磷酸二酯酶-4 抑制剂的研究进展。
Advances in the Development of Phosphodiesterase-4 Inhibitors.
机构信息
Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine of University of Electronic Science and Technology of China, Chengdu 610072, China.
Center for Nanomedicine and Department of Anesthesiology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
出版信息
J Med Chem. 2020 Oct 8;63(19):10594-10617. doi: 10.1021/acs.jmedchem.9b02170. Epub 2020 Jun 10.
Cyclic nucleotide phosphodiesterase 4 (PDE4) specifically hydrolyzes cyclic adenosine monophosphate (cAMP) and plays vital roles in biological processes such as cancer development. To date, PDE4 inhibitors have been widely studied as therapeutics for the treatment of various diseases such as chronic obstructive pulmonary disease, and many of them have progressed to clinical trials or have been approved as drugs. Herein, we review the advances in the development of PDE4 inhibitors in the past decade and will focus on their pharmacophores, PDE4 subfamily selectivity, and therapeutic potential. Hopefully, this analysis will lead to a strategy for development of novel therapeutics targeting PDE4.
环核苷酸磷酸二酯酶 4（PDE4）特异性水解环腺苷酸（cAMP），在癌症发展等生物过程中发挥重要作用。迄今为止，PDE4 抑制剂已被广泛研究作为治疗各种疾病的药物，如慢性阻塞性肺疾病，其中许多已进入临床试验或已被批准为药物。本文综述了过去十年中 PDE4 抑制剂的研究进展，重点讨论了它们的药效团、PDE4 亚家族选择性和治疗潜力。希望本分析能为开发针对 PDE4 的新型治疗药物提供策略。
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