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程魁

 


 

姓名:程魁

职称:教授,博士生导师

联系邮箱:chengk@smu.edu.cn

联系电话:020-61647192



学习经历:

2008.9-2011.6   南京大学,生物学,博士

2009.10-2011.5  美国科罗拉多大学与南京大学联合培养,化学生物学



工作经历:

2016.2-至今      南方医科大学,教授

2014.10-2016.1   清华大学,助理研究员

2011.7-2014.9    科罗拉多大学,博士后



研究方向:

1. 抗炎免疫类新药的发现;

2. 合成药物化学;

3. 分子探针的设计及细胞信号通路研究。



主要获奖情况:

1. 广东省“珠江学者”青年拔尖人才(2018)

2. 广东省药物化学“青年珠江学者”,2016。

3. 教育部自然科学奖二等奖(第5完成人),2009。

4. 湖北省优秀硕士学位论文,2007。



主要科研课题:

1. 广州市科技计划项目,新型靶向TLR2小分子激活剂的发现及其肿瘤免疫机制研究,2019.04-2022.03, 主持。

2. 国家自然科学基金面上项目,新型抗动脉粥样硬化TLR3高选择性抑制剂的结构优化及作用机制研究 (81773558)2018.01-2021.12, 主持。

3. 广东省青年珠江学者项目,珠江学者配套科研经费 (C1034077)2016.10-2019.9,主持。

4. 南方医科大学高层次人才引进科研项目 (C1033269)2016.3-2019.2,主持。



承担课程:

《药物化学》、《有机化学》



代表性论文: 

1. Tang, X.S.; Yang, J.; Wang, W.Q.; Zeng, Y.N.; Li, J.P.; Lin S.S.; Nandakumar, K.S.; Cheng, K.* “Immunotherapy for Treating Methamphetamine, Heroin and Cocaine Use Disorders”. Drug Discov. Today 2019, doi: 10.1016/j.drudis.2019.07.009. (IF 6.88, 小类I区)

2. Yang, J.; Tang, X.S.; Nandakumar, K.S.; Cheng, K.* “Autophagy induced by STING, an unnoticed and primordial function of cGAS”. Cell. Mol. Immunol. 2019, 16, 683-684. doi: 10.1038/s41423-019-0240-2. (IF 8.23, 大类2区)

3. Bi, J.J.; Wang, W.Q.; Du, J.X.; Chen, K.; Cheng, K.* “Structure-activity relationship study and biological evaluation of SAC-Garlic acid conjugates as novel anti-inflammatory agents”. Eur. J. Med. Chem. 2019, 179, 233-245. (IF 4.83, 药学小类I区) doi: 10.1016/j.ejmech.2019.06.059

4. Cen, X.; Zhu, G.Z.; Yang, J.J.; Guo, J.Y.; Jin, J.B.; Nandakumar, K.S.; Yang, W.; Yin, H.; Liu, S.W.; Cheng, K.* “TLR1/2 Specific Small-molecule Agonist Suppresses Leukemia cancer cell growth by stimulating Cytotoxic T lymphocytes”. Adv. Sci. 2019, 6, 1802042. (IF 15.80, 大类1区)doi: 10.1002/advs.201802042 

5. Chen, Z.; Cen, X.; Yang, J.; Lin, Z.; Liu, M.; Cheng, K.* “Synthesis of urea analogues bearing N-alkyl-N'-(thiophen-2-yl) scaffold and evaluation of their innate immune response to toll-like receptors”. Eur. J. Med. Chem. 2019, 169, 42-52. (IF 4.83, 药学小类I区) doi: 10.1016/j.ejmech.2019.02.067

6. Chen, Z.; Cen, X.; Yang, J.; Tang, X.; Cui, K.; Cheng, K.* “Structure-based discovery of a specific TLR1-TLR2 small molecule agonist from ZINC drug library database”. Chem. Comm. 2018, 54, 11411-11414 (IF 6.16, 大类1区) doi:10.1039/C8CC06618C

7. Cen, X.; Cheng, K.* “Ter-cell, a new target for hepatocellular carcinoma therapy”. ChemBioChem 2018, 19, 2254-2256. (IF 2.59, 药学3区) doi: 10.1002/cbic.201800410

