Advances in the structural understanding of opioid allostery.

IF 13.9 1区 医学 Q1 PHARMACOLOGY & PHARMACY
Trends in pharmacological sciences Pub Date : 2025-02-01 Epub Date: 2025-01-17 DOI:10.1016/j.tips.2024.12.007
Nokomis Ramos-Gonzalez, Balazs R Varga, Susruta Majumdar
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引用次数: 0

Abstract

Activation of the μ opioid receptor (MOR) can give analgesia, but also has dangerous side effects. Drugs that target MOR through an allosteric site, meaning they bind outside of the usual pocket, present a novel mode of receptor activation with different pharmacology relative to orthosteric drugs. Recent structural studies give valuable new information on how allosteric modulators interact with MOR.

阿片变构的结构研究进展。
激活μ阿片受体(MOR)可以起到镇痛作用,但也有危险的副作用。通过变构位点靶向MOR的药物,意味着它们在通常的口袋外结合,呈现出一种新的受体激活模式,与正畸药物相比具有不同的药理学。最近的结构研究为变构调节剂如何与MOR相互作用提供了有价值的新信息。
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来源期刊
CiteScore
23.90
自引率
0.70%
发文量
132
审稿时长
6-12 weeks
期刊介绍: Trends in Pharmacological Sciences (TIPS) is a monthly peer-reviewed reviews journal that focuses on a wide range of topics in pharmacology, pharmacy, pharmaceutics, and toxicology. Launched in 1979, TIPS publishes concise articles discussing the latest advancements in pharmacology and therapeutics research. The journal encourages submissions that align with its core themes while also being open to articles on the biopharma regulatory landscape, science policy and regulation, and bioethics. Each issue of TIPS provides a platform for experts to share their insights and perspectives on the most exciting developments in the field. Through rigorous peer review, the journal ensures the quality and reliability of published articles. Authors are invited to contribute articles that contribute to the understanding of pharmacology and its applications in various domains. Whether it's exploring innovative drug therapies or discussing the ethical considerations of pharmaceutical research, TIPS provides a valuable resource for researchers, practitioners, and policymakers in the pharmacological sciences.
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