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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
- Source :
- 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
- Publication Year :
- 2008
- Publisher :
- American Chemical Society (ACS), 2008.
-
Abstract
- 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.
- Subjects :
- 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
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 51
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....0a32d41d73bd05040f7c78cb0d77936e
- Full Text :
- https://doi.org/10.1021/jm8010178