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dc.contributor.authorGingell, Joseph J
dc.contributor.authorRees, Tayla A
dc.contributor.authorHendrikse, Erica R
dc.contributor.authorSiow, Andrew
dc.contributor.authorRennison, David
dc.contributor.authorScotter, John
dc.contributor.authorHarris, Paul W R
dc.contributor.authorBrimble, Margaret A
dc.contributor.authorWalker, Christopher S
dc.contributor.authorHay, Debbie L
dc.date.available2021-04-12T01:22:12Z
dc.date.copyright2020
dc.identifier.urihttp://hdl.handle.net/10523/10879
dc.description.abstractCalcitonin gene-related peptide (CGRP) is a neuropeptide that is involved in the transmission of pain. Drugs targeting CGRP or a CGRP receptor are efficacious in the treatment of migraine. The canonical CGRP receptor is a complex of a G protein-coupled receptor, the calcitonin-like receptor (CLR), with an accessory protein, receptor activity-modifying protein 1 (RAMP1). A second receptor, the AMY1 receptor, a complex of the calcitonin receptor with RAMP1, is a dual high-affinity receptor for CGRP and amylin. Receptor regulatory processes, such as internalization, are crucial for controlling peptide and drug responsiveness. Given the importance of CGRP receptor activity in migraine we compared the internalization profiles of both receptors for CGRP using novel fluorescent probes and a combination of live cell imaging, fixed cell imaging, and ELISA. This revealed stark differences in the regulation of each receptor with the AMY1 receptor unexpectedly showing little internalization.en_NZ
dc.language.isoenen_NZ
dc.publisherACS Publicationsen_NZ
dc.relation.ispartofACS Pharmacology & Translational Scienceen_NZ
dc.subjectamylinen_NZ
dc.subjectCGRPen_NZ
dc.subjectGPCRen_NZ
dc.subjectinternalizationen_NZ
dc.subjectmigraineen_NZ
dc.subjectreceptor activity-modifying proteinen_NZ
dc.titleDistinct Patterns of Internalization of Different Calcitonin GeneRelated Peptide Receptorsen_NZ
dc.typeJournal Articleen_NZ
dc.date.updated2021-04-12T00:33:46Z
otago.schoolPharmacology and Toxicologyen_NZ
otago.relation.issue2en_NZ
otago.relation.volume3en_NZ
dc.identifier.doihttps://doi.org/10.1021/acsptsci.9b00089en_NZ
otago.bitstream.endpage304en_NZ
otago.bitstream.startpage296en_NZ
otago.openaccessOpenen_NZ
dc.rights.statementThis document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Pharmacology & Translational Science, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acsptsci.9b00089en_NZ
dc.description.refereedPeer Revieweden_NZ
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