Modulation of TRP channel activity by hydroxylation and its therapeutic potential

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dc.contributor.authorNagarajan, Y.
dc.contributor.authorRychkov, G.
dc.contributor.authorPeet, D.
dc.date.issued2017
dc.description.abstractTwo transient receptor potential (TRP) channels-TRPA1 and TRPV3-are post-translationally hydroxylated, resulting in oxygen-dependent regulation of channel activity. The enzymes responsible are the HIF prolyl hydroxylases (PHDs) and the asparaginyl hydroxylase factor inhibiting HIF (FIH). The PHDs and FIH are well characterized for their hydroxylation of the hypoxic inducible transcription factors (HIFs), mediating their hypoxic regulation. Consequently, these hydroxylases are currently being targeted therapeutically to modulate HIF activity in anemia, inflammation, and ischemic disease. Modulating the HIFs by targeting these hydroxylases may result in both desirable and undesirable effects on TRP channel activity, depending on the physiological context. For the best outcomes, these hydroxylases could be therapeutically targeted in pathologies where activation of both the HIFs and the relevant TRP channels are predicted to independently achieve positive outcomes, such as wound healing and obesity.
dc.description.statementofresponsibilityYagnesh Nagarajan, Grigori Y. Rychkov and Daniel J. Peet
dc.identifier.citationPharmaceuticals, 2017; 10(2):35-35
dc.identifier.doi10.3390/ph10020035
dc.identifier.issn1424-8247
dc.identifier.issn1424-8247
dc.identifier.orcidRychkov, G. [0000-0002-2788-2977]
dc.identifier.orcidPeet, D. [0000-0002-6085-8936]
dc.identifier.urihttp://hdl.handle.net/2440/105843
dc.language.isoen
dc.publisherMultidisciplinary Digital Publishing Institute
dc.relation.granthttp://purl.org/au-research/grants/arc/DP150102860
dc.rights© 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
dc.source.urihttps://doi.org/10.3390/ph10020035
dc.subjectFIH
dc.subjectHIF
dc.subjectPHD
dc.subjectTRPA1
dc.subjectTRPV3
dc.subjecthydroxylation
dc.subjecthypoxia
dc.subjectoxygen
dc.titleModulation of TRP channel activity by hydroxylation and its therapeutic potential
dc.typeJournal article
pubs.publication-statusPublished

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