新型拮抗剂揭示了 PXR 的抑制机制。

IF 13.9 1区医学 Q1 PHARMACOLOGY & PHARMACY

Trends in pharmacological sciences Pub Date : 2024-11-01 Epub Date: 2024-10-16 DOI:10.1016/j.tips.2024.10.002

Rajamanikkam Kamaraj, Petr Pavek

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引用次数: 0

摘要

孕烷 X 受体（PXR）是新陈代谢的关键调节因子，但其拮抗作用的机制仍不清楚。Garcia-Maldonado 等人报告了新的强效拮抗剂及其共晶体结构，揭示了 PXR 拮抗作用的分子决定因素，为开发拮抗剂作为治疗药物和防止不良 PXR 激活铺平了道路。

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Novel antagonists reveal the mechanism of PXR inhibition.

The pregnane X receptor (PXR) is a key regulator of metabolism, but the mechanisms underlying its antagonism remain unclear. Garcia-Maldonado et al. reported potent new antagonists and their co-crystal structures, revealing molecular determinants of PXR antagonism and paving the way for developing antagonists as therapeutics and preventing undesirable PXR activation.

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来源期刊

Trends in pharmacological sciences 医学-药学

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.