Lydie Burglen, Evelien Van Hoeymissen ... Joris Vriens
Newly identified gain-of-function variants indicate TRPM3 as the cause of a spectrum of autosomal dominant neurodevelopmental disorders with frequent cerebellar involvement in humans.
Katherine E Huffer, Antoniya A Aleksandrova ... Kenton J Swartz
Structure-based alignment of TRP channels enables comparison of structural changes, ion permeation pathways and ligand-binding sites and reveals over-representation of structures that represent non-conducting states.
The 3Å structure and correlated functional analysis of the TRPM2 cation channel from Nematostella vectensis shed light on the molecular mechanisms of TRPM2 regulation by intra- and extracellular Ca2+, and of inactivation of human TRPM2.
Deny Cabezas-Bratesco, Francisco A Mcgee ... Sebastian E Brauchi
Joint sequence, structure, and phylogenetic analyses identify highly conserved features in transmembrane domains of transient receptor potential (TRP) ion channel proteins that offer a novel explanation for how TRPs could integrate stimuli into cellular signals.
Astrid Kollewe, Vladimir Chubanov ... Thomas Gudermann
High-resolution proteomics in conjunction with biochemical and electrophysiological experiments revealed that the channel-kinase TRPM7 in rodent brain forms macromolecular complexes containing the metal transporters CNNM1-4 and a small G-protein ARL15.
High-resolution structures of human TRPM2 in different functional states provided the mechanism underlying ligand recognition, channel activation and inhibition.
Taylor ET Hughes, John Smith Del Rosario ... Vera Y Moiseenkova-Bell
Structure-based virtual screening reveals multiple novel TRPV5 inhibitors that bind and exert their effect from previously unidentified binding sites as characterized by cryo-electron microscopy and electrophysiology.
Disease-associated mutants of the TRPM3 ion channel are overactive, and they are inhibited by the antiepileptic medication primidone, offering a potential therapeutic intervention to treat this channelopathy.
Sandeep Dembla, Marc Behrendt ... Johannes Oberwinkler
Pro-nociceptive and pro-inflammatory TRPM3 (transient receptor potential melastatin 3) channels, expressed in somatosensory neurons, are inhibited by activation of Gαi-coupled receptors, such as µ-opioid receptors, in vitro and in vivo.