2023年5月~?至今，中國科學院上海有機化學研究所生命過程小分子調控全國重點實驗室, 研究員
2016年6月~?2023年5月，暨南大學藥學院，教授，院長（2016-2022）
2006年3月~?2016年6月，中國科學院廣州生物醫(yī)藥與健康研究院, 研究員
2005年3月~ 2006年3月，Research Investigator, 美國密西根大學醫(yī)學院（Ann Arbor）
2001年12月~ 2005年2月，博士后研究，美國密西根大學（Ann?Arbor）腫瘤中心
2001年9月~ 2001年11月，臨時研究人員，無錫藥明康德（上海）
1998年9月~ 2001年7月，有機化學博士，復旦大學（上海有機化學研究所聯合培養(yǎng)）
1995年9月~ 1998年7月，藥物化學碩士，中國藥科大學
1991年9月~ 1995年7月，化學制藥本科，中國藥科大學
藥物化學生物學。主要方向為抗腫瘤藥物的設計、合成與生物學活性研究。
2022，吳階平- 保羅 楊森醫(yī)藥科技獎（吳楊獎，Wu Jieping-Paul Janssen Medical & Pharmaceutical Awards）
2022，美國Prostate Cancer Foundation（PCF）TACTICAL Award
2022，中國藥學會最美科技工作者
2018，國家教學成果二等獎
2018，長江學者特聘教授
2017，中國衛(wèi)計委突出貢獻中青年專家
2016，科技創(chuàng)新創(chuàng)業(yè)領軍人才
2016，Fellow, the Royal Society of Chemistry (UK, FRSC)
2015，科技部人才推進計劃
2014，國家杰出青年基金獲得者
2014，廣東省南粵百杰
2012，國務院政府津貼
2012，無錫藥明康德生命化學獎
2009，第十屆丁穎科技獎
1)?Ling, H.; Li, L.; Duan, L.; Huang, W.; Zheng, J.; Zhang, S.; Li, X.; Qiu, X.; Zhou, Y.; Ma, N.; Ren, X.; Zhang, J.; Wang, Z.; Zhang, Y.; Tian, R.; Zhang, Z.-M.*; Ding, K.* O-Cyanobenzaldehydes Irreversibly Modify Both Buried and Exposed Lysine Residues in Live Cells.?J Am Chem Soc, 2025, 147(14):11955-11963.
2)?He, X.; Wang, Q.-X.; Wei, D.*; Lin, Y.; Zhang, X.; Wu, Y.; Qian, X.; Lin, Z.; Xiao, B.; Wu, Q.; Wang, Z.; Zhou, F.; Wei, Z.; Wang, J.; Gong, R.; Zhang, R.; Zhang, Q.*; Ding, K.*; Gao, S.*; Kang, T.* Lysosomal EGFR acts as a Rheb-GEF independent of its kinase activity to activate mTORC1. Cell Res.?2025. DOI:10.1038/s41422-025-01110-x.
3)?Bao, Y.; Chang, Y.; Tien, J. C.-Y.; Cruz, G.; Yang, F.; Mannan, R.; Mahapatra, S.; Paturu, R.; Cao, X.; Su, F.; Wang, R.; Zhang, Y.; Gunda, M.; Choi, J. E.; Gurkan, J. K.; Miner, S. J.; Robinson, D. R.; Wu, Y.-M.; Zhou, L.; Wang, Z.; Kryczek, I.; Wang, X.; Cieslik, M.; Qia0, Y.; Tsodikov, A.; Zou, W.; Ding, K.* and Chinnaiyan, A. M.* CDK12/13 inactivation triggers STING-mediated anti-tumor immunity in pre-clinical models. J. Clin. Invest.?2025. https://doi.org/10.1172/JCI193745
4)?Yang, J.; Chang, Y.; Zhou, K.; Huang, W.; Tien, J. C.-Y.; Zhang, P.; Liu, W.; Zhou. L.; Zhou, Y.; Ren, X.; Mannan, R.; Mahapatra, S.; Zhang, Y.; Hamadeh, R.; Ervine, G.; Wang, Z.*; Wang, G. X.*; Chinnaiyan, A. M.*; Ding, K.* Discovery of YJZ5118: A Potent and Highly Selective Irreversible CDK12/13 Inhibitor with Synergistic Effects in Combination with Akt Inhibition. J. Med. Chem. 2025, 68, 6718-6734.
5)?Tien, J. C.-T.; Zhai, Y.; Wu, R.; Zhang, Y.; Chang, Y.; Cheng, Y.; Todd, A. J. E. Wheeler, C. E.; Li, S.; Mannan, R.; Cheng, C.; Magnuson, B.; Cruz, G.; Cao, Y.; Mahapatra, S.; Stolfi, C.; Cao, X.; Su, F.; Wang, R.; Yang, J.; Zhou, L.; Qiao, Y.; Xiao, L.; Cieslik, M.; Wang, X.; Wang, Z.; Chou, J.; Fearon, E. R.; Ding, K.*; Cho, K. R.*; and Arul M. Chinnaiyan, A. M.* Defining CDK12 as a tumor suppressor and therapeutic target in mouse models of tubo-ovarian high-grade serous carcinoma.?PNAS, 2025, 122 (24) e2426909122
6)?Yang, B.; Xun, Q.; Tian, Y.; Li, H.; Wu, P.; Zhou, Y.; Chang, S.; Wang, Z.*; Ding, K.*; Ma, D.* Discovery of BW710 as a potent, selective and orally bioavailable fibroblast growth factor receptor 2 (FGFR2) inhibitor. Eur. J. Med. Chem.?2025, 287, 117339. DOI: https://doi.org/10.1016/j.ejmech.2025.117339.
7)?Li, J.; Li, L.; Hou, C.; Tian, Z.; Zhou, Y.; Zhang, J.; Ren, X.; Wang, Z.; Huang, W.*; Ding, K.*; Zhou, F.* Discovery of the first potent ROR1 degrader for the treatment of non-small cell lung cancer. Eur. J. Med. Chem.?2025, 286, 117325. DOI: https://doi.org/10.1016/j.ejmech.2025.117325.
