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丁克
发布时间:2016-09-01

丁克博士,197312月出生。英国皇家化学会Fellow,暨南大学药学院教授、博士生导师。

【受教育经历】

2001/12 ~ 2005/2 美国密西根大学(the University of MichiganAnn Arbor),肿瘤中心,博士后研究。导师:Shaomeng Wang 教授。

1998/9 ~ 2001/7复旦大学,化学系(与中国科学院上海有机化学研究所联合培养),生物有机化学博士。导师:马大为教授。

1995/9 ~ 1998/7中国药科大学,药学院,药物化学硕士。导师:邢为凡教授。

1991/9 ~ 1995/7 中国药科大学,药学院,药学学士,化学制药专业。

【研究工作经历】

2016/6 ~  暨南大学药学院院长、教授。

2008/10 ~ 2016/6 中国科学院广州生物医药与健康研究院化学生物学研究所,研究员,副所长。

2008/06,入选中科院百人计划

2006/03 ~ 至今 中国科学院广州生物医药与健康研究院,研究员,博士生导师。

2005/03 ~ 2006/03美国密西根大学,医学院,Research Investigator

【获得荣誉和奖励】

2016,中组部国家万人计划领军人才(已公示)

2016,英国皇家化学会Fellow

2015科技部中青年科技创新领军人才

2014,获得国家杰出青年基金

2014,第三批百名南粤杰出人才培养工程支持计划

2012,国务院政府特殊津贴

2012,第六届药明康德生命化学研究奖

2012中科院百人计划期终评估优秀(全中科院比例<20%

2009,第十届广东省丁颖科技奖

【学术社团任职】

2015中国药学会药物化学专业委员会副主任委员;

2015,中国药学会应用药理学专业委员会委员。

2015MedChemComm. 副主编

2014J. Chin. Pharm. Sci.(中国药学会), 编委;

2013J. Med. Chem. 顾问编委(Advisory Editorial Board Member);

2011,中国药学会药物化学专业委员会,委员;

2010 ACS Med. Chem. Lett.,顾问编委(Advisory Editorial Board Member);

2010,广州市科学技术协会第九届委员会委员;

2009,广东省药学会药物化学专业委员会,副主任委员;

【研究领域】

重点围绕肿瘤和代谢性疾病等重大临床需求,设计和合成同时具有生物活性和成药性的成(类)药性先导化合物,为创新药物研究奠定基础。

近年来,成功地设计和合成了:

1世界首个亚型选择性ERRa激动剂(国际同行评价)作为新型抗代谢性疾病药物候选物(转让香港CASIGEN Pharma Inc.公司);

2)可克服慢性粒性白血病(CML)临床耐药的新一代Bcr-AblT315I突变体抑制剂(转让广州顺健,已获CFDA临床批件);

3)可克服非小细胞肺癌(NSCLC)对Gefitinib等临床获得性耐药的全新特异性EGFRT790M突变抑制剂(转让南京奥赛康药业);

4)具有治疗肿瘤和肺纤维化良好潜力的世界首个选择性DDR1抑制剂(国际同行评价);

5)可克服耐药结核菌的新型抗结核分子(转让广州艾格医药)等。

6)早期在美国还设计和合成了Spirooxindolep53-MDM2相互作用阻断剂转让世界著名大型药企Sanofi,并进入I期临床研究。

代表性论文

1.          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.* and Ding, K.* Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J. Med. Chem. 2016, 59, 5911–5916. (封面文章)

2.          Tan, L.; Zhang, Z.; Gao, D.; Luo, J.; Tu, Z.-C.; Li, Z.; Peng, L.; Ren, X.*; and Ke Ding.* 4-Oxo-1, 4-Dihydroquinoline-3-Carboxamide Derivatives as New Axl Kinase Inhibitors. J. Med. Chem. 2016, DOI: 10.1021/acs.jmedchem.6b00608.

3.          Li, Y.; Lu, X.; Ren, X.* and Ding, K.* Small Molecule Discoidin Domain Receptor Kinase Inhibitors and Potential Medical Applications. J. Med. Chem. 2015, 58, 3287–3301.

4.          Lu, X. and Ding, K.* Novel Anaplastic Lymphoma Kinase Inhibitors Targeting Clinically Acquired Resistance. J. Med. Chem. 2014, 57, 1167–1169.

5.          Cheng, H.; Chang, Y.; Zhang, L.; Luo, J.; Tu, Z.; Lu, X.; Zhang, Q.; Lu, J.; Ren, X.; and 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, 2692–2703.

6.          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. and Ding, K.* Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Bcr-Abl and overcomes clinically acquired mutation-induced resistance against imatinib. J. Med. Chem. 2013, 56, 879–894.

7.          Gao, M.; Duan, L.; Luo, J.; Zhang, L.; Lu, X.; Zhang, Y.; Zhang, Z.; Tu, Z.; Xu, Y.; Ren, X. and 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, 3281–3295.

8.          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.; and Ding, K.* Tricyclic Pyrimidines as Selective Inhibitors of EGFR Threonine790 ® Methionine790 (T790M) Mutants. Angew. Chem. Int. Edt. 2013, 52, 8387–8390.

9.          Xu, S.; Zhuang, X.; Pan, X.; Zhang, Z.; Duan, L.; Liu, Y.; Zhang, L.; Ren, X. and 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, DOI: 10.1021/jm4003928

10.       Han, C.; Huang, Z.; Zheng, C.; Wan, L.; Zhang, L.; Peng, S.; Ding, K.*; Ji, H.*; Tian, J. and 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, DOI: 10.1021/jm400463q.

11.       Zhou, W.; Liu, X.; Tu, Z.; Zhang, L.; Ku, X.; Bai, F.; Zhao, Z.; Xu, Y.;* Ding, K.* and Li, H.* Discovery of pteridin-7(8H)-one-based Irreversible Inhibitors targeting Epidermal Growth Factor Receptor (EGFR) Kinase T790M/L858R mutant. J. Med. Chem.2013, DOI: 10.1021/jm401045n

12.       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-dihydro pyrimido [4,5-d]pyrimidinyl Derivatives as New Irreversible Epidermal Growth Factor Receptor Inhibitors with Improved Pharmacokinetic Properties. J. Med. Chem.2013, DOI: 10.1021/jm4012388.

13.       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 Threonine315→Isoleucine315 Mutant. J. Med. Chem. 2012, 55, 10033-10046.

14.       Cheng, H.; Wan, J.; Lin, M.-I.; Liu, Y.; Lu, X.; Liu, J.; Xu, Y.; Chen, J.; Tu, Z.; Cheng, Y.-S. E.; 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, 2144-2153.

15.       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 Threonine790 → Methionine790 Mutant. J. Med. Chem. 2012, 55, 2711-2723.

16.       Peng, L.; Gao, X.; Duan L.; Ren, X.; Wu, D. and Ding, K.* Identification of Pyrido[1,2-α]pyrimidine-4-ones as New Molecules Improving the Transcriptional Functions of Estrogen-Related Receptor α. J. Med. Chem. 2011, 54, 7729–7733.