N-Thiazolylamide-based free fatty-acid 2 receptor agonists: Discovery, lead optimization and demonstration of off-target effect in a diabetes model.
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J. Olefsky | F. Ooms | François Lenoir | H. Hoveyda | G. Fraser | J. Bernard | Sébastien Blanc | Joanne C. McNelis | Julien Parcq | L. Zoute | G. Dutheuil | Mohamed El Bousmaqui | C. Brantis | D. Schils | Alexey Lapin | S. Guitard | Sarah Rorive | Sandrine Hospied | Didier Schils
[1] G. Tsujimoto,et al. The short chain fatty acid receptor GPR43 regulates inflammatory signals in adipose tissue M2-type macrophages , 2017, PloS one.
[2] B. Hudson,et al. Complex Pharmacology of Free Fatty Acid Receptors. , 2017, Chemical reviews.
[3] Rockann E. Mosser,et al. Loss of Free Fatty Acid Receptor 2 leads to impaired islet mass and beta cell survival , 2016, Scientific Reports.
[4] A. Van der Aa,et al. Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects , 2016, British journal of clinical pharmacology.
[5] S. Pandey,et al. A protocol for amide bond formation with electron deficient amines and sterically hindered substrates. , 2016, Organic & biomolecular chemistry.
[6] B. Hudson,et al. Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands* , 2015, The Journal of Biological Chemistry.
[7] R. M. Owen,et al. An analysis of the attrition of drug candidates from four major pharmaceutical companies , 2015, Nature Reviews Drug Discovery.
[8] B. Wicksteed,et al. An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion. , 2015, Molecular endocrinology.
[9] Rik van der Kant,et al. GPR43 Potentiates β-Cell Function in Obesity , 2015, Diabetes.
[10] Stefan Offermanns,et al. Loss of FFA2 and FFA3 increases insulin secretion and improves glucose tolerance in type 2 diabetes , 2015, Nature Medicine.
[11] L. Nelles,et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. , 2014, Journal of medicinal chemistry.
[12] A. Hopkins,et al. The role of ligand efficiency metrics in drug discovery , 2014, Nature Reviews Drug Discovery.
[13] W. Garrett,et al. The Microbial Metabolites, Short-Chain Fatty Acids, Regulate Colonic Treg Cell Homeostasis , 2013, Science.
[14] G. Tsujimoto,et al. The gut microbiota suppresses insulin-mediated fat accumulation via the short-chain fatty acid receptor GPR43 , 2013, Nature Communications.
[15] Graeme Milligan,et al. Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor* , 2013, The Journal of Biological Chemistry.
[16] B. Hudson,et al. Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3* , 2012, The Journal of Biological Chemistry.
[17] A. M. Habib,et al. Short-Chain Fatty Acids Stimulate Glucagon-Like Peptide-1 Secretion via the G-Protein–Coupled Receptor FFAR2 , 2012, Diabetes.
[18] Niklas Blomberg,et al. Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules. , 2011, Bioorganic & medicinal chemistry letters.
[19] M. Hann. Molecular obesity, potency and other addictions in drug discovery , 2011 .
[20] John P. Overington,et al. Probing the links between in vitro potency, ADMET and physicochemical parameters , 2011, Nature Reviews Drug Discovery.
[21] S. Wong,et al. The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. , 2010, Bioorganic & medicinal chemistry letters.
[22] P. Rosenstiel,et al. G Protein-Coupled Receptor 43 Is Essential for Neutrophil Recruitment during Intestinal Inflammation1 , 2009, The Journal of Immunology.
[23] T. Ritchie,et al. The impact of aromatic ring count on compound developability--are too many aromatic rings a liability in drug design? , 2009, Drug discovery today.
[24] R. Xavier,et al. Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43 , 2009, Nature.
[25] C. Humblet,et al. Escape from flatland: increasing saturation as an approach to improving clinical success. , 2009, Journal of medicinal chemistry.
[26] Yang Li,et al. Identification and Functional Characterization of Allosteric Agonists for the G Protein-Coupled Receptor FFA2 , 2008, Molecular Pharmacology.
[27] P. Leeson,et al. The influence of drug-like concepts on decision-making in medicinal chemistry , 2007, Nature Reviews Drug Discovery.
[28] Richard Morphy,et al. The influence of target family and functional activity on the physicochemical properties of pre-clinical compounds. , 2006, Journal of medicinal chemistry.
[29] Ki-Choon Choi,et al. Acetate and propionate short chain fatty acids stimulate adipogenesis via GPCR43. , 2005, Endocrinology.
[30] M. Parmentier,et al. Functional Characterization of Human Receptors for Short Chain Fatty Acids and Their Role in Polymorphonuclear Cell Activation* , 2003, Journal of Biological Chemistry.
[31] S. Dowell,et al. The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids* , 2003, The Journal of Biological Chemistry.
[32] M. Bohlooly-y,et al. Improved glucose control and reduced body fat mass in free fatty acid receptor 2-deficient mice fed a high-fat diet. , 2011, American journal of physiology. Endocrinology and metabolism.
[33] J. Comer,et al. Lipophilicity measurements by liquid chromatography. , 2006, Advances in chromatography.