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HCN Channels: New therapeutic targets for pain treatment

dc.contributor.authorRamírez D.
dc.contributor.authorZúñiga R.
dc.contributor.authorConcha G.
dc.contributor.authorZúñiga L.
dc.date.accessioned2020-09-02T22:26:32Z
dc.date.available2020-09-02T22:26:32Z
dc.date.issued2018
dc.identifier10.3390/molecules23092094
dc.identifier.citation23, 9, -
dc.identifier.issn14203049
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5952
dc.descriptionHyperpolarization-activated cyclic nucleotide-gated (HCN) channels are highly regulated proteins which respond to different cellular stimuli. The HCN currents (Ih) mediated by HCN1 and HCN2 drive the repetitive firing in nociceptive neurons. The role of HCN channels in pain has been widely investigated as targets for the development of new therapeutic drugs, but the comprehensive design of HCN channel modulators has been restricted due to the lack of crystallographic data. The three-dimensional structure of the human HCN1 channel was recently reported, opening new possibilities for the rational design of highly-selective HCN modulators. In this review, we discuss the structural and functional properties of HCN channels, their pharmacological inhibitors, and the potential strategies for designing new drugs to block the HCN channel function associated with pain perception. © 2018 by the authors.
dc.language.isoen
dc.publisherMDPI AG
dc.subjectHCN blockers
dc.subjectHCN channels
dc.subjectHCN channels expression
dc.subjectHCN structure
dc.subjectPain condition
dc.subjecthyperpolarization activated cyclic nucleotide gated channel
dc.subjectanalgesia
dc.subjectanimal
dc.subjectantagonists and inhibitors
dc.subjectcentral nervous system
dc.subjectchemistry
dc.subjectdrug design
dc.subjectdrug development
dc.subjectgene expression regulation
dc.subjectgenetics
dc.subjecthuman
dc.subjectmetabolism
dc.subjectmolecularly targeted therapy
dc.subjectnociception
dc.subjectpain
dc.subjectsignal transduction
dc.subjectstructure activity relation
dc.subjectAnimals
dc.subjectCentral Nervous System
dc.subjectDrug Design
dc.subjectDrug Discovery
dc.subjectGene Expression Regulation
dc.subjectHumans
dc.subjectHyperpolarization-Activated Cyclic Nucleotide-Gated Channels
dc.subjectMolecular Targeted Therapy
dc.subjectPain
dc.subjectPain Management
dc.subjectPain Perception
dc.subjectSignal Transduction
dc.subjectStructure-Activity Relationship
dc.titleHCN Channels: New therapeutic targets for pain treatment
dc.typeReview


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