环腺苷酸(cAMP)特异性磷酸二酯酶4(PDE4)抑制剂是治疗炎症性疾病药物研究热点之一。PDE4抑制剂可通过增加cAMP浓度,进而抑制多种炎症细胞的炎症反应。许多针对炎症的PDE4靶向抑制剂目前正处于各期临床试验,如GSK256066治疗哮喘,罗氟司特和GSK256066治疗慢性阻塞性肺病,替托司特治疗炎性肠病,apremilast治疗皮肤病及关节炎等。本文就PDE4抑制剂靶向治疗炎症性疾病的研究新进展作一综述。
cAMP-specific phosphodiesterase type 4 (PDE4) is one of the hot targets for treatment of inflammatory diseases. PDE4 inhibitors can suppress inflammation by increasing the concentration of cAMP in inflammatory cells. The efficacy and safety evaluations of several PDE4 inhibitors are currently carried on in clinical trials, for example GSK256066 in asthma, roflumilast and GSK256066 in chronic obstructive pulmonary disease, tetomilast in inflammatory bowel disease, and apremilast in dermatitis and arthritis etc. This article reviews the recent progress on PDE4-targeted therapy for inflammatory diseases.
国家自然基金项目(30800497, 81170536 );浙江省医药卫生优秀青年科技人才专项科研基金(2008QN009)
宋顺德,汤慧芳 . 环腺苷酸磷酸二酯酶4抑制剂靶向治疗炎症性疾病研究新进展[J]. 浙江大学学报(医学版), 2014, 43(3): 353-358. SONG Shun-de, TANG Hui-fang . Progress in PDE4 targeted therapy for inflammatory diseases. Journal of ZheJiang University(Medical Science), 2014, 43(3): 353-358.
http://www.zjujournals.com/xueshu/med/CN/10.3785/j.issn.10089292.2014.05.015 或 http://www.zjujournals.com/xueshu/med/CN/Y2014/V43/I3/353
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