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Two-pore channel blockade by phosphoinositide kinase inhibitors YM201636 and PI-103 determined by a histidine residue near pore-entrance
Human two-pore channels (TPCs) are endolysosomal cation channels and play an important role in NAADP-evoked Ca(2+) release and endomembrane dynamics. We found that YM201636, a PIKfyve inhibitor, potently inhibits PI(3,5)P(2)-activated human TPC2 with an IC(50) of 0.16 μM. YM201636 also effectively i...
| Autores principales: | , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
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Nature Publishing Group UK
2022
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9308409/ https://www.ncbi.nlm.nih.gov/pubmed/35871252 http://dx.doi.org/10.1038/s42003-022-03701-5 |