IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F967/2025.4
Piezo channels in GtoPdb v.2025.4
David J. Beech1
- University of Leeds, UK
Abstract
PIEZO proteins are the pore-forming subunits of trimeric ion channels that open rapidly in response to mechanical stimuli such as membrane stretch, allowing positively charged ions such as the calcium ion to flow into the cell to change cellular structure and function. The proteins are eukaryotic, not prokaryotic, and lack sequence or structural homology to other proteins. There are two main types: In humans, there is PIEZO1 of 2521 amino acids and PIEZO2 of 2752 amino acids, which can form homomeric PIEZO1 and PIEZO2 channels. Membrane stretching causes complex changes in the channels that include a reduced inward curvature, an expansion of the N-terminal transmembrane helical units and an opening of the central ion pore region comprising the last two C-terminal helices. When there is sustained membrane stretching, the channels may adapt by inactivating at various rates depending on the cell type and context. There are many roles of the channels in diverse organ systems including cardiovascular, gastrointestinal, haematological, hepatobiliary, immune, integumental, musculoskeletal, neuronal, reproductive, respiratory and urinary systems as well as adipose tissue and cancers. The expression and functions of PIEZO1 are broad and diverse across many cell types and organs, whereas PIEZO2 is more restricted.
Contents
This is a citation summary for Piezo channels in the
Guide to Pharmacology
database (GtoPdb). It exists purely as an adjunct to the database to
facilitate the recognition of citations to and from the database by
citation analyzers. Readers will almost certainly want to visit the
relevant sections of the database which are given here under database
links.
GtoPdb is an expert-driven
guide to pharmacological targets and the substances that act on them.
GtoPdb is a reference work which is most usefully represented as an
on-line database. As in any publication this work should be
appropriately cited, and the papers it cites should also be
recognized. This document provides a citation for the relevant parts
of the database, and also provides a reference list for the research
cited by those parts. For further details see [3].
Please note that the database version for the citations given in
GtoPdb are to the most recent preceding version
in which the family or its subfamilies and targets were substantially
changed. The links below are to the current version. If you
need to consult the cited version, rather than the most recent version, please contact
the GtoPdb curators.
Database links
Piezo channels
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=967
Channels and Subunits
Piezo1
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2945
Piezo2
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2946
References
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