8. Cen, X.; Liu, S.W.; Cheng, K.* “The Role of Toll-Like Receptor in Inflammation and Tumor Immunity”. Front. Pharmacol. 2018, 9, 878. (IF 3.84, 药学2)doi: 10.3389/fphar.2018.00878

9. Bhattacharyya, S.*; Wang, W.; Qin, W.; Cheng, K.; Coulup, S.; Chavez, S.; Raparia, K.; De Almeida, L. M.; Stehlik, C.; Tamaki, Z.; Yin, H.*; Varga, J.* “TLR4-Dependent Fibroblast Activation Drives Persistent Organ Fibrosis in Skin and Lung”. JCI Insight 2018, 3, e98850. (IF 6.01)

10. Xu, Y.; Chen, S.J.; Cao, Y.; Zhou, P.Z.; Chen, Z.P.; Cheng, K.* “Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents”. Eur. J. Med. Chem. 2018, 154, 253-266. (IF 4.83, 药学小类I区)doi: 10.1016/j.ejmech.2018.05.033

11. Cai, S.Y.; Zhu, G.Z.; Cen, X.H.; Bi J.J.; Zhang, J.R.; Tang, X.S.; Chen, K.; Cheng, K. * “Synthesis, structure-activity relationships and preliminary mechanism study of N-benzylideneaniline derivatives as potential TLR2 inhibitors”. Bioorg. Med. Chem. 2018, 26, 2041-2050. (IF 2.80,医学/药学3) doi: 10.1016/j.bmc.2018.03.001

12. Zhu, G.Z.; Xu, Y.; Cen, X.H.; Nandakumar, K.S.; Liu, S.W.*; Cheng, K.* “Targeting pattern-recognition receptors to discover new small molecule immune modulators”. Eur. J. Med. Chem. 2018, 154, 82-92. (IF 4.83, 药学小类I区)doi: 10.1016/j.ejmech.2017.12.026

13. Xu, Q.; Zhu, G.Z.; Li, J.;*and Cheng, K.;* “Development of Antibacterial Drugs by Targeting Toll-Like Receptors”, Curr. Top. Med. Chem. 2017, 17, 270-277. (IF 3.44, 医学/药学3区)doi: 10.2174/1568026616666160829161639

14. Bajo, M.; Montgomery, S. E.; Cates, L. N.; Nadav, T.; De Lucchi, A.; Cheng, K.; Yin, H.; Crawford, E. F.; Roberts, A. J.; Roberto, M.; "Evaluation of TLR4 Inhibitor, T5342126, in Modulation of Ethanol Drinking Behavior in Alcohol Dependent Mice", Alcohol Alcohol. 2016, 51, 541-548. (IF 2.77) 

15. Yan, L.; Liang, J.; Yao, C.; Wu, P.; Zeng, X.; Cheng, K.; Yin, H.; " Pyrimidine Triazole Thioether Derivatives as Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitors", ChemMedChem 2016, 11, 822-826 (IF 3.01)

16. Xu, Q.; Jiang, S.; Cheng, K.; Yin, H.; "Progress in Immunomodulators Targeting Toll-Like Receptors", Prog. Pharm. Sci. 2016, 40, 42-55 . [Link]

17. Cheng, K.; Gao, M.; Godfroy, J. I.; Brown, P. N.; Yin, H.; “Specific activation of the TLR1-TLR2 heterodimer by small-molecule agonists”, Sci. Adv. 2015, 1, e1400139. (Science新子刊,IF:12.80). doi: 10.1126/sciadv.1400139

18. Daniele, S. G.; Beraud, D.; Davenport, C.; Cheng, K.; *Yin, H.; *Maguire-Zeiss, K. A.; "Activation of MyD88-Dependent TLR1/2 Signaling by Misfolded Alpha-Synuclein, A Protein Linked to Neurodegenerative Disorders", Sci. Signal. 2015, 8, ra45 (IF 6.48) .doi: 10.1126/scisignal.2005965

