课题组长
姓名：
程建军助理教授 研究员 博士生导师, PhD, 助理教授
职务：
所在院所：
荣誉称号：
教育经历：
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2001/09—2005/06，山东大学，学士
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2005/09—2010/07，中国科学院上海药物研究所，博士
博士后及工作经历：
- 2010/07—2013/10，上海汇伦生命科技，高级研究员
- 2013/11—2016/03，伊利诺伊大学芝加哥分校，博士后
- 2016/03—2022/06，我校，iHuman研究所，副研究员、课题组长
- 2022/07—至今，我校，新葡萄3522登录网页版/iHuman研究所，助理教授（TENURE-TRACK）
课题组简介
研究内容：
1. 基于单胺类GPCR的抗精神疾病药物发现
精神类疾病如精神分裂症、抑郁症主要是与多巴胺受体、血清素受体等单胺类GPCR的功能异常相关。我们以单胺类GPCR为靶标，以“受体-配体”复合物结构为指导，设计合成具有受体亚型高选择性或信号通路“偏向性”的新型小分子化合物，并进行相应的药理药效研究，以获得具有更优药效、更少毒副作用的新型抗精神疾病候选药物。 2. 基于腺苷信号通路的抗肿瘤药物发现 肿瘤微环境中，腺苷是重要的免疫抑制因子。腺苷通过激活腺苷受体发挥免疫抑制作用，而腺苷受体拮抗剂能够拮抗腺苷的免疫抑制作用发挥抗肿瘤活性。我们以腺苷受体为靶标，进行具有新机制的小分子药物的设计合成，并研究其抗肿瘤活性，以获得新型抗肿瘤候选药物。
研究成果展示
1. 基于5-HT2A受体的晶体结构和偏向性激活机制，设计发现不致幻但抗抑郁的新型先导药物IHCH-7086（Science 2022） 2. 基于多巴胺D2受体与5-HT2A受体口袋的晶体结构分析，发现具有多巴胺D2受体高选择性的抗精神分裂症候选药物IHCH-7041（Nature Neuroscience 2022，封面文章） 3. 围绕PCPMA骨架，发现具有抗精神分裂症活性的5-HT2C受体激动剂（J Med Chem 2015; 2016a; 2016b）；具有多巴胺D3受体选择性的配体化合物（J Med Chem 2020）；具有抗精神分裂症活性的多巴胺D2受体部分激动剂（J Med Chem 2021） 4. 腺苷A2a受体拮抗/HDAC活性抑制的双功能抗肿瘤化合物（J Med Chem 2021; Eur J Med Chem 2022）
代表性论文（*第一作者，#通讯作者）
- 1. Cao, Dongmei*; Yu, Jing; Wang, Huan; Luo, Zhipu; Liu, Xinyu; He, Licong; Qi, Jianzhong; Fan, Luyu; Tang, Lingjie; Chen, Zhangcheng; Li, Jinsong; Cheng, Jianjun#; Wang, Sheng#.Structure-based discovery of nonhallucinogenic psychedelic analogs.SCIENCE. 28 Jan 2022. 375(6579).
- 2. Chen, Zhangcheng*; Fan, Luyu; Wang, Huan; Yu, Jing; Lu, Dengyu; Qi, Jianzhong; Nie, Fen; Luo, Zhipu; Liu, Zhen; Cheng, Jianjun#; Wang, Sheng#.Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.NATURE NEUROSCIENCE. Jan 2022.
- 3. Sun, Nan*; Yang, Kexin; Yan, Wenzhong; Yao, Mingyue; Xie, Chengying#; Cheng, Jianjun#; Yu, Chengcheng; Duan, Wenwen; Gu, Xiaoke; Guo, Dong; Jiang, Hualiang.Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response.JOURNAL OF MEDICINAL CHEMISTRY. 01 Mar 2023.
