Structural requirements of steroidal agonists of transient receptor potential melastatin 3 (TRPM3) cation channels
British Journal of Pharmacology2013Vol. 171(4), pp. 1019–1032
Citations Over TimeTop 17% of 2013 papers
Anna Drews, Florian Mohr, Oleksandr Rizun, Thomas F.J. Wagner, Sandeep Dembla, Stephan Rudolph, Sachar Lambert, Maik Konrad, Stephan Philipp, Marc Behrendt, Sandrine Marchais‐Oberwinkler, Douglas F. Covey, Johannes Oberwinkler
Abstract
Our data demonstrate that nifedipine and pregnenolone sulphate act at different binding sites when activating TRPM3. The latter activates TRPM3 by binding to a chiral and thus proteinaceous binding site, as inferred from the differential effects of the enantiomers. The double bond between position C5 and C6 of pregnenolone sulphate is not strictly necessary for the activation of TRPM3 channels, but a negative charge at position C3 of the steroid is highly important. These results provide a solid basis for understanding mechanistically the rapid chemical activation of TRPM3 channels.
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