8)??Chen, Z.; He, R.; Huang, S.; Zhou, Y.; Zhang, Z.; Wang, Z.; Ding, K.* Discovery of CZY43 as a new small-molecule degrader of pseudokinase HER3. Eur. J. Med. Chem.?2025, 285, 117258. DOI: https://doi.org/10.1016/j.ejmech.2025.117258.
9)?Li, C.; Chen, Y.; Huang, W.; Qiu, Y.; Huang, S.; Zhou, Y.; Zhou, F.; Xu, J.; Ren, X.; Zhang, J.; Wang, Z.; Ding, M.; Ding, K.* Structure-Based Design of “Head-to-Tail” Macrocyclic PROTACs. JACS Au 2024. DOI: 10.1021/jacsau.4c00831.
10)?Tien, J. C.; Luo, J.; Chang, Y.; Zhang, Y.; Cheng, Y.; Wang, X.; Yang, J.; Mannan, R.; Mahapatra, S.; Shah, P.; Wang, X. M.; Todd, A. J.; Eyunni, S.; Cheng, C.; Rebernick, R. J.; Xiao, L.; Bao, Y.; Neiswender, J.; Brough, R.; Pettitt, S. J.; Cao, X.; Miner, S. J.; Zhou, L.; Wu, Y. M.; Labanca, E.; Wang, Y.; Parolia, A.; Cieslik, M.; Robinson, D. R.; Wang, Z.; Feng, F. Y.; Chou, J.; Lord, C. J.; Ding, K.*; Chinnaiyan, A. M.* CDK12 loss drives prostate cancer progression, transcription-replication conflicts, and synthetic lethality with paralog CDK13. Cell. Rep. Med.?2024, 5?(10), 101758. DOI: 10.1016/j.xcrm.2024.101758.
11)??Chang, Y.; Wang, X.; Yang, J.; Tien, J. C.; Mannan, R.; Cruz, G.; Zhang, Y.; Vo, J. N.; Magnuson, B.; Mahapatra, S.; Cho, H.; Dhanasekaran, S. M.; Wang, C.; Wang, Z.; Zhou, L.; Zhou, K.; Zhou, Y.; Zhang, P.; Huang, W.; Xiao, L.; Liu, W. R.; Hamadeh, R.; Su, F.; Wang, R.; Miner, S. J.; Cao, X.; Cheng, Y.; Mehra, R.; Ding, K.*; Chinnaiyan, A. M.* Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition. Cell Rep Med?2024, 5?(10), 101752.?DOI: 10.1016/j.xcrm.2024.101752.
12)?Zhou, L.; Zhou, K.; Chang, Y.; Yang, J.; Fan, B.; Su, Y.; Li, Z.; Mannan, R.; Mahapatra, S.; Ding, M.; Zhou, F.; Huang, W.; Ren, X.; Xu, J.; Wang, G. X.; Zhang, J.; Wang, Z.*; Chinnaiyan, A. M.*; Ding, K.*?Discovery of ZLC491 as a Potent, Selective, and Orally Bioavailable CDK12/13 PROTAC Degrader. J Med Chem?2024, 67?(20), 18247-18264. DOI: 10.1021/acs.jmedchem.4c01596.
13)?Liu, L.; Chen, F.; Li, S.; Yang, T.; Chen, S.; Zhou, Y.; Lin, Z.; Zeng, G.; Feng, P.; Shu, H. B.; Zhou, Q. *; Ding, K.?*; Chen, L. * Human/mouse CD137 agonist, JNU-0921, effectively shrinks tumors through enhancing the cytotoxicity of CD8(+) T cells in cis and in trans. Sci Adv?2024, 10?(34), eadp8647. DOI: 10.1126/sciadv.adp8647.
14)?Wen, C.; Gajjala, P. R.; Liu, Y.; Chen, B.; Bal, M. S.; Sutaria, P.; Yuanyuan, Q.; Zheng, Y.; Zhou, Y.; Zhang, J.; Huang, W.; Ren, X.; Wang, Z.;?Ding, K*.; Chinnaiyan, A. M. *; Zhou, F. * Discovery of the first selective and potent PROTAC degrader for the pseudokinase TRIB2. Eur. J. Med. Chem.?2024, 281, 117016. doi: 10.1016/j.ejmech.2024.117016.
15)?Zhu, Z.; Li, J.; Shen, S.; Al-Furas, H.; Li, S.; Tong, Y.; Li, Y.; Zeng, Y.; Feng, Q.; Chen, K.; Ma, N.; Zhou, F.*; Zhang, Z.; Li, Z.; Pang, J.*; Ding, K.*; Xu, F.* Targeting EGFR degradation by autophagosome degraders. Eur. J. Med. Chem.?2024, 270, 116345. DOI: 10.1016/j.ejmech.2024.116345.
16)??Zhao, Y.; Duan, K.; Fan, Y.; Li, S.; Huang, L.; Tu, Z.; Sun, H.; Cook, G. M.; Yang, J.; Sun, P.; Tan, Y.*; Ding, K.*; Li, Z.* Catalyst-free late-stage functionalization to assemble α-acyloxyenamide electrophiles for selectively profiling conserved lysine residues. Commun. Chem. 2024, 7?(1), 31. DOI: 10.1038/s42004-024-01107-4.
17)?Zhang, H.; Lin, G.; Jia, S.; Zhang, Y.; Wu, J.; Tao, Y.; Huang, W.; Song, M.; Ding, K.*; Ma, D.*; Fan, M.* Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7. Eur. J. Med. Chem. 2024, 263, 115955. DOI: 10.1016/j.ejmech.2023.115955.
18)??Zhang, C.; Liu, Y.; Li, G.; Yang, Z.; Han, C.; Sun, X.; Sheng, C.*; Ding, K.*;?Rao, Y.* Targeting the undruggables-the power of protein degraders. Sci. Bull. 2024, 69?(11), 1776-1797. DOI: 10.1016/j.scib.2024.03.056.
