The Experts below are selected from a list of 132195 Experts worldwide ranked by ideXlab platform
Xi Liang - One of the best experts on this subject based on the ideXlab platform.
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identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 ffa4 gpr120
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, Anthony M Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
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Identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 (FFA4/GPR120).
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, M. Anthony Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
Steven M. Sparks - One of the best experts on this subject based on the ideXlab platform.
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identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 ffa4 gpr120
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, Anthony M Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
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Identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 (FFA4/GPR120).
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, M. Anthony Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
Naoki Azuma - One of the best experts on this subject based on the ideXlab platform.
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continuous and consecutive conversion of Free Fatty Acid in rice bran oil to triacylglycerol using immobilized lipase
Applied Microbiology and Biotechnology, 1994Co-Authors: Yoshitsugu Kosugi, Naoki AzumaAbstract:Free Fatty Acid (FFA), monoacylglycerol (MG) and diacylglycerol (DG) in high-FFA rice bran oil were continuously converted with glycerol (G) to form triacylglycerol (TG), using lipase fromRhizomucor miehei immobilized on anion-exchange resin. The reaction was continued for more than 1 month by a reactor with two circulation loops, each being connected to a fixed-bed reactor and a dehydrator. The reaction of 2 FFA + G → DG + 2H2O appeared to occur until the glycerol was exhausted; the reaction of FFA + DG → TG + H2O then followed. The consecutive esterificaion continued in the presence of 2–8 ppm water and the TG content reached 74%–88%. The industrial feasibility of this process was assessed from the standpoints of enzyme cost and value added by esterification.
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continual conversion of Free Fatty Acid in rice bran oil to triacylglycerol by immobilized lipase
Journal of the American Oil Chemists' Society, 1994Co-Authors: Yoshitsugu Kosugi, Tsutomu Kunieda, Naoki AzumaAbstract:Rice bran oil containing 30–50% Free Fatty Acid was continually converted to an oil containing more than 75% of triacylglycerol (TG) by means of immobilized lipase. The reaction was carried out at 60°C for 24 h with dehydration and reactant mixing by dry nitrogen flow under a positive nitrogen atmosphere. Enzymatic TG synthesis with evaporation by heating was not suitable because of the increasing peroxide value of the oil.
Graeme Milligan - One of the best experts on this subject based on the ideXlab platform.
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A single extracellular amino Acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias.
Scientific Reports, 2017Co-Authors: Eugenia Sergeev, Kouki Kawakami, Takayuki Kishi, Brian D Hudson, Anders Hojgaard Hansen, Daniele Bolognini, Asuka Inoue, Trond Ulven, Junken Aoki, Graeme MilliganAbstract:Free Fatty Acid Receptor 2 is a GPCR activated by short chain Fatty Acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates. A major challenge in studying this receptor is that the mouse ortholog does not have significant affinity for antagonists that are able to block the human receptor. Docking of exemplar antagonists from two chemical series to homology models of both human and mouse Free Fatty Acid Receptor 2 suggested that a single lysine - arginine variation at the extracellular face of the receptor might provide the basis for antagonist selectivity and mutational swap studies confirmed this hypothesis. Extending these studies to agonist function indicated that although the lysine - arginine variation between human and mouse orthologs had limited effect on G protein-mediated signal transduction, removal of positive charge from this residue produced a signalling-biased variant of Free Fatty Acid Receptor 2 in which Gi-mediated signalling by both short chain Fatty Acids and synthetic agonists was maintained whilst there was marked loss of agonist potency for signalling via Gq/11 and G12/13 G proteins. A single residue at the extracellular face of the receptor thus plays key roles in both agonist and antagonist function.
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metabolism meets immunity the role of Free Fatty Acid receptors in the immune system
Biochemical Pharmacology, 2016Co-Authors: Elisa Alvarezcurto, Graeme MilliganAbstract:There are significant numbers of nutrient sensing G protein-coupled receptors (GPCRs) that can be found in cells of the immune system and in tissues that are involved in metabolic function, such as the pancreas or the intestinal epithelium. The family of Free Fatty Acid receptors (FFAR1-4, GPR84), plus a few other metabolite sensing receptors (GPR109A, GPR91, GPR35) have been for this reason the focus of studies linking the effects of nutrients with immunological responses. A number of the beneficial anti-inflammatory effects credited to dietary fats such as omega-3 Fatty Acids are attributed to their actions on FFAR4.This might play an important protective role in the development of obesity, insulin resistance or asthma. The role of the short-chain Fatty Acids resulting from fermentation of fibre by the intestinal microbiota in regulating acute inflammatory responses is also discussed. Finally we assess the therapeutic potential of this family of receptors to treat pathologies where inflammation is a major factor such as type 2 diabetes, whether by the use of novel synthetic molecules or by the modulation of the individual's diet.
Jon L. Collins - One of the best experts on this subject based on the ideXlab platform.
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identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 ffa4 gpr120
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, Anthony M Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
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Identification of diarylsulfonamides as agonists of the Free Fatty Acid receptor 4 (FFA4/GPR120).
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Steven M. Sparks, Grace Chen, Jon L. Collins, Dana P. Danger, Steven T. Dock, Channa K. Jayawickreme, Stephen Jenkinson, Christopher P. Laudeman, M. Anthony Leesnitzer, Xi LiangAbstract:The exploration of a diarylsulfonamide series of Free Fatty Acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
