ArticleACS medicinal chemistry letters2015
Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
8 citing papers in PubMed, 33 citations in OpenAlex.
- GPCRs involved in metabolic diseases: pharmacotherapeutic development updates.Acta pharmacologica Sinica · 2024Review
- Recent Developments in Drug Design of Oral Synthetic Free Fatty Acid Receptor 1 Agonists.Drug design, development and therapy · 2024Review
- Immunometabolism changes in fibrosis: from mechanisms to therapeutic strategies.Frontiers in pharmacology · 2023Review
- How Arrestins and GRKs Regulate the Function of Long Chain Fatty Acid Receptors.International journal of molecular sciences · 2022Review
- Identification of behenic acid as medicinal food for the diabetes mellitus: structure-based computational approach and molecular dynamics simulation studies.Journal of molecular modeling · 2022Article
- Targeting metabolic dysregulation for fibrosis therapy.Nature reviews. Drug discovery · 2020Review
- SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.ACS medicinal chemistry letters · 2017Article
- Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist.ACS medicinal chemistry letters · 2016Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 agonists stimulate insulin secretion in the presence of high glucose concentration. On the basis of this mechanism, GPR40 agonists are possible novel insulin secretagogues with reduced or no risk of hypoglycemia. The improvement of in vitro activity and metabolic stability of compound 1 led to the discovery of 13, (3S)-3-ethoxy-3-(4-{[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]oxy}phenyl)propanoic acid, as a potent and orally available GPR40 agonist. Compound 13 (DS-1558) was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.