19)?Tang, Z.; Li, J.; Peng, L.; Xu, F.; Tan, Y.; He, X.; Zhu, C.; Zhang, Z. M.; Zhang, Z.*; Sun, P.*; Ding, K.*;?Li, Z.* Novel covalent probe selectively targeting glutathione peroxidase 4 in vivo: potential applications in pancreatic cancer therapy. J. Med. Chem., 2024, 67?(3), 1872-1887. DOI: 10.1021/acs.jmedchem.3c01608.
20)?Qiu, X.; Liu, R.; Ling, H.; Zhou, Y.; Ren, X.; Zhou, F.; Zhang, J.; Huang, W.*; Wang, Z.*; Ding, K.* Discovery of 5-aminopyrido[2,3-d]pyrimidin-7(8H)-one derivatives as new hematopoietic progenitor kinase 1 (HPK1) inhibitors. Eur. J. Med. Chem. 2024, 269, 116310. DOI: 10.1016/j.ejmech.2024.116310.
21)?Niu, P.; Tao, Y.; Lin, G.; Xu, H.; Meng, Q.; Yang, K.; Huang, W.; Song, M.; Ding, K.*; Ma, D.*; Fan, M.* Design and synthesis of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 7 inhibitors. J. Med. Chem. 2024, 67?(8), 6099-6118. DOI: 10.1021/acs.jmedchem.3c01832.
22)?Liu, W.; Bai, Y.; Zhou, L.; Jin, J.; Zhang, M.; Wang, Y.; Lin, R.; Huang, W.; Ren, X.; Ma, N.; Zhou, F.; Wang, Z.; Ding, K.* Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo?activity against acute myeloid leukemia. Eur. J. Med. Chem.?2024, 264, 115974. DOI: 10.1016/j.ejmech.2023.115974.
23)?Liu, L.; Zhao, L.; Yang, L.; Chai, M.; Liu, Z.; Ma, N.; Wang, Y.; Wu, Q.; Guo, J.; Zhou, F.; Huang, W.; Ren, X.; Wang, J.; Ding, M.; Wang, Z.*; Ding, K.* Discovery of LLC355 as an autophagy-tethering compound for the degradation of discoidin domain receptor 1. J. Med. Chem. 2024, 67?(10), 8043-8059. DOI: 10.1021/acs.jmedchem.4c00162.
24)?Liu, L.; Parolia, A.; Liu, Y.; Hou, C.; He, T.; Qiao, Y.; Eyunni, S.; Luo, J.; Li, C.; Wang, Y.; Zhou, F.; Huang, W.; Ren, X.; Wang, Z.*; Chinnaiyan, A. M.*; Ding, K.* Discovery of LLC0424 as a potent and selective in vivo?NSD2 PROTAC degrader. J. Med. Chem. 2024, 67?(9), 6938-6951. DOI: 10.1021/acs.jmedchem.3c01765.
25)?Li, H.; Ke, R.; Zhou, Y.; Chang, S.; Wang, J.; Su, C.; Wu, P.; Yang, B.; Wang, Z.*; Ding, K.*; Ma, D.* Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor. Eur. J. Med. Chem. 2024, 272, 116473. DOI: 10.1016/j.ejmech.2024.116473.
26)?Yu, Z.; He, X.; Wang, R.; Xu, X.; Zhang, Z.; Ding, K.*; Zhang, Z. M.*; Tan, Y.*; Li, Z*. Simultaneous covalent modification of K-Ras(G12D) and K-Ras(G12C) with tunable oxirane electrophiles. J. Am. Chem. Soc. 2023, 145?(37), 20403-20411. DOI: 10.1021/jacs.3c05899.
27)?Wei, Y.; Xu, X.; Jiang, M.; Wang, Y.; Zhou, Y.; Wang, Z.; Zhang, Z.*; Zhou, F.*; Ding, K.* Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders. Eur. J. Med. Chem. 2023, 258, 115580. DOI: 10.1016/j.ejmech.2023.115580.
28)?Lv, S.; Xu, F.; Fan, Y.; Ding, K.*; Li, Z.* Cyclopropenone, cyclopropeniminium ion, and cyclopropenethione as novel electrophilic warheads for potential target discovery of triple-negative breast cancer. J. Med. Chem. 2023, 66?(4), 2851-2864. DOI: 10.1021/acs.jmedchem.2c01889.
29)?Li, C.; Qiao, Y.; Jiang, X.; Liu, L.; Zheng, Y.; Qiu, Y.; Cheng, C.; Zhou, F.; Zhou, Y.; Huang, W.; Ren, X.; Wang, Y.; Wang, Z.*; Chinnaiyan, A. M.*; Ding, K.* Discovery of a first-in-class degrader for the lipid kinase pikfyve. J. Med. Chem. 2023, 66?(17), 12432-12445. DOI: 10.1021/acs.jmedchem.3c00912.
30)?He, R.; Song, Z.; Bai, Y.; He, S.; Huang, J.; Wang, Y.; Zhou, F.; Huang, W.; Guo, J.; Wang, Z.; Tu, Z. C.; Ren, X.; Zhang, Z.; Xu, J.; Ding, K.* Discovery of AXL degraders with improved potencies in triple-negative breast cancer (TNBC) cells. J. Med. Chem. 2023, 66?(3), 1873-1891. DOI: 10.1021/acs.jmedchem.2c01682.
31)?Guan, T.; Li, M.; Song, Y.; Chen, J.; Tang, J.; Zhang, C.; Wen, Y.; Yang, X.; Huang, L.; Zhu, Y.; Wang, H.; Ding, K.*; Zheng, J.*; Zhang, H.*; Liu, T.* Phosphorylation of USP29 by CDK1 governs TWIST1 stability and oncogenic functions.?Adv. Sci. 2023, 10?(11), e2205873. DOI: 10.1002/advs.202205873.
32)?Zhang, Z.; Li, J.; Chen, H.; Huang, J.; Song, X.; Tu, Z. C.; Zhang, Z.; Peng, L.*; Zhou, Y.*; Ding, K.* Design, synthesis, and biological evaluation of 2-formyl tetrahydronaphthyridine urea derivatives as new selective covalently reversible FGFR4 inhibitors. J. Med. Chem. 2022, 65?(4), 3249-3265. DOI: 10.1021/acs.jmedchem.1c01816.
