摘要
综述近年来亲环素配体在构效关系研究、合成及应用方面的进展,展望了今后的研究动向。亲环素是一类具有肽基脯氨酸顺反异构酶活性的免疫亲和素,广泛分布于各种组织细胞内。它参与脯氨酸肽键的顺反异构化、线粒体膜通透性转变、细胞内及细胞间信号传导等多种生理活动。亲环素配体是与亲环素有一定结合能力的化合物。目前研究的亲环素配体主要是具有免疫抑制或细胞保护作用的抑制剂。
The progresses in the SAR study, synthesis and application of ligands of cyclophilins in recent years have been reviewed, and the perspective also described. Cyclophilins comprise a superfamily of ubiquitously expressed immunophilins with peptidyl-prolyl isomerase activity which plays roles in peptidylprolyl cis-trans isomerization, mitochondrial permeability transition, intraceUular and intercellular communications. Ligands of cyclophilins are of the compounds with the ability to bind to cyclophilins. Now, the most of researches of ligands of cyclophilins focus on inhibitors with activities of immunosuppression or cellular protection.
出处
《药学进展》
CAS
2005年第10期448-453,共6页
Progress in Pharmaceutical Sciences
关键词
亲环素
亲环素配体
环孢素A
构效关系
合成
Cyclophilins
Ligands of cyclophilins
Cyclosporin A
Structure-activity relationship
Synthesis
