Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists
Piezo1, a non-selective cation channel, can transduce diverse mechanical stimuli into electrochemical signals and perform essential physiological functions in the human body. Anomalous Piezo1 activities due to loss-of-function mutations are linked to diverse pathological states ranging from anemia,...
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| Format: | Article |
| Language: | English |
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Elsevier
2025-03-01
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| Series: | Results in Chemistry |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715625000414 |
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| author | Danjiang Li Yuanyuan Song Yuan Zeng Hua Hu Wei Tian |
| author_facet | Danjiang Li Yuanyuan Song Yuan Zeng Hua Hu Wei Tian |
| author_sort | Danjiang Li |
| collection | DOAJ |
| description | Piezo1, a non-selective cation channel, can transduce diverse mechanical stimuli into electrochemical signals and perform essential physiological functions in the human body. Anomalous Piezo1 activities due to loss-of-function mutations are linked to diverse pathological states ranging from anemia, malaria immunity, lymphatic abnormalities, and varicose veins. Thus, targeting and modulating Piezo1 have demonstrated the potential to yield significant therapeutic benefits, thereby affirming Piezo1 as a promising drug target for various diseases. Recent studies have unveiled crystal structures of Piezo1 and identified small-molecule agonists that shed light on the channel’s structure and activation mechanism. This review consolidates our understanding of Piezo1, focusing on its structural features, mechanosensitive activation and potential agonists to guide future investigations in this field. |
| format | Article |
| id | doaj-art-ec1b2137093d49619ed40dbfa336636d |
| institution | OA Journals |
| issn | 2211-7156 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Results in Chemistry |
| spelling | doaj-art-ec1b2137093d49619ed40dbfa336636d2025-08-20T01:58:28ZengElsevierResults in Chemistry2211-71562025-03-011410205810.1016/j.rechem.2025.102058Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonistsDanjiang Li0Yuanyuan Song1Yuan Zeng2Hua Hu3Wei Tian4Central Theater General Hospital, Wuhan 430070 ChinaCentral Theater General Hospital, Wuhan 430070 ChinaCentral Theater General Hospital, Wuhan 430070 ChinaCorresponding authors.; Central Theater General Hospital, Wuhan 430070 ChinaCorresponding authors.; Central Theater General Hospital, Wuhan 430070 ChinaPiezo1, a non-selective cation channel, can transduce diverse mechanical stimuli into electrochemical signals and perform essential physiological functions in the human body. Anomalous Piezo1 activities due to loss-of-function mutations are linked to diverse pathological states ranging from anemia, malaria immunity, lymphatic abnormalities, and varicose veins. Thus, targeting and modulating Piezo1 have demonstrated the potential to yield significant therapeutic benefits, thereby affirming Piezo1 as a promising drug target for various diseases. Recent studies have unveiled crystal structures of Piezo1 and identified small-molecule agonists that shed light on the channel’s structure and activation mechanism. This review consolidates our understanding of Piezo1, focusing on its structural features, mechanosensitive activation and potential agonists to guide future investigations in this field.http://www.sciencedirect.com/science/article/pii/S2211715625000414ProgressPiezo1StructureMechanismAgonist |
| spellingShingle | Danjiang Li Yuanyuan Song Yuan Zeng Hua Hu Wei Tian Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists Results in Chemistry Progress Piezo1 Structure Mechanism Agonist |
| title | Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists |
| title_full | Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists |
| title_fullStr | Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists |
| title_full_unstemmed | Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists |
| title_short | Research progress on PIEZO1 protein structure and activation mechanism by small-molecule agonists |
| title_sort | research progress on piezo1 protein structure and activation mechanism by small molecule agonists |
| topic | Progress Piezo1 Structure Mechanism Agonist |
| url | http://www.sciencedirect.com/science/article/pii/S2211715625000414 |
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