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康东伟 教授

一、基本情况

康东伟,男,1990年3月出生,山东聊城人,教授,博士生导师,入选山东省优青、山东大学齐鲁青年学者、科学影响力排行榜全球前2%科学家等人才计划。申请人近五年主持国家自然科学基金2项、国家重点研发计划子课题1项以及其它省部级和博士后基金6项;以(共)第一/通讯作者在Cell、J Med Chem(15篇)、J Med Virol、Acta Pharm Sin B、Elife、Eur J Med Chem等国际著名期刊发表SCI论文50余篇,文章累计被引3000余次,H-index为30;获授权发明专利25项(美国专利4项);参编抗艾滋病药物化学领域国内首部系统性著作《基于靶标的抗艾滋病药物研究》。发现10余个抗病毒及抗精神分裂症候选化合物,其中抗艾滋病候选药物K-5a2于2023年获国家药监局临床批件。

地址:山东省济南市文化西路44号山东大学药学院

E-mails: kangdongwei@126.com; kangdongwei@sdu.edu.cn;

个人网址:https://www.researchgate.net/profile/Kang-Dongwei

二、研究方向

主要围绕严重危害人类健康的病毒感染(艾滋病、痘病毒、副黏病毒和黄病毒等)以及未满足临床需求的重大慢病(糖尿病、精神分裂症等),通过结构生物学导向的合理药物设计、活性筛选体系的建立与表型筛选、原创靶标结构解析与虚拟筛选开展原创药物先导化合物的发现与优化,为新药发现提供优质的药物原创靶标和候选药物。

三、学习与工作经历

1. 2024.01-至今山东大学,教授,博士生导师

2. 2020.10-2023.12 山东大学,研究员,硕士生导师

3. 2018.07-2020.09山东大学,特别资助类博士后

4. 2015.09-2018.06山东大学,药物化学,博士,导师:刘新泳

5. 2012.09-2015.06山东大学,制药工程,硕士,导师:刘新泳

6. 2008.09-2012.06河北工业大学,制药工程,本科

四、承担课题

1.科技部重点研发计划子课题,2023YFC2308900-02,2024.01-2026.12,主持

2.国家自然科学基金面上项目,82273773,2023.01-2026.12,主持

3.山东省优秀青年基金,ZR2020YQ61,2021.01-2023.12,主持

4.国家自然科学基金青年基金,81903453,2020.01-2022.12,主持

5.中国博士后科学基金特别资助项目,2019T120596,2019.04-2021.03,主持

6.江苏省自然科学基金青年基金,SBK2019041035,2019.07-2022.06,主持

7.山东省博士后创新项目专项资金,2019.07-2021.06,主持

8.山东省自然科学基金博士基金,ZR201808060045,2019.07-2022.06,主持

9.中国博士后科学基金面上资助项目(一等),2018M640641,2018.07-2020.07,主持

五、近五年代表性论文(限10篇)

1.Shang P#, Rong N#, Jiang JJ#, Cheng J#, Zhang MH#,Kang D#, Qi L#, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y*, Li Q*, Shao ZH*, Yang F*, Sun JP*. Structural and signaling mechanisms of TAAR1 enabled preferential agonist design.Cell. 2023 Nov 22;186(24):5347-5362.e24.

2.Zhao F, Zhang H, Xie M, Meng B, Liu N, Dun C, Qin Y, Gao S, De Clercq E, Pannecouque C, Tang YJ, Zhan P*, Liu X*,Kang D*. Structure-Based Optimization of 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Exploiting the Tolerant Regions of the Non-Nucleoside Reverse Transcriptase Inhibitors' Binding Pocket.J Med Chem.2023 Feb 9;66(3):2102-2115.

3.Sun Y, Zhou Z, Feng D, Jing L, Zhao F, Wang Z, Zhang T, Lin H, Song H, De Clercq E, Pannecouque C, Zhan P*, Liu X*,Kang D*. Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs.J Med Chem. 2022 Dec 8;65(23):15608-15626.

4.Kang D*, Sun Y, Feng D, Gao S, Wang Z, Jing L, Zhang T, Jiang X, Lin H, De Clercq E, Pannecouque C, Zhan P*, Liu X*. Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.J Med Chem. 2022 Feb 10;65(3):2458-2470.

5.Wang Z, Zalloum WA, Wang W, Jiang X, De Clercq E, Pannecouque C,Kang D*,Zhan P*, Liu X*. Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles.J Med Chem. 2021 Sep 23;64(18):13658-13675.

6.Kang D*, Ruiz FX, Sun Y, Feng D, Jing L, Wang Z, Zhang T, Gao S, Sun L, De Clercq E, Pannecouque C, Arnold E*, Zhan P*, Liu X*. 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.J Med Chem.2021 Apr 8;64(7):4239-4256.

7.Kang D, Feng D, Tiziana G, Zou J, Wei F, Zhao T, Huang B, Sun Y, Samuel D, De Clercq E, Pannecouque C, Zhan P*, Liu X*.Exploring the hydrophobic channel of NNIBP led to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs.Acta Pharmaceutica Sinica B.2020 May;10(5):878-894.

8.Kang D, Feng D, Sun Y, Fang Z, Wei F, De Clercq E, Pannecouque C*, Liu X*, Zhan P*. Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.J Med Chem. 2020 May 14;63(9):4837-4848.

9.Kang D, Ruiz FX, Feng D, Pilch A, Zhao T, Wei F, Wang Z, Sun Y, Fang Z, De Clercq E, Pannecouque C, Arnold E*, Liu X*,Zhan P*. Discovery and Characterization of Fluorine-Substituted Diarylpyrimidines Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.J Med Chem.2020 Feb 13;63(3):1298-1312.

10.Kang D, Zhang H, Wang Z, Zhao T, Ginex T, Luque FJ, Yang Y, Wu G, Feng D, Wei F, Zhang J, De Clercq E, Pannecouque C, Chen CH, Lee KH, Murugan NA, Steitz TA*, Zhan P*, Liu X*.Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.J Med Chem. 2019 Feb 14;62(3):1484-1501.

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