33)?Guo, J.; Xiang, S.; Wang, J.; Zhou, Y.; Wang, Z.; Zhang, Z.*; Ding, K.*; Lu, X.* Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies. Eur. J. Med. Chem. 2022, 228, 114022. DOI: 10.1016/j.ejmech.2021.114022.
34)?Zhang, Y.; Chan, S.; He, R.; Liu, Y.; Song, X.; Tu, Z. C.; Ren, X.; Zhou, Y.; Zhang, Z.*; Wang, Z.*; Zhou, F.*; Ding, K.* 1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino) -1H-pyrazole-4-carboxamide derivatives as new rearranged during transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions. Eur. J. Med. Chem. 2022, 244, 114862. DOI: 10.1016/j.ejmech.2022.114862.
35)?Yang, J.; Chang, Y.; Tien, J. C.; Wang, Z.; Zhou, Y.; Zhang, P.; Huang, W.; Vo, J.; Apel, I. J.; Wang, C.; Zeng, V. Z.; Cheng, Y.; Li, S.; Wang, G. X. *; Chinnaiyan, A. M.*; Ding, K.* Discovery of a highly potent and selective dual PROTAC degrader of CDK12 and CDK13. J. Med. Chem. 2022, 65?(16), 11066-11083. DOI: 10.1021/acs.jmedchem.2c00384.
36)?Xu, F.; Zhang, X.; Chen, Z.; He, S.; Guo, J.; Yu, L.; Wang, Y.; Hou, C.; Ai-Furas, H.; Zheng, Z.; Smaill, J. B.; Patterson, A. V.; Zhang, Z. M.; Chen, L.*; Ren, X.*; Ding, K.* Discovery of isoform-selective Akt3 degraders overcoming osimertinib-induced resistance in non-small cell lung cancer cells. J. Med. Chem. 2022, 65?(20), 14032-14048. DOI: 10.1021/acs.jmedchem.2c01246.
37)?Wang, Z.; Wang, J.; Wang, Y.; Xiang, S.; Song, X.; Tu, Z.; Zhou, Y.; Zhang, Z. M*.; Zhang, Z.*; Ding, K.*; Lu, X.* Discovery of the first highly selective and broadly effective macrocycle-based type II Trk inhibitors that overcome clinically acquired resistance. J. Med. Chem. 2022, 65?(8), 6325-6337. DOI: 10.1021/acs.jmedchem.2c00308.
38)?Wang, Z.*; Huang, W.; Zhou, K.; Ren, X.; Ding, K.* Targeting the non-catalytic functions: a new paradigm for kinase drug discovery? J. Med. Chem. 2022, 65?(3), 1735-1748.?DOI: 10.1021/acs.jmedchem.1c01978.
39)?Wang, Y.; Zhou, Y.; Shi, C.; Liu, J.; Lv, G.; Huang, H.; Li, S.; Duan, L.; Zheng, X.; Liu, Y.; Zhou, H.; Wang, Y.; Li, Z.; Ding, K*; Sun, P.*; Huang, Y.*; Lu, X.*; Zhang, Z. M.* A toxin-deformation dependent inhibition mechanism in the T7SS toxin-antitoxin system of Gram-positive bacteria. Nat. Commun. 2022, 13?(1), 6434. DOI: 10.1038/s41467-022-34034-w.
40)?Lu, J.; Huang, Y.; Huang, J.; He, R.; Huang, M.; Lu, X.; Xu, Y.; Zhou, F.*; Zhang, Z.*; Ding, K.* Discovery of the first examples of threonine tyrosine kinase PROTAC degraders. J. Med. Chem. 2022, 65?(3), 2313-2328. DOI: 10.1021/acs.jmedchem.1c01768.
41)?Li, S.; Zhang, T.; Zhu, S. J.; Lei, C.; Lai, M.; Peng, L.; Tong, L.; Pang, Z.; Lu, X.; Ding, J.; Ren, X.*; Yun, C. H.*; Xie, H.*; Ding, K.* Optimization of brigatinib as new wild-type sparing inhibitors of EGFR(T790M/C797S) mutants. ACS Med. Chem. Lett., 2022, 13?(2), 196-202. DOI: 10.1021/acsmedchemlett.1c00555.
42)?Li, S.; Zhang, P.; Xu, F.; Hu, S.; Liu, J.; Tan, Y.; Tu, Z.; Sun, H.; Zhang, Z. M.; He, Q. Y.; Sun, P.*; Ding, K.*; Li, Z.* Ynamide electrophile for the profiling of ligandable carboxyl residues in live cells and the development of new covalent inhibitors. J. Med. Chem., 2022, 65?(15), 10408-10418. DOI: 10.1021/acs.jmedchem.2c00272.
43)?Li, S.; Si, H.; Song, X.; Lei, C.; He, X.; Wang, J.; Liu, Y.; Zhou, Y.; Song, J. G.; Peng, L.; Tang, X.; Chan, S.; Ren, X.; Tu, Z.; Li, Z.*; Wang, Z.*; Zhang, Z.*; Ding, K.* Discovery of hexahydrofuro[3,2-b]furans as new kinase-selective and orally bioavailable JAK3 inhibitors for the treatment of leukemia harboring a JAK3 activating mutant. J. Med. Chem. 2022, 65?(15), 10674-10690. DOI: 10.1021/acs.jmedchem.2c00922.
44)?Chen, H.; Lai, M.; Zhang, T.; Chen, Y.; Tong, L.; Zhu, S.; Zhou, Y.; Ren, X.; Ding, J.; Xie, H.*; Lu, X.*; Ding, K.* Conformational constrained 4-(1-sulfonyl-3-indol)yl-2 -phenylaminopyrimidine derivatives as new fourth-generation epidermal growth factor receptor inhibitors targeting T790M/C797S mutations. J. Med. Chem., 2022, 65?(9), 6840-6858. DOI: 10.1021/acs.jmedchem.2c00168.
