Histidine(7.36(305)) in the conserved peptide receptor activation domain of the gonadotropin releasing hormone receptor couples peptide binding and receptor activation
DC Field | Value | Language |
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dc.contributor.author | Mayevu, Nkateko M. I. | - |
dc.contributor.author | Choe, Han | - |
dc.contributor.author | Abagyan, Ruben | - |
dc.contributor.author | Seong, Jae Young | - |
dc.contributor.author | Millar, Robert P. | - |
dc.contributor.author | Katz, Arieh A. | - |
dc.contributor.author | Flanagan, Colleen A. | - |
dc.date.accessioned | 2021-09-04T19:12:28Z | - |
dc.date.available | 2021-09-04T19:12:28Z | - |
dc.date.created | 2021-06-15 | - |
dc.date.issued | 2015-02-15 | - |
dc.identifier.issn | 0303-7207 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/94396 | - |
dc.description.abstract | Transmembrane helix seven residues of G protein-coupled receptors (GPCRs) couple agonist binding to a conserved receptor activation mechanism. Amino-terminal residues of the GnRH peptide determine agonist activity. We investigated GnRH interactions with the His(7.36(305)) residue of the GnRH receptor, using functional and computational analysis of modified GnRH receptors and peptides. Non-polar His(7.36(305)) substitutions decreased receptor affinity for GnRH four- to forty-fold, whereas GnRH signaling potency was more decreased (similar to 150-fold). Uncharged polar His(7.36(305)) substitutions decreased GnRH potency, but not affinity. [2-Nal(3)]-GnRH retained high affinity at receptors with non-polar His(7.36(305)) substitutions, supporting a role for His(7.36(305)) in recognizing Trp(3) of GnRH. Compared with GnRH, [2-Nal(3)]-GnRH potency was lower at the wild type GnRH receptor, but unchanged or higher at mutant receptors. Results suggest that His(7.36(305)) of the GnRH receptor forms two distinct interactions that determine binding to Trp(3) and couple agonist binding to the conserved transmembrane domain network that activates GPCRs. (C) 2015 Elsevier Ireland Ltd. All rights reserved. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | ELSEVIER IRELAND LTD | - |
dc.subject | DIFFERENTIAL LIGAND SELECTIVITY | - |
dc.subject | HUMAN P2Y(12) RECEPTOR | - |
dc.subject | GNRH RECEPTOR | - |
dc.subject | EXTRACELLULAR LOOP-3 | - |
dc.subject | NEUROTENSIN RECEPTOR | - |
dc.subject | CRITICAL DETERMINANT | - |
dc.subject | ANTAGONIST BINDING | - |
dc.subject | CRYSTAL-STRUCTURE | - |
dc.subject | PROSTATE-CANCER | - |
dc.subject | MAMMALIAN GNRH | - |
dc.title | Histidine(7.36(305)) in the conserved peptide receptor activation domain of the gonadotropin releasing hormone receptor couples peptide binding and receptor activation | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Seong, Jae Young | - |
dc.identifier.doi | 10.1016/j.mce.2015.01.008 | - |
dc.identifier.scopusid | 2-s2.0-84921451239 | - |
dc.identifier.wosid | 000350093800011 | - |
dc.identifier.bibliographicCitation | MOLECULAR AND CELLULAR ENDOCRINOLOGY, v.402, no.C, pp.95 - 106 | - |
dc.relation.isPartOf | MOLECULAR AND CELLULAR ENDOCRINOLOGY | - |
dc.citation.title | MOLECULAR AND CELLULAR ENDOCRINOLOGY | - |
dc.citation.volume | 402 | - |
dc.citation.number | C | - |
dc.citation.startPage | 95 | - |
dc.citation.endPage | 106 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Cell Biology | - |
dc.relation.journalResearchArea | Endocrinology & Metabolism | - |
dc.relation.journalWebOfScienceCategory | Cell Biology | - |
dc.relation.journalWebOfScienceCategory | Endocrinology & Metabolism | - |
dc.subject.keywordPlus | DIFFERENTIAL LIGAND SELECTIVITY | - |
dc.subject.keywordPlus | HUMAN P2Y(12) RECEPTOR | - |
dc.subject.keywordPlus | GNRH RECEPTOR | - |
dc.subject.keywordPlus | EXTRACELLULAR LOOP-3 | - |
dc.subject.keywordPlus | NEUROTENSIN RECEPTOR | - |
dc.subject.keywordPlus | CRITICAL DETERMINANT | - |
dc.subject.keywordPlus | ANTAGONIST BINDING | - |
dc.subject.keywordPlus | CRYSTAL-STRUCTURE | - |
dc.subject.keywordPlus | PROSTATE-CANCER | - |
dc.subject.keywordPlus | MAMMALIAN GNRH | - |
dc.subject.keywordAuthor | G protein-coupled receptor (GPCR) | - |
dc.subject.keywordAuthor | Peptide hormone | - |
dc.subject.keywordAuthor | Hormone receptor | - |
dc.subject.keywordAuthor | Receptor structure-function | - |
dc.subject.keywordAuthor | Peptide interaction | - |
dc.subject.keywordAuthor | GnRH | - |
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