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.

中文翻译：

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pH 对阿片受体激活的影响及其对药物设计的影响


G 蛋白偶联受体是完整的膜蛋白，可将化学信号从细胞外基质转导至细胞内。传统的药物设计仅考虑正常条件下的配体-受体相互作用。然而，对阿片类药物的研究表明，这种相互作用在患病组织中非常不同。在这样的微环境中，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这些方面，以减少不良副作用，同时保留新化合物的预期效果。