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个人简介

2001.09 – 2005.06,山东大学药学院,药学学士 2005.09 – 2010.07,中国科学院上海药物研究所,药物化学博士(导师:杨玉社) 2010.07 – 2013.10,上海汇伦生命科技有限公司,高级研究员、部门经理 2013.11 – 2016.03,美国伊利诺伊大学芝加哥校区,博士后(导师:Alan P. Kozikowski) 2016.03至今,上海科技大学iHuman研究所,Research Associate Professor 、PI

研究领域

GPCRs play important roles in many physiological and pathophysiological conditions and their dysregulations play causal roles in many diseases. Accordingly, more than 30% of known small molecule drugs target GPCRs to exert their therapeutic effects. We focus on important GPCRs, including both well-established as well as emerging GPCR targets, for the design of novel small molecular ligands. These ligands will be useful as tool compounds for the biological study of GPCRs, and more importantly, as novel drug-like compounds that have therapeutic potential and translational value. Besides conventional GPCR agonists and antagonists, the design and discovery of “biased” GPCR ligands is also one of our most important research directions. Biased ligands are attracting extensive attention as they are being investigated as novel therapeutics with enhanced efficacy and/or reduced side effects compared to balanced agonists or antagonists. We focus on central nervous system (CNS) diseases, for example schizophrenia and depression, as well as (immuno-)oncology, for the design and discovery of novel therapeutics.

近期论文

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Cao D#, Yu J#, Wang H#, Luo Z#, Liu X#, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J*, Wang S*. Structure-based discovery of non-hallucinogenic psychedelic analogs. Science, 2022, 375, 403-411. Chen Z#, Fan L#, Wang H#, Yu J#, Lu D#, Qi J, Nie F, Luo Z, Liu Z, Cheng J*, Wang S*. Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. Nat Neurosci, 2022, 25, 39–49. Yan W#, Fan L#, Yu J, Liu R, Wang H, Tan L, Wang S*, Cheng J*. 2-Phenylcyclopropyl-methylamine (PCPMA) derivatives as dopamine D2 receptor partial agonists: Design, synthesis and biological evaluation. J Med Chem, 2021, 64, 17239-17258. Yan W#, Ling L#, Wu Y, Yang K, Liu R, Zhang J, Zhao S, Zhong G, Zhao S, Jiang H*, Xie C*, Cheng J*. Structure-based design of dual-acting compounds targeting adenosine A2A receptor and histone deacetylase as novel tumor immunotherapeutic agents. J Med Chem, 2021, 64, 16573-16597. Duan W#, Sun Y#, Wu M#, Zhang Z, Zhang T, Wang H, Li F, Yang L, Xu Y, Liu Z-J, Hua T*, Nie H*, Cheng J*. Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis. Eur J Med Chem, 2021, 226, 113878. Tan L#, Zhou Q#, Yan W, Sun J, Kozikowski AP, Zhao S, Huang X-P*, Cheng J*. Design and Synthesis of Bitopic 2‑Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. J Med Chem, 2020, 63, 4579-4602. Fan L#, Tan L#, Chen Z, Qi J, Nie F, Luo Z, Cheng J*, Wang S*. Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands. Nat Commun, 2020, 11, 1074. Chan HCS#, Xu Y#, Tan L#, Vogel H, Cheng J*, Wu D*, Yuan S*. Enhancing the Signaling of GPCRs via Orthosteric Ions, ACS Cent Sci, 2020, 6, 274−282. Tan L, Yan W, McCorvy JD*, Cheng J*. Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. J Med Chem, 2018, 61, 9841−9878.

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