Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes
| Autor: | Andreas Spinrath, Christian Urban, Andrew D. Bond, Elisabeth Christiansen, Evi Kostenis, Matthias U. Kassack, Nicole Merten, Alexandra Hamacher, Trond Ulven, Christel Drewke, Susanne Ullrich, Kasper K. Karlsen, Kathrin Liebscher |
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| Rok vydání: | 2008 |
| Předmět: |
Models
Molecular Agonist medicine.medical_specialty Time Factors medicine.drug_class Carboxylic acid medicine.medical_treatment Type 2 diabetes Crystallography X-Ray Receptors G-Protein-Coupled Mice Structure-Activity Relationship Free fatty acid receptor 1 Diabetes mellitus Internal medicine Insulin Secretion Drug Discovery medicine Animals Humans Insulin G protein-coupled receptor chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Stereoisomerism medicine.disease In vitro Rats Glucose Endocrinology Diabetes Mellitus Type 2 chemistry Cinnamates Molecular Medicine |
| Zdroj: | Christiansen, E, Urban, C, Merten, N, Liebscher, K, Karlsen, K, Hamacher, A, Spinrath, A, Bond, A, Drewke, C, Ullrich, S, Kassack, M, Kostenis, E & Ulven, T 2008, ' Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes ', Journal of Medicinal Chemistry, vol. 51, no. 22, pp. 7061-7064 . https://doi.org/10.1021/jm8010178 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm8010178 |
| Popis: | Udgivelsesdato: 2008-Oct-24 A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA 1) has been discovered and explored. The preferred compound 20 (TUG-424, EC 50 = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA 1 in metabolic diseases such as diabetes or obesity. |
| Databáze: | OpenAIRE |
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