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Optical control of L-type Ca2+ channels using a diltiazem photoswitch.
Fehrentz, Timm; Huber, Florian M E; Hartrampf, Nina; Bruegmann, Tobias; Frank, James A; Fine, Nicholas H F; Malan, Daniela; Danzl, Johann G; Tikhonov, Denis B; Sumser, Martin; Sasse, Philipp; Hodson, David J; Zhorov, Boris S; Klöcker, Nikolaj; Trauner, Dirk.
Afiliação
  • Fehrentz T; Institute of Neural and Sensory Physiology, Medical Faculty, University of Düsseldorf, Düsseldorf, Germany. timm.fehrentz@gmail.com.
  • Huber FME; Department of Chemistry, University of Munich and Center for Integrated Protein Science (CIPSM), Munich, Germany.
  • Hartrampf N; Roche Diagnostics GmbH, DXRERA, Penzberg, Germany.
  • Bruegmann T; Department of Chemistry, University of Munich and Center for Integrated Protein Science (CIPSM), Munich, Germany.
  • Frank JA; Institute of Physiology I, Medical Faculty, University of Bonn, Bonn, Germany.
  • Fine NHF; Research Training Group 1873, University of Bonn, Bonn, Germany.
  • Malan D; Department of Chemistry, University of Munich and Center for Integrated Protein Science (CIPSM), Munich, Germany.
  • Danzl JG; Research Laboratory of Electronics, Massachusetts Institute of Technology, Cambridge, MA, USA.
  • Tikhonov DB; Institute of Metabolism and Systems Research (IMSR) and Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham, Birmingham, UK.
  • Sumser M; Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, UK.
  • Sasse P; Institute of Physiology I, Medical Faculty, University of Bonn, Bonn, Germany.
  • Hodson DJ; Department of NanoBiophotonics, Max Planck Institute for Biophysical Chemistry, Göttingen, Germany.
  • Zhorov BS; Institute of Science and Technology Austria, Klosterneuburg, Austria.
  • Klöcker N; Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia.
  • Trauner D; Department of Chemistry, University of Munich and Center for Integrated Protein Science (CIPSM), Munich, Germany.
Nat Chem Biol ; 14(8): 764-767, 2018 08.
Article em En | MEDLINE | ID: mdl-30013061
L-type Ca2+ channels (LTCCs) play a crucial role in excitation-contraction coupling and release of hormones from secretory cells. They are targets of antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a photoswitchable diltiazem, FHU-779, which can be used to reversibly block endogenous LTCCs by light. FHU-779 is as potent as diltiazem and can be used to place pancreatic ß-cell function and cardiac activity under optical control.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Diltiazem / Canais de Cálcio Tipo L / Células Secretoras de Insulina / Imagem Óptica / Corantes Fluorescentes / Coração Limite: Humans Idioma: En Revista: Nat Chem Biol Assunto da revista: BIOLOGIA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Alemanha
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Diltiazem / Canais de Cálcio Tipo L / Células Secretoras de Insulina / Imagem Óptica / Corantes Fluorescentes / Coração Limite: Humans Idioma: En Revista: Nat Chem Biol Assunto da revista: BIOLOGIA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Alemanha