Chemical chaperone-conjugated exendin-4 as a cytoprotective agent for pancreatic β-cells
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Son, S. | - |
dc.contributor.author | Park, E.J. | - |
dc.contributor.author | Kim, Y. | - |
dc.contributor.author | Lee, K.C. | - |
dc.contributor.author | Na, D.H. | - |
dc.date.available | 2019-03-08T06:58:20Z | - |
dc.date.issued | 2018-12 | - |
dc.identifier.issn | 1357-2725 | - |
dc.identifier.issn | 1878-5875 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/3451 | - |
dc.description.abstract | Endoplasmic reticulum stress has been considered a major cause of pancreatic β-cell dysfunction and apoptosis leading to diabetes. Glucagon-like peptide-1 receptor activation and chemical chaperones have been known to reduce endoplasmic reticulum stress and improve β-cell function and survival. The purpose of this study was to prepare and evaluate the chemical chaperone tauroursodeoxycholic acid-conjugated exendin-4 as a protective agent for pancreatic β-cells. Mono-tauroursodeoxycholic acid-Lys27-exendin-4 conjugate (TUM1-Ex4) showed better receptor binding affinity than other conjugates with strong in vitro insulinotropic activity in rat pancreatic β-cells and in vivo hypoglycemic activity in type 2 diabetic db/db mice. In INS-1 cells under endoplasmic reticulum stress induced by thapsigargin, TUM1-Ex4 promoted cell survival in a dose-dependent manner. In western blot analysis, TUM1-Ex4 reduced the expression of the endoplasmic reticulum stress marker GRP78 and phosphorylation of the translation initiation factor eIF2α. These results reveal that TUM1-Ex4 accelerates translational recovery and contributes to β-cell protection and survival. The present study indicates that the chemical chaperone-coupled glucagon-like peptide-1 receptor agonist is a feasible therapeutic strategy to enhance β-cell function and survival. © 2018 Elsevier Ltd | - |
dc.format.extent | 7 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | Elsevier Ltd | - |
dc.title | Chemical chaperone-conjugated exendin-4 as a cytoprotective agent for pancreatic β-cells | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.biocel.2018.09.018 | - |
dc.identifier.bibliographicCitation | International Journal of Biochemistry and Cell Biology, v.105, pp 13 - 19 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000453642700002 | - |
dc.identifier.scopusid | 2-s2.0-85054172599 | - |
dc.citation.endPage | 19 | - |
dc.citation.startPage | 13 | - |
dc.citation.title | International Journal of Biochemistry and Cell Biology | - |
dc.citation.volume | 105 | - |
dc.type.docType | Article | - |
dc.publisher.location | 영국 | - |
dc.subject.keywordAuthor | Chemical chaperone | - |
dc.subject.keywordAuthor | Diabetes | - |
dc.subject.keywordAuthor | Exendin-4 | - |
dc.subject.keywordAuthor | Endoplasmic reticulum stress | - |
dc.subject.keywordAuthor | Tauroursodeoxycholic acid | - |
dc.subject.keywordPlus | ENDOPLASMIC-RETICULUM STRESS | - |
dc.subject.keywordPlus | REDUCE ER STRESS | - |
dc.subject.keywordPlus | GLP-1 RECEPTOR | - |
dc.subject.keywordPlus | MOUSE MODEL | - |
dc.subject.keywordPlus | STABILITY | - |
dc.subject.keywordPlus | MASS | - |
dc.subject.keywordPlus | PEGYLATION | - |
dc.subject.keywordPlus | EXENATIDE | - |
dc.subject.keywordPlus | SURVIVAL | - |
dc.subject.keywordPlus | THERAPY | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Cell Biology | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Cell Biology | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
84, Heukseok-ro, Dongjak-gu, Seoul, Republic of Korea (06974)02-820-6194
COPYRIGHT 2019 Chung-Ang University All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.