45)?Chan, S.; Zhang, Y.; Wang, J.; Yu, Q.; Peng, X.; Zou, J.; Zhou, L.; Tan, L.; Duan, Y.; Zhou, Y.; Hur, H.; Ai, J.*; Wang, Z.*; Ren, X.*; Zhang, Z.*; Ding, K.* Discovery of 3-aminopyrazole derivatives as new potent and orally bioavailable AXL inhibitors. J. Med. Chem., 2022, 65?(22), 15374-15390. DOI: 10.1021/acs.jmedchem.2c01346.
46)?Xia, Y.; Zou, R.; Escouboué, M.; Zhong, L.; Zhu, C.; Pouzet, C.; Wu, X.; Wang, Y.; Lv, G.; Zhou, H.; Sun, P.*; Ding, K.*; Deslandes, L *; Yuan, S.*; Zhang, Z. M.* Secondary-structure switch regulates the substrate binding of a YopJ family acetyltransferase. Nat. Commun. 2021, 12?(1), 5969. DOI: 10.1038/s41467-021-26183-1.
47)?Jiang, L.; Wang, Y.; Li, Q.; Tu, Z.; Zhu, S.; Tu, S.; Zhang, Z.*; Ding, K.*; Lu, X.* Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta Pharm. Sin. B 2021, 11?(5), 1315-1328.?DOI: 10.1016/j.apsb.2020.11.009.
48)?Huang, M.; Huang, Y.; Guo, J.; Yu, L.; Chang, Y.; Wang, X.; Luo, J.; Huang, Y.; Tu, Z.; Lu, X.; Xu, Y.; Zhang, Z.-M.*; Zhang, Z.*; Ding, K.*?Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors. Eur. J. Med. Chem. 2021, 211, 113023. DOI: 10.1016/j.ejmech.2020.113023.
49)?Fan, Y.; Si, H.; Zhang, Z.; Zhong, L.; Sun, H.; Zhu, C.; Yin, Z.; Li, H.; Tang, G.; Yao, S. Q.; Sun, P.*; Zhang, Z.-M.*; Ding, K.*; Li, Z.* Novel electrophilic warhead targeting a triple-negative breast cancer driver in live cells revealed by "inverse drug discovery". J. Med. Chem. 2021, 64?(21), 15582-15592. DOI: 10.1021/acs.jmedchem.0c02024.
50)?Zhang, X.; Xu, F.; Tong, L.; Zhang, T.; Xie, H.; Lu, X.; Ren, X.*; Ding, K.*?Design and synthesis of selective degraders of EGFR(L858R/T790M) mutant. Eur. J. Med. Chem., 2020, 192, 112199. DOI: 10.1016/j.ejmech.2020.112199.
51)?Zhang, T.; Qu, R.; Chan, S.; Lai, M.; Tong, L.; Feng, F.; Chen, H.; Song, T.; Song, P.; Bai, G.; Liu, Y.; Wang, Y.; Li, Y.; Su, Y.; Shen, Y.; Sun, Y.; Chen, Y.; Geng, M.; Ding, K.*; Ding, J.*; Xie, H.* Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol. Cancer 2020, 19?(1), 90. DOI: 10.1186/s12943-020-01202-9.
52)?Yang, J.; Shibu, M. A.; Kong, L.; Luo, J.; BadrealamKhan, F.; Huang, Y.; Tu, Z. C.; Yun, C. H.*; Huang, C. Y.*; Ding, K.*; Lu, X.* Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. J. Med. Chem. 2020, 63?(5), 2114-2130. DOI: 10.1021/acs.jmedchem.9b00664.
53)?Mo, C.; Zhang, Z.; Li, Y.; Huang, M.; Zou, J.; Luo, J.; Tu, Z. C.; Xu, Y.; Ren, X.*; Ding, K.*; Lu, X.* Design and optimization of 3'-(imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl] -3-carboxamides as selective DDR1 inhibitors. ACS Med. Chem. Lett. 2020, 11?(3), 379-384. DOI: 10.1021/acsmedchemlett.9b00495.
54)?Ma, N.; Hu, J.; Zhang, Z. M.; Liu, W.; Huang, M.; Fan, Y.; Yin, X.; Wang, J.*; Ding, K.*; Ye, W.*; Li, Z.* 2H-Azirine-based reagents for chemoselective bioconjugation at carboxyl residues inside live cells. J. Am. Chem. Soc. 2020, 142?(13), 6051-6059. DOI: 10.1021/jacs.9b12116.
55)?Lu, X.*; Smaill, J. B.; Ding, K.*?Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. J. Med. Chem. 2020, 63?(19), 10726-10741. DOI: 10.1021/acs.jmedchem.0c00507.
56)?Lu, X.*; Smaill, J. B.; Ding, K.* New Promise and Opportunities for Allosteric Kinase Inhibitors. Angew. Chem. ?Int. ?Ed. 2020, 59?(33), 13764-13776. DOI: 10.1002/anie.201914525.
57)?Hu, X.; Xun, Q.; Zhang, T.; Zhu, S.-J.; Li, Q.; Tong, L.; Lai, M.; Huang, T.; Yun, C.-H. *; Xie, H. *; Ding, K.?*; Lu, X. * 2-Oxo-3,4-dihydropyrimido[4,5-d] pyrimidines as new reversible inhibitors of EGFR C797S (Cys797 to Ser797) mutant. Chin. Chem. Lett., 2020, 31?(5), 1281-1287. DOI: 10.1016/j.cclet.2019.09.044.
58)?Fan, Z.; Tian, Y.; Chen, Z.; Liu, L.; Zhou, Q.; He, J.; Coleman, J.; Dong, C.; Li, N.; Huang, J.; Xu, C.; Zhang, Z.; Gao, S.; Zhou, P.*; Ding, K.*; Chen, L.* Blocking interaction between SHP2 and PD-1 denotes a novel opportunity for developing PD-1 inhibitors. EMBO Mol. Med. 2020, 12?(6), e11571. DOI: 10.15252/emmm.201911571.
