磷酸二酯酶-4抑制剂的研发进展
Advances in the development of phosphodiesterase-4 inhibitors.
作者信息
Li Gang, He Dengqin, Cai Xiaojia, Guan Wen, Zhang Yali, Wu Jia-Qiang, Yao Hongliang
机构信息
Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, 510260, China.
School of Biotechnology and Health Sciences, Wuyi University, 22 Dongchengcun, Jianmen, 529020, China.
出版信息
Eur J Med Chem. 2023 Mar 15;250:115195. doi: 10.1016/j.ejmech.2023.115195. Epub 2023 Feb 9.
Phosphodiesterase 4 (PDE4) hydrolyzes cyclic adenosine monophosphate (cAMP) and plays a vital roles in many biological processes. PDE4 inhibitors have been widely studied as therapeutics for the treatment of various diseases, including asthma, chronic obstructive pulmonary disease (COPD) and psoriasis. Many PDE4 inhibitors have progressed to clinical trials and some have been approved as therapeutic drugs. Although many PDE4 inhibitors have been approved to enter clinical trials, however, the development of PDE4 inhibitors for the treatment of COPD or psoriasis has been hampered by their side effects of emesis. Herein, this review summarizes advances in the development of PDE4 inhibitors over the last ten years, focusing on PDE4 sub-family selectivity, dual target drugs, and therapeutic potential. Hopefully, this review will contribute to the development of novel PDE4 inhibitors as potential drugs.
磷酸二酯酶4（PDE4）可水解环磷酸腺苷（cAMP），并在许多生物学过程中发挥重要作用。PDE4抑制剂作为治疗包括哮喘、慢性阻塞性肺疾病（COPD）和银屑病在内的各种疾病的药物已得到广泛研究。许多PDE4抑制剂已进入临床试验阶段，有些已被批准作为治疗药物。然而，尽管许多PDE4抑制剂已被批准进入临床试验，但用于治疗COPD或银屑病的PDE4抑制剂的开发却因其呕吐副作用而受到阻碍。在此，本综述总结了过去十年中PDE4抑制剂的开发进展，重点关注PDE4亚家族选择性、双靶点药物和治疗潜力。希望本综述将有助于新型PDE4抑制剂作为潜在药物的开发。
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