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从双结合位点乙酰胆碱酯酶抑制剂到多靶点导向配体(MTDLs):阿尔茨海默病治疗的一大进步。

From dual binding site acetylcholinesterase inhibitors to multi-target-directed ligands (MTDLs): a step forward in the treatment of Alzheimer's disease.

作者信息

Bolognesi Maria Laura, Minarini Anna, Rosini Michela, Tumiatti Vincenzo, Melchiorre Carlo

机构信息

Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

Mini Rev Med Chem. 2008 Sep;8(10):960-7. doi: 10.2174/138955708785740652.

Abstract

Alzheimer's disease is a complex neurodegenerative disorder with a multifaceted pathogenesis. This fact has long halted the development of effective anti-Alzheimer drugs. Recently, however, basis for a therapeutic strategy based on multi-target-directed ligands has been formed. In this context, dual binding site acetylcholinesterase inhibitors represent a suitable starting point. The rational modification of their structures to provide them with additional biological properties has emerged as a successful approach.

摘要

阿尔茨海默病是一种具有多方面发病机制的复杂神经退行性疾病。这一事实长期以来阻碍了有效抗阿尔茨海默病药物的研发。然而,最近基于多靶点导向配体的治疗策略的基础已经形成。在这种背景下,双结合位点乙酰胆碱酯酶抑制剂是一个合适的起点。对其结构进行合理修饰以赋予它们额外的生物学特性已成为一种成功的方法。

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