Scalise Mariafrancesca, Console Lara, Galluccio Michele, Pochini Lorena, Indiveri Cesare
Department of DiBEST (Biologia, Ecologia, Scienze della Terra) Unit of Biochemistry and Molecular Biotechnology, via Bucci 4C, University of Calabria, 87036 Arcavacata di Rende, Italy.
ACS Omega. 2020 Jan 28;5(5):2069-2080. doi: 10.1021/acsomega.9b04078. eCollection 2020 Feb 11.
Chemical modification of proteins is a vintage strategy that is still fashionable due to the information that can be obtained from this approach. An interesting application of chemical modification is linked with membrane transporters. These proteins have peculiar features such as the presence of hydrophobic and hydrophilic domains, which show different degree of accessibility to chemicals. The presence of reactive residues in the membrane transporters is at the basis of the chemical targeting strategy devoted to investigating structure/function relationships; in particular, information on the substrate binding site, regulatory domains, dimerization domains, and the interface between hydrophilic loops and transmembrane domains has been obtained over the years by chemical targeting. Given the difficulty in handling membrane transporters, their study experienced a great delay, particularly concerning structural information. Chemical targeting has been applied with reasonable success to some membrane transporters belonging to the families SLC1, SLC6, SLC7, and SLC22. Furthermore, some data on the potential application of chemical targeting in pharmacology are also discussed.
蛋白质的化学修饰是一种古老的策略，由于可以从该方法中获得相关信息，至今仍很流行。化学修饰的一个有趣应用与膜转运蛋白有关。这些蛋白质具有独特的特征，例如存在疏水和亲水结构域，它们对化学物质的可及程度不同。膜转运蛋白中反应性残基的存在是致力于研究结构/功能关系的化学靶向策略的基础；多年来，通过化学靶向已经获得了关于底物结合位点、调节结构域、二聚化结构域以及亲水环与跨膜结构域之间界面的信息。鉴于处理膜转运蛋白存在困难，它们的研究经历了很大的延迟，特别是在结构信息方面。化学靶向已成功应用于一些属于SLC1、SLC6、SLC7和SLC22家族的膜转运蛋白。此外，还讨论了化学靶向在药理学中的潜在应用的一些数据。
