在美国国立卫生研究院/国家癌症研究所从事博士后研究；2008年至2011年在葛兰素史克中国研发中心工作，担任Senior Scientist从事中枢神经领域新药研究；2011年至2015年在方正医药研究院担任副院长开展创新药物研发工作；2015年9月起任中国医学科学院药物研究所课题组长，主要进行小分子创新药物的设计与研发。

1) 抗肿瘤小分子药物设计与研发
2) 抗自身免疫性疾病小分子药物设计与研发
3) 基于蛋白靶向降解技术的药物设计与研发
4) 光控药物设计与发现

代表性论文：
(1) Lin, S.#; Du, T. #; Zhang, J. #; Wu, D.; Tian, H.; Zhang, K.; Jiang, L.; Lu, D.; Sheng, L.; Lin, Y.; Ji, M.*; Chen, X.*; Xu, H.* Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J. Med. Chem. 2022, 65, 16372−16391.
(2) Zhang, J. #; Jiang, H. #; Lin, S. #; Wu, D.; Tian, H.; Jiang, L.; Cui, Y.; Jin, J.*; Chen, X.*; Xu, H.* Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies. J. Med. Chem. 2022, 65, 8011-8028.
(3) Zhang, Y.; Peng, S.; Lin, S.; Ji, M.; Du, T.*; Chen, X.*; Xu, H.* Discovery of a Novel Photoswitchable PI3K Inhibitor toward Optically-Controlled Anticancer Activity. Bioorg. Med. Chem. 2022, 116975.
(4) Ji, M.#; Wang, D.#; Lin, S., Wang, C.; Li, L.; Zhang, Z.; Jin, J.; Wu, D.; Dong, Y.; Xu, H.*; Lu, D.*; Chen, X.* A novel PI3K inhibitor XH30 suppresses orthotopic glioblastoma growth and brain metastasis in mice models. Acta Pharm. Sin. B 2022, 12, 774-786.
(5) Zhang, K.#; Ji, M.#; Lin, S.; Peng, S.; Zhang, Z.; Zhang, M.; Zhang, J.; Zhang, Y.; Wu, D.; Tian, H.; Chen, X.*; Xu, H.* Design, Synthesis and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment. J. Med. Chem. 2021, 64, 7331-7340.
(6) Dong, Y. #; Fu, R. #; Chen, J.; Zhang, K.; Ji, M.; Wang, M.; Jiang, H.; Ye, W.; Hu, J.; Li, Y.; Jin, J.*; Chen, X.*; Xu, H.* Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J. Med. Chem. 2021, 64, 16626-16640.
(7) Dong, Y. #; Mei, B. #; Zhang, X.*; Xu, H.* Selective gram-scale C–H carbenoid functionalization of N-sulfonylarylamides with rhodium catalyst. J. Org. Chem. 2021, 86, 11660-11672.
(8) Sun, Y.#; Fu, R.#; Lin, S.; Zhang, J.; Ji, M.; Zhang, Y.; Wu, D.; Zhang, K.; Tian, H.; Zhang, M.; Sheng, L.; Li, Y.; Jin, J.*; Chen, X.*; Xu, H.* Discovery of New Thieno[2,3-d]pyrimidine and Thiazolo[5,4-d]pyrimidine Derivatives as Orally Active Phosphoinositide 3-Kinase Inhibitors. Bioorg. Med. Chem. 2021, 29, 115890.
(9) Du, T.; Lin, S.; Ji, M.; Xue, N.; Liu, Y.; Zhang, Z.; Zhang, K.; Zhang, J.; Zhang, Y.; Wang, Q.; Sheng, L.; Li, Y.; Lu, D.*; Chen, X.*; Xu, H.* A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity. Cancer Lett. 2020, 495, 22-32.
(10) Dong, Y.#; Chen, J.#; Cui, Y.; Bao, L.; Xu, H.* Cp*RhIII-catalyzed sulfonamide directed ortho arene C–H carbenoid functionalization with pyridotriazoles. Org. Lett., 2020, 22, 772-775.
(11) Lin, S.#; Jin, J.#; Liu, Y.#; Tian, H.; Zhang, Y.; Fu, R.; Zhang, J.; Wang, M.; Du, T.; Ji, M.; Wu, D.; Zhang, K.; Sheng, L.; Li, Y.; Chen, X.*; Xu, H.* Discovery of 4-Methyl Quinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem. 2019, 62, 8873-8879.
(12) Zhang, K.#; Lai, F.#; Lin, S.; Ji, M.; Zhang, J.; Zhang, Y.; Jin, J.; Fu, R.; Wu, D.; Tian, H.; Xue, N.; Sheng, L.; Zou, X.; Li, Y.; Chen, X.*; Xu, H.* Design, Synthesis and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J. Med. Chem. 2019, 62, 6992-7014.
(13) Dong, Y.#; Zhang, X.#; Chen, J.; Zou, W.; Lin, S.; Xu, H.* Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles. Chem. Sci., 2019, 10, 8744-8751.
(14) Dong, Y.; Chen, J.; Xu, H.* Rhodium(III)-catalyzed sulfonamide directed ortho C–H carbenoid functionalization via metal carbene migratory insertion. Chem.Commun. 2019, 55, 2027-2030.
(15) Lin, S.#; Wang, C.#; Ji, M.; Wu, D.; Lv, Y.; Zhang, K.; Dong, Y.; Jin, J.; Chen, J.; Zhang, J.; Sheng, L.; Li, Y.; Chen, X.*; Xu, H.* Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-kinase Inhibitors for Cancer Treatment. J. Med. Chem. 2018, 61, 6087–6109.
(16) Dong, Y.#; Chen, J.#; Xu, H.* Rhodium(III)-catalyzed directed amidation of unactivated C(sp3)–H bonds to afford 1,2-amino alcohol derivatives. Chem. Commun. 2018, 54, 11096-11099.