ArticleJournal of medicinal chemistry2007
Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition.
Article in Journal of medicinal chemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 87 citations in OpenAlex.
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- Orphan G protein-coupled receptors: the ongoing search for a home.Frontiers in pharmacology · 2024Review
- Molecular mechanism of fatty acid activation of FFAR1.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Mechanistic Studies on the Stereoselectivity of FFAR1 Modulators.Journal of chemical information and modeling · 2022Article
- In Silico Searching for Alternative Lead Compounds to Treat Type 2 Diabetes through a QSAR and Molecular Dynamics Study.Pharmaceutics · 2022Article
- Free fatty acid receptor 1: a ray of hope in the therapy of type 2 diabetes mellitus.Inflammopharmacology · 2021Review
- Anti-Apoptotic Effect of G-Protein-Coupled Receptor 40 Activation on Tumor Necrosis Factor-α-Induced Injury of Rat Proximal Tubular Cells.International journal of molecular sciences · 2019Article
- Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.Journal of medicinal chemistry · 2019Review
- Fatty Acid Signaling Mechanisms in Neural Cells: Fatty Acid Receptors.Frontiers in cellular neuroscience · 2019Review
- Quantum mechanics implementation in drug-design workflows: does it really help?Drug design, development and therapy · 2017Review
- Identifying ligands at orphan GPCRs: current status using structure-based approaches.British journal of pharmacology · 2016Review
- Free fatty acid receptors: structural models and elucidation of ligand binding interactions.BMC structural biology · 2015Article
- Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4.British journal of pharmacology · 2015Review
- The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120).The Journal of biological chemistry · 2014Article
- An efficient multistep ligand-based virtual screening approach for GPR40 agonists.Molecular diversity · 2014Article
- In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.Molecular pharmacology · 2013Article
- α-Ketoglutarate regulates acid-base balance through an intrarenal paracrine mechanism.The Journal of clinical investigation · 2013Article
- FFA1-selective agonistic activity based on docking simulation using FFA1 and GPR120 homology models.British journal of pharmacology · 2013Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
GPR40, free fatty acid receptor 1 (FFAR1), is a member of the GPCR superfamily and a possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional iterative investigation, including computational modeling and site-directed mutagenesis, aimed at delineating amino acid residues forming the functional "chemoprint" of GPR40 for agonist recognition. The computational and experimental studies revolved around the recognition of the potent synthetic agonist GW9508. Our experimentally supported model suggested that H137(4.56), R183(5.39), N244(6.55), and R258(7.35) are directly involved in interactions with the ligand. We have proposed a polarized NH-pi interaction between H137(4.56) and GW9508 as one of the contributing forces leading to the high potency of GW9508. The modeling approach presented in this work provides a general strategy for the exploration of receptor-ligand interactions in G-protein coupled receptors beginning prior to acquisition of experimental data.
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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.