在离子通道药物发现中使用自动膜片钳电生理学平台:行业视角。

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Drug Discovery Pub Date : 2024-05-01 Epub Date: 2024-03-13 DOI:10.1080/17460441.2024.2329104
Marc Rogers, Alison Obergrussberger, Artem Kondratskyi, Niels Fertig
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引用次数: 0

摘要

简介:自动膜片钳(APC)现已成为学术界、生物技术和制药公司以及合同研究组织(CRO)用于离子通道药物发现的成熟技术,可用于通道病研究、化合物筛选、靶点验证和心脏安全性测试等多种应用:离子通道是一类重要的药物和已批准的药物靶点。作者回顾了离子通道药物发现的现状,以及涉及 APC 的离子通道研究中令人兴奋的新进展。其中包括离子通道药物发现中的原生细胞和 iPSC 衍生细胞、通道病研究、离子通道药物发现中的细胞器和生物制剂等主题:我们相信,APC 将继续在离子通道药物发现中发挥关键作用,不仅在 "经典 "药物筛选、靶点验证和心脏安全性测试方面,而且将这些应用扩展到高通量细胞器官记录和光遗传学。这样,随着 APC 功能和应用的进步,再加上高分辨率低温电子显微镜结构,离子通道药物发现将重新焕发活力,从而使越来越多的离子通道配体进入临床开发阶段。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Using automated patch clamp electrophysiology platforms in ion channel drug discovery: an industry perspective.

Introduction: Automated patch clamp (APC) is now well established as a mature technology for ion channel drug discovery in academia, biotech and pharma companies, and in contract research organizations (CRO), for a variety of applications including channelopathy research, compound screening, target validation and cardiac safety testing.

Areas covered: Ion channels are an important class of drugged and approved drug targets. The authors present a review of the current state of ion channel drug discovery along with new and exciting developments in ion channel research involving APC. This includes topics such as native and iPSC-derived cells in ion channel drug discovery, channelopathy research, organellar and biologics in ion channel drug discovery.

Expert opinion: It is our belief that APC will continue to play a critical role in ion channel drug discovery, not only in 'classical' hit screening, target validation and cardiac safety testing, but extending these applications to include high throughput organellar recordings and optogenetics. In this way, with advancements in APC capabilities and applications, together with high resolution cryo-EM structures, ion channel drug discovery will be re-invigorated, leading to a growing list of ion channel ligands in clinical development.

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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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