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Advances in the Development of Phosphodiesterase-4 Inhibitors.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-07 , DOI: 10.1021/acs.jmedchem.9b02170 Ting Peng 1 , Baowen Qi 2 , Jun He 3 , Hengming Ke 4 , Jianyou Shi 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-07 , DOI: 10.1021/acs.jmedchem.9b02170 Ting Peng 1 , Baowen Qi 2 , Jun He 3 , Hengming Ke 4 , Jianyou Shi 1
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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.
中文翻译：
磷酸二酯酶4抑制剂的开发进展。
环状核苷酸磷酸二酯酶4（PDE4）特异性水解环状单磷酸腺苷（cAMP），并在生物学过程（例如癌症发展）中发挥重要作用。迄今为止，已经广泛研究了PDE4抑制剂作为用于治疗诸如慢性阻塞性肺疾病的各种疾病的治疗剂，并且其中许多已经发展到临床试验或已被批准为药物。本文中，我们回顾了过去十年中PDE4抑制剂的开发进展，并将重点关注其药效团，PDE4亚家族选择性和治疗潜力。希望这种分析将导致开发针对PDE4的新型疗法的策略。
更新日期：2020-04-07
中文翻译：
磷酸二酯酶4抑制剂的开发进展。
环状核苷酸磷酸二酯酶4（PDE4）特异性水解环状单磷酸腺苷（cAMP），并在生物学过程（例如癌症发展）中发挥重要作用。迄今为止，已经广泛研究了PDE4抑制剂作为用于治疗诸如慢性阻塞性肺疾病的各种疾病的治疗剂，并且其中许多已经发展到临床试验或已被批准为药物。本文中，我们回顾了过去十年中PDE4抑制剂的开发进展，并将重点关注其药效团，PDE4亚家族选择性和治疗潜力。希望这种分析将导致开发针对PDE4的新型疗法的策略。
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