Tavassoli Ali
Chemistry, University of Southampton, Southampton SO17 1BJ, United Kingdom.
Curr Opin Chem Biol. 2017 Jun;38:30-35. doi: 10.1016/j.cbpa.2017.02.016. Epub 2017 Mar 1.
Cyclic peptide libraries have demonstrated significant potential when employed against challenging targets such as protein-protein interactions. While a variety of methods for library generation exist, genetically encoded libraries hold several advantages over their chemically synthesized counterparts; they are more readily accessible and allow straightforward hit deconvolution. One method for the intracellular generation of such libraries is split-intein circular ligation of peptides and proteins (SICLOPPS). Here we detail and discuss the deployment of SICLOPPS libraries for the identification of cyclic peptide inhibitors of a variety of targets.
当用于对抗诸如蛋白质-蛋白质相互作用等具有挑战性的靶点时,环肽文库已展现出巨大潜力。虽然存在多种构建文库的方法,但与化学合成的文库相比,基因编码文库具有多个优势;它们更容易获得,并且能直接进行命中反卷积分析。细胞内生成此类文库的一种方法是肽和蛋白质的分裂内含肽环化连接(SICLOPPS)。在此,我们详细阐述并讨论SICLOPPS文库在鉴定多种靶点的环肽抑制剂方面的应用。