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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents
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A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents

机译：脂肪酸酰胺水解酶（FAAH）抑制剂作为潜在治疗剂的透视综述

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摘要

Fatty acid amide hydrolase (FAAH) is an important enzyme creditworthy of hydrolyzing endocannabinoids and related-amidated signalling lipids, discovery of which has pioneered novel arena of pharmacological canvasses to unwrap its curative potency in various diseased circumstances. It presents contemporary basis for understanding molecules regulating and mediating inflammatory reactions, pain, anxiety, depression, and neurodegeneration. FAAH inhibitors form vital approach for discovery of therapeutic agents that are concerned with local elevation of endocannabinoids under certain stimuli, debarring adverse/unwanted secondary effects from global activation of cannabinoid receptors by exogenous cannabimimetics. During past decades, several molecules with excellent potency developed through tailor-made approaches entered into clinical trials, but none could reach market. Hence, hunt for novel, non-toxic and selective FAAH inhibitors are on horizon. This review summarizes present perception on FAAH in conjunction with its structure, mechanism of catalysis and biological functions. It also foregrounds recent development of molecules belonging to diverse chemical classes as potential FAAH inhibitors bobbing up from in-depth chemical, mechanistic and computational studies published since 2015-November 2019, focusing on their potency. This review will assist readers to obtain rationale on FAAH as potential target for addressing various disease conditions, acquiring significant knowledge on recently established inhibitor scaffolds and their development potentials. New technologies including MD-MM simulations and 3D-QSAR studies allow mechanistic characterization of enzyme. Assessment of in-vitro and in-vivo efficacy of existing FAAH inhibitors will facilitate researchers to design novel ligands utilizing modern drug design methods. The discussions will also impose precaution in decision making process, quashing possibility of late stage failure. (C) 2020 Elsevier Masson SAS. AU rights reserved.
机译：脂肪酸酰胺水解酶（FAAH）是一种重要的酶信誉，其是水解的内凸蛋白和相关酰胺化的信号脂质，发现其具有促进的药理学诊断的新阶段，以解开其各种患病情况的治疗效力。它为了解调节和介导炎症反应，疼痛，焦虑，抑郁和神经变性的分子，呈现当代的当代基础。 FAAH抑制剂形成了治疗剂的重要方法，该治疗剂涉及在某些刺激下涉及内胆碱素的局部升高，从外源大麻素来自全局激活大麻素受体的全局激活的替代副/不需要的二次效果。在过去的几十年中，通过定制的方法进入临床试验，几个具有优异效力的分子，但无可以达到市场。因此，寻找新颖，无毒和选择性的FAAH抑制剂在地平线上。本综述总结了对FAAH的目前与其结构，催化机制和生物学功能的影响。它还前景地区最近发展属于不同化学课程的分子，因为潜在的FAAH抑制剂从2015年11月以来发表的深入化学，机械和计算研究，重点是他们的效力。本综述将协助读者获得FAAH的理由，作为解决各种疾病条件的潜在目标，以获得最近建立的抑制作用脚手架及其发展潜力的重要知识。包括MD-MM模拟的新技术和3D-QSAR研究允许酶的机械表征。对现有的FAAH抑制剂的体外和体内疗效评估将促进研究人员利用现代药物设计方法设计新型配体。讨论还将在决策过程中施加预防措施，急转阶段失败的可能性。 （c）2020 Elsevier Masson SAS。 AU权利保留。

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