Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor
Micael Rodrigues Cunha, Rajesh Bhardwaj, Aline Lucie Carrel, Sonja Lindinger, Christoph Romanin, Roberto Parise‐Filho, Matthias A. Hediger, Jean‐Louis Reymond
Abstract
= 0.082 ± 0.004 μM) and ion channel selectivity, but with high microsomal stability and very low off-target effects. This natural product-inspired inhibitor does not exhibit any non-specific toxicity effects on various cell lines and is proposed as a new tool compound to test pharmacological inhibition of TRPV6 mediated calcium flux in disease models.
Topics & Concepts
TRPV6Calcium channelChemistryCalciumNatural productPharmacologyMicrosomeTransient receptor potential channelVoltage-dependent calcium channelBiochemistryBiophysicsIn vitroReceptorBiologyOrganic chemistryBioactive Compounds and Antitumor AgentsMorinda citrifolia extract usesPhytochemicals and Antioxidant Activities