Full metadata record
DC Field | Value | Language |
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dc.contributor.author | Park, Bong Gyu | - |
dc.contributor.author | Kim, Gyeong Min | - |
dc.contributor.author | Lee, Hye-Jin | - |
dc.contributor.author | Ryu, Jae Ha | - |
dc.contributor.author | Kim, Dong-Hoon | - |
dc.contributor.author | Seong, Jae-Young | - |
dc.contributor.author | Kim, Soojeong | - |
dc.contributor.author | Park, Zee-Yong | - |
dc.contributor.author | Kim, Young-Joon | - |
dc.contributor.author | Lee, Jaemin | - |
dc.contributor.author | Kim, Jae Il | - |
dc.date.accessioned | 2021-10-13T05:30:01Z | - |
dc.date.available | 2021-10-13T05:30:01Z | - |
dc.date.created | 2021-09-30 | - |
dc.date.issued | 2022-01 | - |
dc.identifier.issn | 1462-8902 | - |
dc.identifier.uri | http://hdl.handle.net/20.500.11750/15488 | - |
dc.description.abstract | Aim: To develop more effective and long-lasting antiobesity and antidiabetic therapeutics by employing novel chemical modifications of glucagon-like peptide-1 receptor (GLP-1R) agonists. Methods: We constructed novel unimolecular dual agonists of GLP-1R and glucagon receptor prepared by linking sEx-4 and native glucagon (GCG) via lysine or triazole [sEx4-GCG(K) and sEx4-GCG(T), respectively] and evaluated their antiobesity and antidiabetic efficacy in the diabetic and obese mouse model. Results: Both sEx4-GCG(K) and sEx4-GCG(T) showed the beneficial metabolic effects of GLP-1 and glucagon: they promoted weight loss and ameliorated insulin resistance and hepatic steatosis. They also increased thermogenesis in brown adipose tissue, and lipolysis and β-oxidation in white adipose tissue, with concomitant suppression of lipogenesis. Furthermore, both dual agonists activated the 5′-AMP-activated protein kinase signalling pathway and prevented palmitate-induced oxidative stress in skeletal muscle cells. Conclusion: Through their complementary dual agonism, sEx4-GCG(T) and sEx4-GCG(K) induce more marked weight loss and metabolic improvements than conventional agonists, and could be developed as novel therapeutic agents for the treatment of obesity and associated metabolic disorders in humans. © 2021 John Wiley & Sons Ltd. | - |
dc.language | English | - |
dc.publisher | John Wiley and Sons Inc | - |
dc.title | Antiobesity therapeutics with complementary dual-agonist activities at glucagon and glucagon-like peptide 1 receptors | - |
dc.type | Article | - |
dc.identifier.doi | 10.1111/dom.14546 | - |
dc.identifier.wosid | 000698628600001 | - |
dc.identifier.scopusid | 2-s2.0-85115636810 | - |
dc.identifier.bibliographicCitation | Diabetes, Obesity and Metabolism, v.24, no.1, pp.50 - 60 | - |
dc.description.isOpenAccess | TRUE | - |
dc.subject.keywordAuthor | GLP-1 analogue | - |
dc.subject.keywordAuthor | glucagon | - |
dc.subject.keywordAuthor | weight control | - |
dc.subject.keywordAuthor | energy regulation | - |
dc.subject.keywordAuthor | glycaemic control | - |
dc.subject.keywordAuthor | lipid-lowering therapy | - |
dc.subject.keywordPlus | INSULIN-SECRETION | - |
dc.subject.keywordPlus | ACID | - |
dc.subject.keywordPlus | OBESITY | - |
dc.subject.keywordPlus | OVERWEIGHT | - |
dc.subject.keywordPlus | RESISTANCE | - |
dc.subject.keywordPlus | AMPK | - |
dc.citation.endPage | 60 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 50 | - |
dc.citation.title | Diabetes, Obesity and Metabolism | - |
dc.citation.volume | 24 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Endocrinology & Metabolism | - |
dc.relation.journalWebOfScienceCategory | Endocrinology & Metabolism | - |
dc.type.docType | Article | - |
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