Barlow Nicholas, Thompson Philip E
Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia.
Front Pharmacol. 2020 Sep 25;11:585930. doi: 10.3389/fphar.2020.585930. eCollection 2020.
The insulin regulated aminopeptidase (IRAP) has been proposed as an important therapeutic target for indications including Alzheimer's disease and immune disorders. To date, a number of IRAP inhibitor designs have been investigated but the total number of molecules investigated remains quite small. As a member the M1 aminopeptidase family, IRAP shares numerous structural features with the other M1 aminopeptidases. The study of those enzymes and the development of inhibitors provide key learnings and new approaches and are potential sources of inspiration for future IRAP inhibitors.
胰岛素调节氨肽酶(IRAP)已被提议作为包括阿尔茨海默病和免疫紊乱等适应症的重要治疗靶点。迄今为止,已经研究了多种IRAP抑制剂设计,但所研究的分子总数仍然相当少。作为M1氨肽酶家族的一员,IRAP与其他M1氨肽酶具有许多结构特征。对这些酶的研究以及抑制剂的开发提供了关键的经验教训和新方法,并且是未来IRAP抑制剂潜在的灵感来源。