2023
Human TRPV1 structure and inhibition by the analgesic SB-366791
Neuberger A, Oda M, Nikolaev Y, Nadezhdin K, Gracheva E, Bagriantsev S, Sobolevsky A. Human TRPV1 structure and inhibition by the analgesic SB-366791. Nature Communications 2023, 14: 2451. PMID: 37117175, PMCID: PMC10147690, DOI: 10.1038/s41467-023-38162-9.Peer-Reviewed Original ResearchMeSH KeywordsAnalgesicsCryoelectron MicroscopyHumansPainTransient Receptor Potential ChannelsTRPV Cation ChannelsConceptsSB-366791Transient receptor potential (TRP) ion channelsPotential ion channelsPain pathwaysPain therapyPain treatmentPsychiatric disordersOpioid crisisTherapy targetTRPV1 inhibitorElectrophysiological recordingsHuman TRPV1TRP channelsTRPV1New drugsDisease conditionsVanilloid subfamilyIon channelsTreatmentInhibitorsOpioidsPainTherapyDiseaseCryo-electron microscopy structure
2021
Extracellular cap domain is an essential component of the TRPV1 gating mechanism
Nadezhdin KD, Neuberger A, Nikolaev YA, Murphy LA, Gracheva EO, Bagriantsev SN, Sobolevsky AI. Extracellular cap domain is an essential component of the TRPV1 gating mechanism. Nature Communications 2021, 12: 2154. PMID: 33846324, PMCID: PMC8041747, DOI: 10.1038/s41467-021-22507-3.Peer-Reviewed Original ResearchConceptsCap domainC-terminusIon conductance pathwaysNumerous physiological processesTransient receptor potential channelsTRP channel familyCryo-EMPhysiological processesChannel familyExtracellular entranceHuman diseasesGating mechanismΒ-sheetConductance pathwayCritical determinantMolecular sensorsOpen probabilityPotential channelsIon selectivityEssential componentTRPV1 functionDomainTerminusProteinDeletion