Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na+ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases

  title={Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na+ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases},
  author={Quentin Coquerel and Claire Legendre and Jacinthe Frangieh and Stephan De Waard and J{\'e}r{\^o}me Montnach and Leos Cmarko and Joseph Khoury and Charifat Said Hassane and Dimitri Br{\'e}ard and Benjamin Siegler and Ziad Fajloun and Harold de Pomyers and Kamel Mabrouk and Norbert Weiss and Daniel Henrion and Pascal Richomme and C{\'e}sar Mattei and Michel de Waard and A-M Le Ray and Christian Legros},
Voltage-gated Na+ (NaV) channels are significant therapeutic targets for the treatment of cardiac and neurological disorders, thus promoting the search for novel NaV channel ligands. With the objective of discovering new blockers of NaV channel ligands, we screened an In-House vegetal alkaloid library using fluorescence cell-based assays. We screened 62 isoquinoline alkaloids (IA) for their ability to decrease the FRET signal of voltage sensor probes (VSP), which were induced by the activation… 



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