- 4. Liu, Ruiquan*; Qi, Jianzhong; Wang, Huan; Fan, Luyu; Zhang, Pei; Yu, Jing; Tan, Liang; Wang, Sheng#; Cheng, Jianjun#.Transformation of a Dopamine D2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents.JOURNAL OF MEDICINAL CHEMISTRY. 11 May 2023. 66(9).
- 5. Zhang, Haoran*; Yan, Wenzhong; Sun, Yongzhan; Yuan, Haoxing; Su, Limin; Cao, Xudong; Wang, Peng; Xu, Zhou; Hu, Youhui; Wang, Zhongjian; Wang, Yinan; Fu, Kequan; Sun, Ying; Chen, Yupeng#; Cheng, Jianjun#; Guo, Dong#.Long Residence Time at the Vasopressin V-2 Receptor Translates into Superior Inhibitory Effects in Ex Vivo and In Vivo Models of Autosomal Dominant Polycystic Kidney Disease.JOURNAL OF MEDICINAL CHEMISTRY. 09 Jun 2022. 65(11).
- 6. Gu, Xiaoke*; Yuan, Haoxing; Zhao, Wenchao; Sun, Nan; Yan, Wenzhong; Jiang, Chunyu; He, Yan; Liu, Hongli; Cheng, Jianjun#; Guo, Dong#.Optical-Controlled Kinetic Switch: Fine-Tuning of the Residence Time of an Antagonist Binding to the Vasopressin V2 Receptor in In Vitro, Ex Vivo, and In Vivo Models of ADPKD.JOURNAL OF MEDICINAL CHEMISTRY. 01 Dec 2022. 66(2).
- 7. Zhang, Jinfeng*; Luo, Ziwei; Duan, Wenwen; Yang, Kexin; Ling, Lijun; Yan, Wenzhong; Liu, Ruiquan; Wuthrich, Kurt; Jiang, Hualiang#; Xie, Chengying#; Cheng, Jianjun#.Dual-acting antitumor agents targeting the A 2A adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H- pyrazolo[3,4-d]pyrimidin-6-amine derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 05 Jun 2022. 5(236):1-14.
- 8. Wang, Jingjing*; Wu, Meng; Chen, Zhangcheng; Wu, Lijie; Wang, Tian; Cao, Dongmei; Wang, Huan; Liu, Shenhui; Xu, Yueming; Li, Fei; Liu, Junlin; Chen, Na; Zhao, Suwen; Cheng, Jianjun#; Wang, Sheng#; Hua, Tian#.The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands.NATURE COMMUNICATIONS. 23 May 2022. 13(1).
- 9. Yan, Wenzhong*; Fan, Luyu; Yu, Jing; Liu, Ruiquan; Wang, Huan; Tan, Liang; Wang, Sheng#; Cheng, Jianjun#.2-Phenylcyclopropylmethylamine Derivatives as Dopamine D-2 Receptor Partial Agonists: Design, Synthesis, and Biological Evaluation.JOURNAL OF MEDICINAL CHEMISTRY. 09 Dec 2021. 64(23).
- 10. Yan, Wenzhong*; Ling, Lijun; Wu, Yiran; Yang, Kexin; Liu, Ruiquan; Zhang, Jinfeng; Zhao, Simeng; Zhong, Guisheng; Zhao, Suwen; Jiang, Hualiang#; Xie, Chengying#; Cheng, Jianjun#.Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A(2A) Receptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents.JOURNAL OF MEDICINAL CHEMISTRY. 25 Nov 2021. 64(22).
- 11. Duan, Wenwen*; Sun, Ying; Wu, Meng; Zhang, Zhiyuan; Zhang, Taotao; Wang, Huan; Li, Fei; Yang, Lingyun; Xu, Yueming; Liu, Zhi-Jie; Hua, Tian#; Nie, Hong#; Cheng, Jianjun#.Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 15 Dec 2021. 226.
- 12. Chan, H. C. Stephen*; Xu, Yueming; Tan, Liang; Vogel, Horst; Cheng, Jianjun#; Wu, Dong#; Yuan, Shuguang#.Enhancing the Signaling of GPCRs via Orthosteric Ions.ACS CENTRAL SCIENCE. 26 Feb 2020. 6(2):274-282.
