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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2018.1
- 수록면
- 201 - 209 (9page)
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초록· 키워드
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G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay. Among the synthesized derivatives, YH18968 showed cAMP=2.8 nM; in GLUTag cell, GLP-1secretion=2.3 fold; in the HIT-T15 cell, and insulin secretion=1.9 fold. Single oral administration of YH18968 improved glucose tolerance and combined treatment with a dipeptidyl peptidase 4 (DPP-4) inhibitor augmented the glucose lowering effect as well as the plasma level of active GLP-1 in normal mice. Single oral administration of YH18968 improved glucose tolerance in a diet induced obese mice model. This effect was maintained after repeated dosing for 4 weeks. The results indicate that YH18968 combined with a DPP-4 inhibitor may be an effective therapeutic candidate for the treatment of type 2 diabetes.
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참고문헌 (27)
참고문헌 신청
Bailey, C. J. / 2008 / Metformin: effects on micro and macrovascular complications in type 2 diabetes / Cardiovasc. Drugs Ther. 22:215~224
Blad, C. C. / 2012 / G protein-coupled receptors for energy metabolites as new therapeutic targets / Nat. Rev. Drug Discov. 11:603~619
Chu, Z. L. / 2007 / A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release / Endocrinology 148:2601~2609
Cornall, L. M. / 2015 / Direct activation of the proposed anti-diabetic receptor, GPR119 in cardiomyoblasts decreases markers of muscle metabolic activity / Mol. Cell Endocrinol. 402:72~85
Cusi, K. / 1996 / Metabolic effects of metformin on glucose and lactate metabolism in noninsulin-dependent diabetes mellitus / J. Clin. Endocrinol. Metab. 81:4059~4067
Blad, C. C. / 2012 / G protein-coupled receptors for energy metabolites as new therapeutic targets / Nat. Rev. Drug Discov. 11:603~619
Chu, Z. L. / 2007 / A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release / Endocrinology 148:2601~2609
Cornall, L. M. / 2015 / Direct activation of the proposed anti-diabetic receptor, GPR119 in cardiomyoblasts decreases markers of muscle metabolic activity / Mol. Cell Endocrinol. 402:72~85
Cusi, K. / 1996 / Metabolic effects of metformin on glucose and lactate metabolism in noninsulin-dependent diabetes mellitus / J. Clin. Endocrinol. Metab. 81:4059~4067
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