19. Yan, L.; de Jesus, A. J.; Tamura, R.; Li, V.; Cheng, K.; Yin, H.; "Curvature sensing MARCKS-ED peptides bind to membranes in a stereo-independent manner", J. Pept. Sci. 2015, 21, 577-585. (IF: 2.08) 

20. Gao, M.‡; Cheng, K. ‡; Yin, H. “Targeting Protein-Protein Interfaces Using Macrocyclic Peptides”, Biopolymers-Pept. Sci., 2015, 104, 310-316. (IF: 1.84). doi: 10.1002/bip.22625

21. D'Atri, L. P.; Etulain, J.; Rivadeneyra, L.; Lapponi, M. J.; Centrurion, M.; Cheng, K.; Yin, H.; Schattner, M.; "Expression and Functionality of Toll-Like Receptor 3 in the Megakaryocytic Lineage", J. Thromb. Haemost. 2015, 13, 839-850 (IF 4.66). 

22. Gao, M. ‡; London, N.; Cheng, K. ‡; Tamura, R.; Jin, J.; Schueler-Furman, O.; Yin, H.; "Rationally Designed Macrocyclic Peptides as Synergistic Agonists of LPS-Induced Inflammatory Response", Tetrahedron 2014, 70, 7664-7668. (IF 2.37, ‡ Co-first author) doi: 10.1016/j.tet.2014.07.026

23. Wang, X. H.; Grace, P. M.; Pham, M. N.; Cheng, K.; Strand, K. A.; Smith, C.; Li, J.; Watkins, L. R.; Yin, H.; "Rifampin Inhibits Toll-Like Receptor 4 Signaling by Targeting Myeloid Differentiation Protein 2 and Attenuates Neuropathic Pain", FASEB J. 2013, 27, 2713-2722. (IF 5.39) 

24. Cheng, K.; Xue, J.Y.; Zhu, H.L.; “Design, synthesis and antibacterial activity studies of thiazole derivatives as potent ecKAS III inhibitors”, Bioorg. Med. Chem. Lett. 2013, 23, 4235-4238. (IF: 2.44, 医学/药学3区) doi: 10.1016/j.bmcl.2013.05.006

25. Cheng, K.; Wang, X. H.; Zhang, S. T.; Yin, H.; “Discovery of Small Molecule Inhibitors of the TLR1-TLR2 Complex”, Angew. Chem. Int. Edit. 2012, 51, 12246-12249. [Cover Article] [C&EN] (IF: 12.25, 综合1区) doi:10.1002/anie.201204910

26. Zhang, S. T.; Cheng, K.; Wang, X. H.; Yin, H.; “Selection, Synthesis, and Anti-Inflammatory Evaluation of the Arylidene Malonate Derivatives as TLR4 Signaling Inhibitor”, Bioorg. Med. Chem. 2012, 20, 6073-6079. (IF: 2.80)

27. Miyauchi, K.; Urano,E.; Takeda, S.; Murakami, T.; Okada, Y.; Cheng, K.; Yin, H.; Masato, K.; Komano, J.; “Toll-like receptor (TLR) 3 as a surrogate sensor of retroviral infection in human cells”, Biochem. Biophys. Res. Commun. 2012, 424, 519-523. (IF: 2.70) 

28. Wang, X. H.; Loram, L. C.; Ramos, K.; de Jesus, A.; Thomas, J.; Cheng, K.; Reddy, A.; Somogyi, A. A.; Hutchinson, M. R.; Watkins, L. R.; Yin, H.; "Morphine activates neuroinflammation in a manner parallel to endotoxin ", Proc. Natl. Acad. Sci. U. S. A. 2012, 109, 6325-6330. [Nature Research Highlights] (IF: 9.58) (被引135次)doi: 10.1073/pnas.1200130109

29. Cheng, K.; Wang, X. H.; Yin, H.; “Small Molecule Inhibitors of the TLR3/dsRNA Complex”, J. Am. Chem. Soc. 2011, 133, 3764-3767. (IF: 14.65, 综合1区) doi: 10.1021/ja111312h

