磷酸二酯酶5抑制剂研发进展  

Phosphodiesterase 5 Inhibitor Research Progress

作　　者：刘碧秀 吴婧 骆田田 冯贻东 LIU Bixiu;WU Jing;LUO Tiantian;FENG Yidong(Shenzhen Neptunus Pharmaceutical Research Institute Co.,Ltd.,Shenzhen 518057,China;China Resources Sanjiu Medical&Pharmaceutical Co.,Ltd.,Shenzhen 518110,China)

机构地区：[1]深圳海王医药科技研究院有限公司,广东深圳518057 [2]华润三九医药股份有限公司,广东深圳518110

出　　处：《生物化工》2024年第5期215-220,共6页Biological Chemical Engineering

基　　金：“十三五”国家科技重大专项重大新药创制(2017ZX09301036)。

摘　　要：磷酸二酯酶(Phosphodiesterase,PDE)是一类重要的催化酶,通过调节胞内的环磷酸腺苷(cyclic Adenosine Monophosphate,cAMP)和环磷酸鸟苷(cyclic Guanosine Monophosphate,cGMP)影响相应的生物学功能。PDE5是PDE中开发较为成功的药物靶点,已有多个上市药物,主要用于肺动脉高压和勃起功能障碍。但在2011年后,针对该靶点的药物研发热度降低。本文针对PDE5与其抑制剂的开发进行概述并对未来基于该靶点的开发方向进行简要分析。Phosphodiesterases,an important class of catalytic enzymes,affect the corresponding biological function,by adjusting the ring of intracellular cyclic adenosine monophosphate(cAMP)and cyclic guanosine phosphate(cGMP).As a successful drug target,several drugs are developed based on inhibiting PDE5,one sub-class of PDE,which is mainly used for pulmonary hypertension and erectile dysfunction.However,drug development for this target slows significantly after 2011.In this review,we summarize the development of PDE5 and its inhibitors and briefly analyze the future development based on this target.

关 键 词：磷酸二酯酶5 西地那非 他达拉非 

分 类 号：TQ463[化学工程—制药化工]