Key aspects of modern GPCR drug discovery

IF 2.7 4区生物学 Q2 BIOCHEMICAL RESEARCH METHODS SLAS Discovery Pub Date : 2024-01-01 DOI:10.1016/j.slasd.2023.08.007

Phil Addis , Utsav Bali , Frank Baron , Adrian Campbell , Steven Harborne , Liz Jagger , Gavin Milne , Martin Pearce , Elizabeth M Rosethorne , Rupert Satchell , Denise Swift , Barbara Young , John F Unitt

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Abstract

G-protein-coupled receptors (GPCRs) are the largest and most versatile cell surface receptor family with a broad repertoire of ligands and functions. We've learned an enormous amount about discovering drugs of this receptor class since the first GPCR was cloned and expressed in 1986, such that it's now well-recognized that GPCRs are the most successful target class for approved drugs. Here we take the reader through a GPCR drug discovery journey from target to the clinic, highlighting the key learnings, best practices, challenges, trends and insights on discovering drugs that ultimately modulate GPCR function therapeutically in patients. The future of GPCR drug discovery is inspiring, with more desirable drug mechanisms and new technologies enabling the delivery of better and more successful drugs.

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现代GPCR药物发现的关键方面。

G蛋白偶联受体（GPCR）是最大、最通用的细胞表面受体家族，具有广泛的配体和功能。自1986年第一个GPCR被克隆和表达以来，我们已经了解到了大量关于发现这类受体药物的信息，因此现在人们已经认识到GPCR是批准药物中最成功的靶点类别。在这里，我们带读者经历了从靶点到临床的GPCR药物发现之旅，重点介绍了发现最终在患者中调节GPCR功能的药物的关键经验、最佳实践、挑战、趋势和见解。GPCR药物发现的未来令人鼓舞，有了更理想的药物机制和新技术，可以提供更好、更成功的药物。

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来源期刊

SLAS Discovery Chemistry-Analytical Chemistry

CiteScore

7.00

自引率

3.20%

发文量

审稿时长

39 days

期刊介绍： Advancing Life Sciences R&D: SLAS Discovery reports how scientists develop and utilize novel technologies and/or approaches to provide and characterize chemical and biological tools to understand and treat human disease. SLAS Discovery is a peer-reviewed journal that publishes scientific reports that enable and improve target validation, evaluate current drug discovery technologies, provide novel research tools, and incorporate research approaches that enhance depth of knowledge and drug discovery success. SLAS Discovery emphasizes scientific and technical advances in target identification/validation (including chemical probes, RNA silencing, gene editing technologies); biomarker discovery; assay development; virtual, medium- or high-throughput screening (biochemical and biological, biophysical, phenotypic, toxicological, ADME); lead generation/optimization; chemical biology; and informatics (data analysis, image analysis, statistics, bio- and chemo-informatics). Review articles on target biology, new paradigms in drug discovery and advances in drug discovery technologies. SLAS Discovery is of particular interest to those involved in analytical chemistry, applied microbiology, automation, biochemistry, bioengineering, biomedical optics, biotechnology, bioinformatics, cell biology, DNA science and technology, genetics, information technology, medicinal chemistry, molecular biology, natural products chemistry, organic chemistry, pharmacology, spectroscopy, and toxicology. SLAS Discovery is a member of the Committee on Publication Ethics (COPE) and was published previously (1996-2016) as the Journal of Biomolecular Screening (JBS).