School of Biological Sciences, The University of Auckland, 3A Symonds Street, Auckland, 1010, New Zealand.
School of Biological Sciences and Surgical and Translational Research Centre, The University of Auckland, 3A Symonds Street, Auckland, 1010, New Zealand.
ChemMedChem. 2024 Sep 16;19(18):e202400131. doi: 10.1002/cmdc.202400131. Epub 2024 Jul 30.
Integrin proteins have received a significant increase in attention in recent scientific endeavors. The current trend uses the pre-established knowledge that the arginyl-glycyl-aspartic acid (RGD) structural motif present in the A20FMDV2 peptide is highly selective for the integrin class αvβ6 which is overexpressed in many cancer types. This review will provide an extensive overview of the existing literature research to date to the best of our knowledge, highlighting significant improvements and drawbacks of structure-activity relationships (SAR) work undertaken, aiding future research to identify established SAR for an informed design of future A20FMDV2 mimetic inhibitors. Herein, the review aims to collate the existing structural chemical modifications present on A20FMDV2 in the literature to highlight key structural analogues that display more potent biological activity.
近年来，整合素蛋白在科学研究中受到了极大的关注。目前的趋势是利用已有的知识，即 A20FMDV2 肽中存在的精氨酸-甘氨酸-天冬氨酸（RGD）结构基序高度选择性地与许多癌症类型中过度表达的整合素 αvβ6 类结合。这篇综述将提供迄今为止的现有文献研究的广泛概述，据我们所知，突出了结构-活性关系（SAR）工作的显著改进和缺点，以帮助未来的研究确定已建立的 SAR，从而为未来的 A20FMDV2 模拟抑制剂的设计提供信息。在此，综述旨在整理文献中 A20FMDV2 上现有的结构化学修饰，以突出显示显示出更强生物活性的关键结构类似物。