59)?Duan, Y.; Wang, J.; Zhu, S.; Tu, Z. C.; Zhang, Z.*; Chan, S.*; Ding, K.*?Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors. Eur. J. Med. Chem. 2020, 203, 112552. DOI: 10.1016/j.ejmech.2020.112552.
60)?Chen, H.; Smaill, J. B.; Liu, T.; Ding, K.*; Lu, X.* Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics. J. Med. Chem. 2020, 63?(23), 14404-14424. DOI: 10.1021/acs.jmedchem.0c01312.
61)?Zhu, D.; Huang, H.; Pinkas, D. M.; Luo, J.; Ganguly, D.; Fox, A. E.; Arner, E.; Xiang, Q.; Tu, Z. C.; Bullock, A. N.*; Brekken, R. A.*; Ding, K.*; Lu, X.* 2-Amino-2,3-dihydro-1H-indene-5-carboxamide-based discoidin domain receptor 1 (DDR1) inhibitors: design, synthesis, and in vivo?antipancreatic cancer efficacy. J. Med. Chem. 2019, 62?(16), 7431-7444. DOI: 10.1021/acs.jmedchem.9b00365.
62)?Tan, L.; Zhang, Z.; Gao, D.; Chan, S.; Luo, J.; Tu, Z. C.; Zhang, Z. M.; Ding, K.*; Ren, X.*; Lu, X.* Quinolone antibiotic derivatives as new selective Axl kinase inhibitors. Eur. J. Med. Chem. 2019, 166, 318-327. DOI: 10.1016/j.ejmech.2019.01.065.
63)?Shen, J.; Zhang, T.; Zhu, S. J.; Sun, M.; Tong, L.; Lai, M.; Zhang, R.; Xu, W.; Wu, R.; Ding, J.; Yun, C. H.*; Xie, H.*; Lu, X.*; Ding, K.*?Structure-based design of 5-methylpyrimidopyridone derivatives as new wild-type sparing inhibitors of the epidermal growth factor receptor triple mutant (EGFR(L858R/T790M/C797S)). J. Med. Chem. 2019, 62?(15), 7302-7308. DOI: 10.1021/acs.jmedchem.9b00576.
64)?Peng, L.*; Zhang, Z.; Lei, C.; Li, S.; Zhang, Z.; Ren, X.; Chang, Y.; Zhang, Y.; Xu, Y.; Ding, K.*?Identification of new small-molecule inducers of estrogen-related receptor α (ERRα) degradation. ACS Med. Chem. Lett. 2019, 10?(5), 767-772. DOI: 10.1021/acsmedchemlett.9b00025.
65)?Ma, N.; Zhang, Z. M.; Lee, J. S.; Cheng, K.; Lin, L.; Zhang, D. M.; Hao, P.*; Ding, K.;* Ye, W. C.*; Li, Z.* affinity-based protein profiling reveals cellular targets of photoreactive anticancer inhibitors. ACS Chem. Biol., 2019, 14?(12), 2546-2552. DOI: 10.1021/acschembio.9b00784.
66)?Hu, X.; Wan, B.; Liu, Y.; Shen, J.; Franzblau, S. G.; Zhang, T.*; Ding, K.*; Lu, X.* Identification of pyrazolo[1,5-a]pyridine-3-carboxamide diaryl derivatives as drug resistant antituberculosis agents. ACS Med. Chem. Lett. 2019, 10?(3), 295-299. DOI: 10.1021/acsmedchemlett.8b00410.
67)?Cui, S.; Wang, Y.; Wang, Y.; Tang, X.; Ren, X.; Zhang, L.; Xu, Y.; Zhang, Z.*; Zhang, Z. M.*; Lu, X.*; Ding, K.*?Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors. Eur. J. Med. Chem. 2019, 179, 470-482. DOI: 10.1016/j.ejmech.2019.06.064.
68)?Chang, Y.; Xu, S.; Ding, K.*?Tyrosine kinase 2 (TYK2) allosteric inhibitors to treat autoimmune diseases. J. Med. Chem. 2019, 62?(20), 8951-8952. DOI: 10.1021/acs.jmedchem.9b01612.
69)?Zhu, D.; Guo, H.; Chang, Y.; Ni, Y.; Li, L.; Zhang, Z. M.; Hao, P.*; Xu, Y.; Ding, K.*; Li, Z.* Cell- and tissue-based proteome profiling and dual imaging of apoptosis markers with probes derived from venetoclax and idasanutlin. Angew. Chem. Int. Ed. 2018, 57?(30), 9284-9289. DOI: 10.1002/anie.201802003.
70)?Xun, Q.; Zhang, Z.; Luo, J.; Tong, L.; Huang, M.; Wang, Z.; Zou, J.; Liu, Y.; Xu, Y.; Xie, H.; Tu, Z. C.; Lu, X.*; Ding, K.*?Design, synthesis, and structure-activity relationship study of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidines as new colony stimulating factor 1 receptor (CSF1R) kinase inhibitors. J. Med. Chem. 2018, 61?(6), 2353-2371. DOI: 10.1021/acs.jmedchem.7b01612.
71)?Wang, Z.; Zhang, Y.; Pinkas, D. M.; Fox, A. E.; Luo, J.; Huang, H.; Cui, S.; Xiang, Q.; Xu, T.; Xun, Q.; Zhu, D.; Tu, Z.; Ren, X.; Brekken, R. A.; Bullock, A. N.; Liang, G.*; Ding, K.;* Lu, X.* Design, synthesis, and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl) -4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a dual inhibitor of discoidin domain receptors 1 and 2. J. Med. Chem. 2018, 61?(17), 7977-7990. DOI: 10.1021/acs.jmedchem.8b01045.
72)?Lu, X.*; Zhang, T.; Zhu, S. J.; Xun, Q.; Tong, L.; Hu, X.; Li, Y.; Chan, S.; Su, Y.; Sun, Y.; Chen, Y.; Ding, J.; Yun, C. H.*; Xie, H.*; Ding, K.*?Discovery of JND3229 as a new EGFR(C797S) mutant inhibitor with in vivo?monodrug efficacy. ACS Med. Chem. Lett. 2018, 9?(11), 1123-1127. DOI: 10.1021/acsmedchemlett.8b00373.
