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氨基糖苷类及其衍生物作为靶向核糖体的配体。

Aminoglycoside and its derivatives as ligands to target the ribosome.

作者信息

Tok Jeffrey B-H, Bi Lanrong

机构信息

York College and Graduate Center, The University of New York, Department of Medicinal Chemistry, Jamaica, NY 11451, USA.

出版信息

Curr Top Med Chem. 2003;3(9):1001-19. doi: 10.2174/1568026033452131.

Abstract

Protein synthesis is a central function in cellular physiology, and this important process is the target of many naturally occurring antibiotics and toxins. One such antibiotic is the aminoglycoside, which has been widely utilized in the clinical in the last fifty years due to their low cost and reliable activities. However the usage and applications of aminoglycosides have been severely limited due to their numerous side effects and resistance mechanism acquired by bacteria. Advances in understanding their mechanism of action have led to attempts in developing novel aminoglycoside-derivatives that would potentially eliminate harmful side effects and be resistant to aminoglycoside-modifying enzymes. This account provides a brief introduction to the various classes of antibiotics that target the ribosome, and also provide highlights in recent advancement of the synthesis of aminoglycoside analogs.

摘要

蛋白质合成是细胞生理学的核心功能,这一重要过程是许多天然抗生素和毒素的作用靶点。一种这样的抗生素是氨基糖苷类,由于其成本低且活性可靠,在过去五十年里已在临床上广泛使用。然而,由于其众多副作用以及细菌获得的耐药机制,氨基糖苷类的使用和应用受到了严重限制。对其作用机制理解的进展促使人们尝试开发新型氨基糖苷类衍生物,这些衍生物可能消除有害副作用并对氨基糖苷类修饰酶具有抗性。本综述简要介绍了靶向核糖体的各类抗生素,并突出了氨基糖苷类似物合成的最新进展。

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