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Chemical activation of the mechanotransduction channel Piezo1.
Syeda, Ruhma; Xu, Jie; Dubin, Adrienne E; Coste, Bertrand; Mathur, Jayanti; Huynh, Truc; Matzen, Jason; Lao, Jianmin; Tully, David C; Engels, Ingo H; Petrassi, H Michael; Schumacher, Andrew M; Montal, Mauricio; Bandell, Michael; Patapoutian, Ardem.
Afiliación
  • Syeda R; Department of Molecular and Cellular Neuroscience, Howard Hughes Medical Institute, The Scripps Research Institute, La Jolla, United States.
  • Xu J; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Dubin AE; Department of Molecular and Cellular Neuroscience, Howard Hughes Medical Institute, The Scripps Research Institute, La Jolla, United States.
  • Coste B; Department of Molecular and Cellular Neuroscience, Howard Hughes Medical Institute, The Scripps Research Institute, La Jolla, United States.
  • Mathur J; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Huynh T; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Matzen J; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Lao J; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Tully DC; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Engels IH; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Petrassi HM; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Schumacher AM; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Montal M; University of California, San Diego, La Jolla, United States.
  • Bandell M; Genomics Institute of the Novartis Research Foundation, San Diego, United States.
  • Patapoutian A; Department of Molecular and Cellular Neuroscience, Howard Hughes Medical Institute, The Scripps Research Institute, La Jolla, United States.
Elife ; 42015 May 22.
Article en En | MEDLINE | ID: mdl-26001275
Piezo ion channels are activated by various types of mechanical stimuli and function as biological pressure sensors in both vertebrates and invertebrates. To date, mechanical stimuli are the only means to activate Piezo ion channels and whether other modes of activation exist is not known. In this study, we screened ~3.25 million compounds using a cell-based fluorescence assay and identified a synthetic small molecule we termed Yoda1 that acts as an agonist for both human and mouse Piezo1. Functional studies in cells revealed that Yoda1 affects the sensitivity and the inactivation kinetics of mechanically induced responses. Characterization of Yoda1 in artificial droplet lipid bilayers showed that Yoda1 activates purified Piezo1 channels in the absence of other cellular components. Our studies demonstrate that Piezo1 is amenable to chemical activation and raise the possibility that endogenous Piezo1 agonists might exist. Yoda1 will serve as a key tool compound to study Piezo1 regulation and function.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Mecanotransducción Celular / Bibliotecas de Moléculas Pequeñas / Canales Iónicos Límite: Animals / Humans Idioma: En Revista: Elife Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Mecanotransducción Celular / Bibliotecas de Moléculas Pequeñas / Canales Iónicos Límite: Animals / Humans Idioma: En Revista: Elife Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido