DC Field | Value | Language |
---|---|---|
dc.contributor.author | Lee, Jung Gi | ko |
dc.contributor.author | Ryu, Jae Ha | ko |
dc.contributor.author | Kim, Seon-Myung | ko |
dc.contributor.author | Park, Moon-Young | ko |
dc.contributor.author | Kim, San-Ho | ko |
dc.contributor.author | Shin, Young G. | ko |
dc.contributor.author | Sohn, Jong Woo | ko |
dc.contributor.author | Kim, Ha Hyung | ko |
dc.contributor.author | Park, Zee-Yong | ko |
dc.contributor.author | Seong, Jae Young | ko |
dc.contributor.author | Kim, Jae Il | ko |
dc.date.accessioned | 2018-04-24T02:15:13Z | - |
dc.date.available | 2018-04-24T02:15:13Z | - |
dc.date.created | 2018-03-23 | - |
dc.date.created | 2018-03-23 | - |
dc.date.created | 2018-03-23 | - |
dc.date.issued | 2018-05 | - |
dc.identifier.citation | BIOCHEMICAL PHARMACOLOGY, v.151, pp.59 - 68 | - |
dc.identifier.issn | 0006-2952 | - |
dc.identifier.uri | http://hdl.handle.net/10203/241084 | - |
dc.description.abstract | Exendin-4, a 39 amino acid peptide isolated from the saliva of the Gila monster, plays an important role in regulating glucose homeostasis, and is used clinically for the treatment of type 2 diabetes. Exendin-4 shares 53% sequence identity with the incretin hormone glucagon-like peptide 1 (GLP-1) but, unlike GLP-1, is highly resistant to proteolytic enzymes such as dipeptidyl peptidase IV (DPP-IV) and neutral endopeptidase 24.11 (NEP 24.11). Herein, we focused on the structure and function of the C-terminal Trp-cage of exendin-4, and suggest that it may be structurally required for resistance to proteolysis by NEP 24.11. Using a series of substitutions and truncations of the C-terminal Trp-cage, we found that residues 1–33, including the N-terminal and helical regions of wild-type (WT) exendin-4, is the minimum motif required for both high peptidase resistance and potent activity toward the GLP-1 receptor comparable to WT exendin-4. To improve the therapeutic utility of C-terminally truncated exendin-4, we incorporated various fatty acids into exendin-4(1–33) in which Ser | - |
dc.language | English | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | GLUCAGON-LIKE PEPTIDE-1 | - |
dc.subject | TYPE-2 DIABETES-MELLITUS | - |
dc.subject | INCRETIN MIMETICS | - |
dc.subject | GLP-1 RECEPTOR | - |
dc.subject | EXTRACELLULAR DOMAIN | - |
dc.subject | CONJUGATED EXENDIN-4 | - |
dc.subject | EXTENDED-RELEASE | - |
dc.subject | IV INHIBITORS | - |
dc.subject | IN-VIVO | - |
dc.subject | ALBUMIN | - |
dc.title | Replacement of the C-terminal Trp-cage of exendin-4 with a fatty acid improves therapeutic utility | - |
dc.type | Article | - |
dc.identifier.wosid | 000431099400007 | - |
dc.identifier.scopusid | 2-s2.0-85043355234 | - |
dc.type.rims | ART | - |
dc.citation.volume | 151 | - |
dc.citation.beginningpage | 59 | - |
dc.citation.endingpage | 68 | - |
dc.citation.publicationname | BIOCHEMICAL PHARMACOLOGY | - |
dc.identifier.doi | 10.1016/j.bcp.2018.03.004 | - |
dc.contributor.localauthor | Sohn, Jong Woo | - |
dc.contributor.nonIdAuthor | Lee, Jung Gi | - |
dc.contributor.nonIdAuthor | Ryu, Jae Ha | - |
dc.contributor.nonIdAuthor | Kim, Seon-Myung | - |
dc.contributor.nonIdAuthor | Park, Moon-Young | - |
dc.contributor.nonIdAuthor | Kim, San-Ho | - |
dc.contributor.nonIdAuthor | Shin, Young G. | - |
dc.contributor.nonIdAuthor | Kim, Ha Hyung | - |
dc.contributor.nonIdAuthor | Park, Zee-Yong | - |
dc.contributor.nonIdAuthor | Seong, Jae Young | - |
dc.contributor.nonIdAuthor | Kim, Jae Il | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | Diabetes | - |
dc.subject.keywordAuthor | Exendin-4 | - |
dc.subject.keywordAuthor | Fatty acid | - |
dc.subject.keywordAuthor | GLP-1 receptor | - |
dc.subject.keywordAuthor | Neutral endopeptidase 24.11 | - |
dc.subject.keywordPlus | GLUCAGON-LIKE PEPTIDE-1 | - |
dc.subject.keywordPlus | TYPE-2 DIABETES-MELLITUS | - |
dc.subject.keywordPlus | INCRETIN MIMETICS | - |
dc.subject.keywordPlus | GLP-1 RECEPTOR | - |
dc.subject.keywordPlus | EXTRACELLULAR DOMAIN | - |
dc.subject.keywordPlus | CONJUGATED EXENDIN-4 | - |
dc.subject.keywordPlus | EXTENDED-RELEASE | - |
dc.subject.keywordPlus | IV INHIBITORS | - |
dc.subject.keywordPlus | IN-VIVO | - |
dc.subject.keywordPlus | ALBUMIN | - |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.