Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators

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dc.contributor.authorLeGay, Christina M
dc.contributor.authorGorobets, Evgueni
dc.contributor.authorIftinca, Mircea
dc.contributor.authorRamachandran, Rithwik
dc.contributor.authorAltier, Christophe
dc.contributor.authorDerksen, Darren J
dc.date.accessioned2021-09-01T22:42:06Z
dc.date.available2021-09-01T22:42:06Z
dc.date.issued2016-01
dc.description.abstractA library of novel structural hybrids of menthol and cubebol was tested for each derivative's ability to interact with the transient receptor potential subfamily melastatin member 8 (TRPM8) channel. This structure-activity relationship study revealed three potent modulators of the TRPM8 ion channel: a novel agonist (4) with an EC50 value of 11 ± 1 μM, an antagonist (15) with an IC50 value of 2 ± 1 μM, and an allosteric modulator (21) that minimized channel desensitization toward menthol. Each of these novel exocyclic olefin analogues of menthol is readily accessible by synthesis and was tested using Ca(2+) assays and electrophysiology.en_US
dc.identifier.citationLeGay, C. M., Gorobets, E., Iftinca, M., Ramachandran, R., Altier, C., & Derksen, D. J. (2016). Natural-product-derived transient receptor potential melastatin 8 (TRPM8) channel modulators. Organic letters, 18(11), 2746-2749.en_US
dc.identifier.doihttp://dx.doi.org/10.1021/acs.orglett.6b01222en_US
dc.identifier.urihttp://hdl.handle.net/1880/113802
dc.identifier.urihttps://doi.org/10.11575/PRISM/46119
dc.language.isoengen_US
dc.publisher.departmentChemistryen_US
dc.publisher.facultyCumming School of Medicineen_US
dc.publisher.facultyScienceen_US
dc.publisher.hasversionacceptedVersionen_US
dc.publisher.institutionUniversity of Calgaryen_US
dc.rightsUnless otherwise indicated, this material is protected by copyright and has been made available with authorization from the copyright owner. You may use this material in any way that is permitted by the Copyright Act or through licensing that has been assigned to the document. For uses that are not allowable under copyright legislation or licensing, you are required to seek permission.en_US
dc.subjectCalciumen_US
dc.subjectAlcoholsen_US
dc.subjectReaction productsen_US
dc.subjectModulatorsen_US
dc.subjectPharmaceuticalsen_US
dc.titleNatural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulatorsen_US
dc.typejournal articleen_US
ucalgary.item.requestcopytrueen_US
ucalgary.scholar.levelFacultyen_US
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