Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China.
Curr Med Chem. 2011;18(7):964-76. doi: 10.2174/092986711794940879.
Aminopeptidases play essential roles in protein maturation, activation, and stability as well as in the degradation and regulation of hormonal and nonhormonal peptides that can serve as important enzyme targets for drug design. This review will focus on an effective inhibitor of aminopeptidases, bestatin, including work to find better inhibitors in the past three decades that has sought to optimize bestatin and prospective developments in bestatin optimization in the future.
氨肽酶在蛋白质成熟、激活和稳定性以及激素和非激素肽的降解和调节中发挥着重要作用,这些肽可以作为药物设计的重要酶靶标。这篇综述将集中讨论氨肽酶的一种有效抑制剂——亮抑酶肽,包括过去三十年寻找更好抑制剂的工作,旨在优化亮抑酶肽,并对未来亮抑酶肽的优化进行展望。