30. Chavez, S. A.; Martinko, A. J.; Lau, C.; Pham, M. N.; Cheng, K.; Mollnes, T. E.; Yin, H.; “Development of Beta-Amino Alcohol Derivatives that Inhibit Toll-Like Receptor 4 Mediated Inflammatory Response as Potential Antiseptics”, J. Med. Chem. 2011, 54, 4659-4669. (IF: 6.05). doi: 10.1021/jm2003365

31. Cheng, K.; Zheng, Q. Z.; Hou, J.; Zhou, Y.; Liu, C. H.; Zhao, J.; Zhu, H. L.; “Synthesis, molecular modeling and biological evaluation of PSB as targeted antibiotics”, Bioorg. Med. Chem. 2010, 18, 2447-2455. (IF: 2.80, 医学/药学3区) doi: 10.1016/j.bmc.2010.02.052

32. Fu, J.; Cheng, K.; Zhang, Z. M.; Fang, R. Q.; Zhu, H. L.; “Synthesis, structure and structure-activity relationship analysis of caffeic acid amides as potential antimicrobials”, Eur. J. Med. Chem. 2010, 45, 2638-2643. (IF: 4.83)

33. Cheng, K.; Zheng, Q. Z.; Qian, Y.; Shi, L.; Zhao, J.; Zhu, H. L.; “Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics”, Bioorg. Med. Chem. 2009, 17, 7861-7871. (IF: 2.80, 医学/药学3区)doi: 10.1016/j.bmc.2009.10.037

34. Cheng, K.; Zheng, Q. Z.; Zhu, H. L.; “Syntheses, structures and urease inhibitory activities of mononuclear cobalt(III) and 1D cobalt(II) complexes with ligands derived from 3-formylsalicylic acid”, Inorg. Chem. Commun. 2009, 19, 1116-1119. (IF: 1.75) doi: 10.1016/j.inoche.2009.09.001

 

 

专利:

1. Yin, H.; Cheng, K. “2-(4-Aryl-1H-Imidazol-1-yl)Aniline Compounds”, Prov. Appl. 2014, 61/989,603. PCT Int. Appl. 2015, US2015/29780.

2. Yin, H.; Cheng, K. “Antagonists of the Toll-Like Receptor 1/2 Complex”, Prov. Appl. 2012, 61/676,992; PCT Int. Appl. 2013, US2013/52517; USA Appl. 2014, 14/417,676; EU Appl. 2015, 13826030.2; Patent No. US 9,517,993 B2, issued on December 13, 2016. (已授权,此项专利已经与企业合作进行临床前研究)

3. Yin, H.; Cheng, K. “Modulators of TLR3/dsRNA Complex and Uses Thereof”, Prov. Appl. 2011, 61/434,492; PCT Int. Appl. 2012, US2012/021207; USA Appl. 2013, 13/980,874; EU Appl. 2013, 12736857.9; Patent No. US 9,409,880 B2, issued on August 9, 2016. (已授权,licensed by Tocris Bioscience, UK)

4. “Antitumor activity of benzoic nitrogen mustard derivatives and their preparation”, Originator: Zhu, H. L.; Zeng, Q. Z.; Cheng, K.; Jiao Q. C.; Patent (China) 200910036290.4

5. 程魁,朱耿桢。1,4-二苯基-1H-咪唑和2,4-二苯基噻唑类衍生物及其制备方法和用途,国际发明专利申请号:PCT/CN2018/082243,2018年4月9日申请。

6. 程魁,许尧。一种咔唑β-氨基醇类衍生物及其制备方法和用途,专利申请号:201810122217.8,2018年2月7日申请。

7. 程魁,许尧。一种取代苯酚β-氨基醇类衍生物及其制备方法和用途,专利申请号:201810122219.7,2018年2月7日申请。

8. 程魁,陈之朋,刘叔文。2-硫脲基(脲基)噻吩-3-甲酸酯类衍生物及其用途,专利申请号:201811074103.7,2018年9月14日申请。

9. 程魁,毕静杰。N-(苯甲酰基)-L-半胱氨酸甲酯类衍生物及其制备方法和用途,专利申请号:201910395765.2,2019年5月14日申请。



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