- 13. Tan, Liang*; Zhou, Qingtong; Yan, Wenzhong; Sun, Jian; Kozikowski, Alan P.; Zhao, Suwen; Huang, Xi-Ping#; Cheng, Jianjun#.Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.JOURNAL OF MEDICINAL CHEMISTRY. 14 May 2020. 63(9):4579-4602.
- 14. Fan, Luyu*; Tan, Liang; Chen, Zhangcheng; Qi, Jianzhong; Nie, Fen; Luo, Zhipu; Cheng, Jianjun#; Wang, Sheng#.Haloperidol bound D-2 dopamine receptor structure inspired the discovery of subtype selective ligands.NATURE COMMUNICATIONS. 26 Feb 2020. 11(1).
- 15. Zhang, Jinfeng*; Yan, Wenzhong; Duan, Wenwen; Wuthrich, Kurt; Cheng, Jianjun#.Tumor Immunotherapy Using A(2A) Adenosine Receptor Antagonists.PHARMACEUTICALS. Sep 2020. 13(9).
- 16. Peng, Yao*; McCorvy, John D.; Harpsoe, Kasper; Lansu, Katherine; Yuan, Shuguang; Popov, Petr; Qu, Lu; Pu, Mengchen; Che, Tao; Nikolajsen, Louise F.; Huang, Xi-Ping; Wu, Yiran; Shen, Ling; Bjorn-Yoshimoto, Walden E.; Ding, Kang; Wacker, Daniel; Han, Gye Won; Cheng, Jianjun; Katritch, Vsevolod; Jensen, Anders A.; Hanson, Michael A.; Zhao, Suwen; Gloriam, David E.; Roth, Bryan L.#; Stevens, Raymond C.#; Liu, Zhi-Jie#.5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.CELL. 08 Feb 2018. 172(4):719-+.
- 17. Tan, Liang*; Yan, Wenzhong; McCorvy, John D.#; Cheng, Jianjun#.Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.JOURNAL OF MEDICINAL CHEMISTRY. 22 Nov 2018. 61(22):9841-9878.
奖励
- 1. 2022，上海市优秀学术带头人（青年）
- 2. 2020，我校优秀员工
- 3. 2017，上海高校青年东方学者
课题组成员及合影
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姓名：闫文仲
身份：助理研究员
在组时间：2017-至今
邮箱：yanwzh@shanghaitech.edu.cn
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姓名：王欢
身份：助理研究员
在组时间：2018-至今
邮箱：wanghuan1@shanghaitech.edu.cn
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姓名：张金凤
身份：博士后
在组时间：2022-至今
邮箱：zhangjf4@shanghaitech.edu.cn
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姓名：黎慧琼
身份：博士研究生
在组时间：2022-至今
邮箱：lihq@shanghaitech.edu.cn
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姓名：李荣研
身份：硕士研究生
在组时间：2021-至今
邮箱：liry@shanghaitech.edu.cn
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姓名：刘洋洋
身份：硕士研究生
在组时间：2021-至今
邮箱：liuyy3@shanghaitech.edu.cn
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姓名：陈玉晋
身份：硕士研究生
在组时间：2022-至今
邮箱：chenyj2022@shanghaitech.edu.cn
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姓名：黄瑞
身份：硕士研究生
在组时间：2022-至今
邮箱：huangrui2022@shanghaitech.edu.cn
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姓名：吉忻
身份：硕士研究生
在组时间：2022-至今
邮箱：jixin2022@shanghaitech.edu.cn
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姓名：李会林
身份：硕士研究生
在组时间：2022-至今
邮箱：lihl2022@shanghaitech.edu.cn
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姓名：李天恒
身份：本科生
在组时间：2023/06-至今
邮箱：lith2022@shanghaitech.edu.cn
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姓名：毛建航
身份：硕士研究生
在组时间：2020-2023
邮箱：maojh@shanghaitech.edu.cn
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