Tanasova Marina, Fedie Joseph R
Department of Chemistry, Michigan Technological University, 1400 Townsend Drive, Houghton, MI, 49931, USA.
Chembiochem. 2017 Sep 19;18(18):1774-1788. doi: 10.1002/cbic.201700221. Epub 2017 Aug 1.
Facilitative carbohydrate transporters-Gluts-have received wide attention over decades due to their essential role in nutrient uptake and links with various metabolic disorders, including diabetes, obesity, and cancer. Endeavors directed towards understanding the mechanisms of Glut-mediated nutrient uptake have resulted in a multidisciplinary research field spanning protein chemistry, chemical biology, organic synthesis, crystallography, and biomolecular modeling. Gluts became attractive targets for cancer research and medicinal chemistry, leading to the development of new approaches to cancer diagnostics and providing avenues for cancer-targeting therapeutics. In this review, the current state of knowledge of the molecular interactions behind Glut-mediated sugar uptake, Glut-targeting probes, therapeutics, and inhibitors are discussed.
易化性碳水化合物转运蛋白——葡萄糖转运蛋白(Gluts)——几十年来一直备受广泛关注,因为它们在营养物质摄取中起着至关重要的作用,并且与包括糖尿病、肥胖症和癌症在内的各种代谢紊乱存在关联。旨在理解Glut介导的营养物质摄取机制的努力催生了一个多学科研究领域,涵盖蛋白质化学、化学生物学、有机合成、晶体学和生物分子建模。Gluts成为癌症研究和药物化学的有吸引力的靶点,从而推动了癌症诊断新方法的开发,并为癌症靶向治疗提供了途径。在这篇综述中,我们将讨论关于Glut介导的糖摄取背后的分子相互作用、Glut靶向探针、治疗方法和抑制剂的当前知识状态。