ArticleBritish journal of pharmacology2023
Improved PIEZO1 agonism through 4-benzoic acid modification of Yoda1.
Article in British journal of pharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 51 citations in OpenAlex.
- Article
- Piezo1 agonists are potent off-target inhibitors of the Kv1.3 channel via gating modification.Molecular pharmacology · 2026Article
- Protection againstMicrobiology spectrum · 2026Article
- Piezo1 channel: structure, mechanogating mechanism, functions, diseases and therapeutic strategy.Molecular biomedicine · 2026Review
- Orai1 is required for CabioRxiv : the preprint server for biology · 2026Article
- Yoda molecules agonize PIEZO2.bioRxiv : the preprint server for biology · 2026Article
- Piezo1 in the central nervous system: decoding the mechanical signature of neuroinflammation.Journal of neuroinflammation · 2026Review
- Lipid Regulation of Mechanosensitive Ion Channels.International journal of molecular sciences · 2026Review
- A functional and robust cellular model for high-throughput screening of piezo1 modulators.Scientific reports · 2026Article
- The mechano-immunological barrier in fibrosis-associated lung cancer: targeting matrix stiffness and the Piezo1 axis for microenvironment normalization.Frontiers in pharmacology · 2026Review
- Targeting Piezo1/2 ion channels for modulation of the lymphatic system: mechanisms, applications, and therapeutic prospects.Burns & trauma · 2026Review
- The role of Piezo1 in immune cells and pregnancy.Frontiers in immunology · 2026Review
- Mechanotransduction and cell fate: from molecular sensors to multicellular self-organization.Frontiers in cell and developmental biology · 2026Review
- 3D-MINFLUX nanoscopy reveals distinct allosteric mechanisms for activation and modulation of PIEZO1 by Yoda1.Nature communications · 2025Article
- Activation of the Piezo1 channel stimulates protein kinase D and migration in human aortic endothelial cells.American journal of physiology. Cell physiology · 2025Article
- Cluster nanoarchitecture and structural diversity of PIEZO1 at rest and during activation in intact cells.Science advances · 2025Article
- Advances in ligand-based surface engineering strategies for fine-tuning T cell mechanotransduction toward efficient immunotherapy.Biophysical journal · 2025Review
- PIEZO1 mechanical insensitivity in generalized lymphatic dysplasia with the potential for pharmacological rescue.iScience · 2025Article
- Combined Effects of Mechanical Loading and Piezo1 Chemical Activation on 22-Months-Old Female Mouse Bone Adaptation.Aging cell · 2025Article
- Review
Corrections and comments
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Authors and funding
19 authors at 2 institutions in 2 countries.
Funding
Abstract
background and purposeThe protein PIEZO1 forms mechanically activated, calcium-permeable, non-selective cation channels in numerous cell types from several species. Options for pharmacological modulation are limited and so we modified a small-molecule agonist at PIEZO1 channels (Yoda1) to increase the ability to modulate these channels. EXPERIMENTAL APPROACH: Medicinal chemistry generated Yoda1 analogues that were tested in intracellular calcium and patch-clamp assays on cultured cells exogenously expressing human or mouse PIEZO1 or mouse PIEZO2. Physicochemical assays and wire myography assays on veins from mice with genetic disruption of PIEZO1. KEY
resultsA Yoda1 analogue (KC159) containing 4-benzoic acid instead of the pyrazine of Yoda1 and its potassium salt (KC289) have equivalent or improved reliability, efficacy and potency, compared with Yoda1 in functional assays. Tested against overexpressed mouse PIEZO1 in calcium assays, the order of potency (as EC CONCLUSION AND IMPLICATIONS: 4-Benzoic acid modification of Yoda1 improves PIEZO1 agonist activity at PIEZO1 channels. We suggest naming this new modulator Yoda2. It should be a useful tool compound in physiological assays and facilitate efforts to identify a binding site. Such compounds may have therapeutic potential, for example, in diseases linked genetically to PIEZO1 such as lymphatic dysplasia.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.