73)?Yu, L.; Huang, M.; Xu, T.; Tong, L.; Yan, X. E.; Zhang, Z.; Xu, Y.; Yun, C.; Xie, H.*; Ding, K.*; Lu, X.* A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR(L858R/T790M) mutant with improved pharmacokinetic properties. Eur. J. Med. Chem. 2017, 126, 1107-1117. DOI: 10.1016/j.ejmech.2016.12.006.
74)?Wang, Z.; Zhang, Y.; Bartual, S. G.; Luo, J.; Xu, T.; Du, W.; Xun, Q.; Tu, Z.; Brekken, R. A.; Ren, X.; Bullock, A. N.*; Liang, G.*; Lu, X.*; Ding, K.*?Tetrahydroisoquinoline-7-carboxamide derivatives as new selective discoidin domain receptor 1 (DDR1) inhibitors. ACS Med. Chem. Lett. 2017, 8?(3), 327-332. DOI: 10.1021/acsmedchemlett.6b00497.
75)?Mo, C.; Zhang, Z.; Guise, C. P.; Li, X.; Luo, J.; Tu, Z.; Xu, Y.; Patterson, A. V.; Smaill, J. B.*; Ren, X.*; Lu, X.*; Ding, K.?* 2-Aminopyrimidine derivatives as new selective fibroblast growth factor receptor 4 (FGFR4) Inhibitors. ACS Med. Chem. Lett. 2017, 8?(5), 543-548. DOI: 10.1021/acsmedchemlett.7b00091.
76)?Li, X.; Guise, C. P.; Taghipouran, R.; Yosaatmadja, Y.; Ashoorzadeh, A.; Paik, W. K.; Squire, C. J.; Jiang, S.; Luo, J.; Xu, Y.; Tu, Z. C.; Lu, X.; Ren, X.; Patterson, A. V.*; Smaill, J. B.*; Ding, K.*?2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors. Eur. J. Med. Chem. 2017, 135, 531-543. DOI: 10.1016/j.ejmech.2017.04.049.
77)?Guo, H.; Xu, J.; Hao, P.*; Ding, K.*; Li, Z.* Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid. Chem. Commun. 2017, 53?(69), 9620-9623, 10.1039/C7CC04190J. DOI: 10.1039/C7CC04190J.
78)?Cheng, K.; Lee, J. S.; Hao, P.; Yao, S. Q.; Ding, K.*; Li, Z.* Tetrazole-based probes for integrated phenotypic screening, affinity-based proteome profiling, and sensitive detection of a cancer biomarker. Angew. Chem. Int. Ed. 2017, 56?(47), 15044-15048. DOI: 10.1002/anie.201709584.
79)?Chang, Y.; Lu, X.; Shibu, M. A.; Dai, Y. B.; Luo, J.; Zhang, Y.; Li, Y.; Zhao, P.; Zhang, Z.; Xu, Y.; Tu, Z. C.; Zhang, Q. W.*; Yun, C. H.*; Huang, C. Y.*; Ding, K.*?Structure based design of N-(3-((1h-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as selective leucine-zipper and sterile-α motif kinase (ZAK) inhibitors. J. Med. Chem. 2017, 60?(13), 5927-5932. DOI: 10.1021/acs.jmedchem.7b00572.
80)?Zhang, Z.; Ren, X.; Lu, X.; Wang, D.; Hu, X.; Zheng, Y.; Song, L.; Pang, H.; Yu, R.*; Ding, K.*?GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro?and in vivo. Cancer Lett. 2016, 375?(1), 172-178. DOI: 10.1016/j.canlet.2016.02.017.
81)?Wang, Z.; Bian, H.; Bartual, S. G.; Du, W.; Luo, J.; Zhao, H.; Zhang, S.; Mo, C.; Zhou, Y.; Xu, Y.; Tu, Z.; Ren, X.; Lu, X.; Brekken, R. A.; Yao, L.; Bullock, A. N.*; Su, J.*; Ding, K.*?Structure-based design of tetrahydroisoquinoline-7-carboxamides as selective discoidin domain receptor 1 (DDR1) inhibitors. J. Med. Chem. 2016, 59?(12), 5911-5916.?DOI: 10.1021/acs.jmedchem.6b00140.
82)?Tan, L.; Zhang, Z.; Gao, D.; Luo, J.; Tu, Z. C.; Li, Z.; Peng, L.; Ren, X.*; Ding, K.*?4-Oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new Axl kinase inhibitors. J. Med. Chem. 2016, 59?(14), 6807-6825. DOI: 10.1021/acs.jmedchem.6b00608.
83)?Tang, J.; Wang, B.; Wu, T.; Wan, J.; Tu, Z.; Njire, M.; Wan, B.; Franzblauc, S. G.; Zhang, T.*; Lu, X.*; Ding, K.*?Design, Synthesis, and biological evaluation of pyrazolo[1,5-a]pyridine-3-carboxamides as novel antitubercular agents. ACS Med. Chem. Lett. 2015, 6?(7), 814-818. DOI: 10.1021/acsmedchemlett.5b00176.
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85)?Li, Y.; Zhuang, X.; Peng, L.*; Ding, K.* Synthesis and biological evaluation of 2,7-diphenyl-4H-pyrido[1,2-a]pyrimidin-4-ones as transcriptional function suppressors of estrogenrelated receptor a?(ERR a). Sci. China-Chem 2015, 45?(9), 968-978. DOI: 10.1360/n032015-00104.
86)?Li, Y.; Cheng, H.; Zhang, Z.; Zhuang, X.; Luo, J.; Long, H.; Zhou, Y.; Xu, Y.; Taghipouran, R.; Li, D.; Patterson, A.; Smaill, J.; Tu, Z.; Wu, D.; Ren, X.*; Ding, K.*?N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide derivatives as selective Raf inhibitors. ACS Med. Chem. Lett. 2015, 6?(5), 543-547. DOI: 10.1021/acsmedchemlett.5b00039.
