G protein-coupled receptors (GPCRs) detect compounds on the cell surface and are the starting point of a number of medically relevant signaling cascades. Indeed, over 30% of FDA approved drugs target GPCRs, making them a primary target for drug discovery. Computational and experimental high-throughput screening (HTS) approaches of clinically relevant GPCRs are a first-line drug discovery effort in biomedical research. In this opinion, we review recent advances in GPCR HTS. We focus primarily on cell-based assays, and highlight recent advances in in vitro assays using purified receptors, and computational approaches for GPCR HTS. To date, GPCR HTS has led to the identification of new and repurposing of existing drugs, and the deorphanization of GPCRs with unknown ligands. As automation equipment becomes more common, GPCR HTS will move beyond a drug discovery tool to a key technology to probe basic biological processes that will have an outsized impact on personalized medicine.

中文翻译：

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G蛋白偶联受体高通量筛选研究进展

G 蛋白偶联受体 (GPCR) 可检测细胞表面的化合物，并且是许多医学相关信号级联反应的起点。事实上，超过 30% 的 FDA 批准的药物靶向 GPCR，使它们成为药物发现的主要目标。临床相关 GPCR 的计算和实验高通量筛选 (HTS) 方法是生物医学研究中的一线药物发现工作。在这个观点中，我们回顾了 GPCR HTS 的最新进展。我们主要关注基于细胞的检测，并重点介绍使用纯化受体的体外检测的最新进展，以及 GPCR HTS 的计算方法。迄今为止，GPCR HTS 已导致新药物的鉴定和现有药物的再利用，以及具有未知配体的 GPCR 的脱孤。随着自动化设备变得越来越普遍，