PIEZO1 是一种真核膜蛋白，可组装为三聚体，形成钙渗透性、非选择性阳离子通道，具有精湛的机械力感应能力，并将力传导到多种细胞类型中，包括血细胞、内皮细胞、上皮细胞、成纤维细胞干细胞和不同的系统，包括骨骼、淋巴管和肌肉。该通道具有广泛的作用，被认为是癌症和心血管、牙科、胃肠道、肝胆、感染、肌肉骨骼、神经系统、眼部、妊娠、肾脏、呼吸和泌尿系统疾病等疾病的新疗法的靶点。 PIEZO1 调节剂的识别还处于起步阶段，但已经出现了一些有用的实验工具来激活通道，并在较小程度上抑制通道。 Yoda 系列小分子激动剂的基本结构-活性关系众所周知，显示出多种物理化学和药理学特性的潜力。 Yoda1 的有趣作用包括刺激去除多余的脑脊液。尽管 PIEZO1 表达广泛，但仍建议进行选择性正向或负向调节，而不会产生无法忍受的副作用。在这里，我们对该药理学的进展进行了有针对性的、非系统的、叙述性的回顾，并讨论了该领域未来潜在的研究方向。© 2024 作者。约翰·威利出版的《英国药理学杂志》

PIEZO1 is a eukaryotic membrane protein that assembles as trimers to form calcium-permeable, non-selective cation channels with exquisite capabilities for mechanical force sensing and transduction of force into effect in diverse cell types that include blood cells, endothelial cells, epithelial cells, fibroblasts and stem cells and diverse systems that include bone, lymphatics and muscle. The channel has wide-ranging roles and is considered as a target for novel therapeutics in ailments spanning cancers and cardiovascular, dental, gastrointestinal, hepatobiliary, infectious, musculoskeletal, nervous system, ocular, pregnancy, renal, respiratory and urological disorders. The identification of PIEZO1 modulators is in its infancy but useful experimental tools emerged for activating, and to a lesser extent inhibiting, the channels. Elementary structure-activity relationships are known for the Yoda series of small molecule agonists, which show the potential for diverse physicochemical and pharmacological properties. Intriguing effects of Yoda1 include the stimulated removal of excess cerebrospinal fluid. Despite PIEZO1's broad expression, opportunities are suggested for selective positive or negative modulation without intolerable adverse effects. Here we provide a focused, non-systematic, narrative review of progress with this pharmacology and discuss potential future directions for research in the area.© 2024 The Author(s). British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.