87)?Yang, F.*; Deng, R.; Qian, X. J.; Chang, S. H.; Wu, X. Q.; Qin, J.; Feng, G. K.; Ding, K.*; Zhu, X. F.* Feedback loops blockade potentiates apoptosis induction and antitumor activity of a novel AKT inhibitor DC120 in human liver cancer. Cell Death Dis. 2014, 5?(3), e1114-e1114. DOI: 10.1038/cddis.2014.43.
88)?Lu, X.; Ding, K.*?Novel anaplastic lymphoma kinase inhibitors targeting clinically acquired resistance. J. Med. Chem. 2014, 57?(4), 1167-1169. DOI: 10.1021/jm500178r.
89)?Guise, C. P.; Mowday, A. M.; Ashoorzadeh, A.; Yuan, R.; Lin, W.-H.; Wu, D.-H.; Smaill, J. B.; Patterson, A. V.; Ding, K.*?Bioreductive prodrugs as cancer therapeutics: targeting tumor hypoxia. Chin. J. Cancer 2014, 33?(2), 80-86. DOI: 10.5732/cjc.012.10285.
90)?Cheng, H.; Chang, Y.; Zhang, L.; Luo, J.; Tu, Z.; Lu, X.; Zhang, Q.; Lu, J.; Ren, X.; Ding, K.*?Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. J. Med. Chem. 2014, 57?(6), 2692-2703. DOI: 10.1021/jm500007h.
91)?Zhou, W.; Liu, X.; Tu, Z.; Zhang, L.; Ku, X.; Bai, F.; Zhao, Z.; Xu, Y.*; Ding, K.*; Li, H.* Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. J. Med. Chem. 2013, 56?(20), 7821-7837. DOI: 10.1021/jm401045n.
92)?Xu, T.; Zhang, L.; Xu, S.; Yang, C. Y.; Luo, J.; Ding, F.; Lu, X.*; Liu, Y.; Tu, Z.; Li, S.; Pei, D.; Cai, Q.; Li, H.; Ren, X.; Wang, S.; Ding, K.*?Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives as selective inhibitors of EGFR threonine790 to methionine790 (T790M) mutants. Angew. Chem. Int. Ed. 2013, 52?(32), 8387-8390. DOI: 10.1002/anie.201302313.
93)?Xu, S.; Zhuang, X.; Pan, X.; Zhang, Z.; Duan, L.; Liu, Y.; Zhang, L.; Ren, X.*; Ding, K.*1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as orally bioavailable transcriptional function suppressors of estrogen-related receptor α. J. Med. Chem. 2013, 56?(11), 4631-4640. DOI: 10.1021/jm4003928.
94)?Xu, S.; Xu, T.; Zhang, L.; Zhang, Z.; Luo, J.; Liu, Y.; Lu, X.; Tu, Z.; Ren, X.; Ding, K.*?Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties. J. Med. Chem. 2013, 56?(21), 8803-8813. DOI: 10.1021/jm4012388.
95)?Ren, X.; Pan, X.; Zhang, Z.; Wang, D.; Lu, X.; Li, Y.; Wen, D.; Long, H.; Luo, J.; Feng, Y.; Zhuang, X.; Zhang, F.; Liu, J.; Leng, F.; Lang, X.; Bai, Y.; She, M.; Tu, Z.; Pan, J.; Ding, K.*?Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J. Med. Chem. 2013, 56?(3), 879-894. DOI: 10.1021/jm301581y.
96)?Han, C.; Huang, Z.; Zheng, C.; Wan, L.; Zhang, L.; Peng, S.; Ding, K.*; Ji, H.*; Tian, J.; Zhang, Y.* Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. J. Med. Chem. 2013, 56?(11), 4738-4748. DOI: 10.1021/jm400463q.
97)?Gao, M.; Duan, L.; Luo, J.; Zhang, L.; Lu, X.; Zhang, Y.; Zhang, Z.; Tu, Z.*; Xu, Y.; Ren, X.; Ding, K.* Discovery and optimization of 3-(2-(pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J. Med. Chem. 2013, 56?(8), 3281-3295. DOI: 10.1021/jm301824k.
98)?Li, Y.; Shen, M.; Zhang, Z.; Luo, J.; Pan, X.; Lu, X.; Long, H.; Wen, D.; Zhang, F.; Leng, F.; Li, Y.; Tu, Z.; Ren, X.; Ding, K.*?Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. J. Med. Chem. 2012, 55?(22), 10033-10046. DOI: 10.1021/jm301188x.
99)?Cheng, H.; Wan, J.; Lin, M. I.; Liu, Y.; Lu, X.; Liu, J.; Xu, Y.; Chen, J.; Tu, Z.; Cheng, Y. S.; Ding, K.* Design, synthesis, and in vitro?biological evaluation of 1H-1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents targeting virus nucleoprotein. J. Med. Chem. 2012, 55?(5), 2144-2153. DOI: 10.1021/jm2013503.
100)?Chang, S.; Zhang, L.; Xu, S.; Luo, J.; Lu, X.; Zhang, Z.; Xu, T.; Liu, Y.; Tu, Z.; Xu, Y.; Ren, X.; Geng, M.; Ding, J.; Pei, D.; Ding, K.*?Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine??→ methionine????mutant. J. Med. Chem. 2012, 55?(6), 2711-2723. DOI: 10.1021/jm201591k.?
1）中國首個克服Bcr-AblT315I突變耐藥的1類抗白血病新藥Olverembatinib（奧雷巴替尼（GZD824））于2021年獲批上市；被美國FDA和歐洲委員會授予“孤兒藥”資格，納入美國National Comprehensive Cancer Network (NCCN)2024版白血病診療指南。
2）克服非小細胞肺癌耐藥的1類新藥Limertinib（利厄替尼（ASK120067））于2025年1月獲批上市；
3）HH30134等4個原創(chuàng)候選藥物在中外獲準進入臨床研究。
