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采用生物信息学和化学信息学相结合的方法，开发非对称双价 AMPA 受体正变构调节剂作为神经保护剂。

A combined bioinformatics and chemoinformatics approach for developing asymmetric bivalent AMPA receptor positive allosteric modulators as neuroprotective agents.

机构信息

Chemical Biology Program, Department of Pharmacology & Toxicology, Center for Addiction Research, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555, USA.

出版信息

ChemMedChem. 2013 Feb;8(2):226-30. doi: 10.1002/cmdc.201200554. Epub 2012 Dec 20.

DOI:10.1002/cmdc.201200554
PMID:23281122
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3733225/
Abstract

PAMs new in town! An effective, combined bioinformatics and chemoinformatics approach was applied to the design of novel asymmetric bivalent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor positive allosteric modulators (PAMs) with marked potency in vitro and efficacy in vivo for preventing neuroapoptosis. The novel chemotype could provide pharmacological probes and potential therapeutic agents for glutamatergic hypofunction and its related neurological and psychiatric disorders.

摘要

PAMs 新到小镇！采用有效的组合生物信息学和化学信息学方法，设计了新型不对称双价 α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体正变构调节剂（PAMs），该调节剂具有显著的体外活性和体内预防神经细胞凋亡的功效。这种新型化学结构类型可为谷氨酸能功能低下及其相关神经和精神疾病提供药理学探针和潜在的治疗剂。

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A combined bioinformatics and chemoinformatics approach for developing asymmetric bivalent AMPA receptor positive allosteric modulators as neuroprotective agents.采用生物信息学和化学信息学相结合的方法，开发非对称双价 AMPA 受体正变构调节剂作为神经保护剂。
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