Effects of pH on opioid receptor activation and implications for drug design.

IF 3.2 3区 生物学 Q2 BIOPHYSICS Biophysical journal Pub Date : 2024-12-17 Epub Date: 2024-07-05 DOI:10.1016/j.bpj.2024.07.007
Christoph Stein
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引用次数: 0

Abstract

G-protein-coupled receptors are integral membrane proteins that transduce chemical signals from the extracellular matrix into the cell. Traditional drug design has considered ligand-receptor interactions only under normal conditions. However, studies on opioids indicate that such interactions are very different in diseased tissues. In such microenvironments, protons play an important role in structural and functional alterations of both ligands and receptors. The pertinent literature strongly suggests that future drug design should take these aspects into account in order to reduce adverse side effects while preserving desired effects of novel compounds.

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pH 值对阿片受体活化的影响及其对药物设计的意义。
G 蛋白偶联受体(GPCR)是一种完整的膜蛋白,可将化学信号从细胞外基质传递到细胞内。传统的药物设计只考虑正常情况下配体与受体之间的相互作用。然而,对阿片类药物的研究表明,这种相互作用在病变组织中截然不同。在这种微环境中,质子在配体和受体的结构和功能改变中发挥着重要作用。相关文献强烈建议,未来的药物设计应考虑到这些方面,以减少不良副作用,同时保留新型化合物的预期效果。
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来源期刊
Biophysical journal
Biophysical journal 生物-生物物理
CiteScore
6.10
自引率
5.90%
发文量
3090
审稿时长
2 months
期刊介绍: BJ publishes original articles, letters, and perspectives on important problems in modern biophysics. The papers should be written so as to be of interest to a broad community of biophysicists. BJ welcomes experimental studies that employ quantitative physical approaches for the study of biological systems, including or spanning scales from molecule to whole organism. Experimental studies of a purely descriptive or phenomenological nature, with no theoretical or mechanistic underpinning, are not appropriate for publication in BJ. Theoretical studies should offer new insights into the understanding ofexperimental results or suggest new experimentally testable hypotheses. Articles reporting significant methodological or technological advances, which have potential to open new areas of biophysical investigation, are also suitable for publication in BJ. Papers describing improvements in accuracy or speed of existing methods or extra detail within methods described previously are not suitable for BJ.
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