A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias.

Autor: Bolognini D; From the Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom., Moss CE; From the Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom, the Medical Research Council Toxicology Unit, University of Leicester, Leicester LE1 9HN, United Kingdom., Nilsson K; the Cardiovascular and Metabolic Diseases., Petersson AU; Respiratory, Inflammatory and Autoimmune Diseases Innovative Medicines and Early Development Biotech Unit, Department of Medicinal Chemistry, and., Donnelly I; the Institute of Cardiovascular and Medical Sciences, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom., Sergeev E; From the Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom., König GM; Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany, and., Kostenis E; the Molecular, Cellular and Pharmacobiology Section., Kurowska-Stolarska M; the Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom., Miller A; the Institute of Cardiovascular and Medical Sciences, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom., Dekker N; the Discovery Sciences, Reagents and Assay Development, AstraZeneca, Mölndal, Pepparedsleden 1, SE-431 83, Mölndal, Sweden., Tobin AB; From the Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom, the Medical Research Council Toxicology Unit, University of Leicester, Leicester LE1 9HN, United Kingdom., Milligan G; From the Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom, Graeme.Milligan@glasgow.ac.uk.

Publikováno v: The Journal of biological chemistry [J Biol Chem] 2016 Sep 02; Vol. 291 (36), pp. 18915-31. Date of Electronic Publication: 2016 Jul 05.

GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.

Autor: Georgsson J; CVMD Medicinal Chemistry, ‡CVMD DMPK, ∥CVMD Bioscience, +Discovery Sciences, and ⊥RIA Medicinal Chemistry, AstraZeneca, Pepparedsleden 1, 431 83 Mölndal, Sweden., Bergström F, Nordqvist A, Watson MJ, Blundell CD, Johansson MJ, Petersson AU, Yuan ZQ, Zhou Y, Kristensson L, Kakol-Palm D, Tyrchan C, Wellner E, Bauer U, Brodin P, Svensson Henriksson A

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2014 Jul 24; Vol. 57 (14), pp. 5935-48. Date of Electronic Publication: 2014 Jul 02.

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Autor: Barlind JG; Cardiovascular and Gastrointestinal Innovative Medicines Unit Mölndal, AstraZeneca R&D, S-431 83 Mölndal, Sweden., Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2012 Dec 13; Vol. 55 (23), pp. 10610-29. Date of Electronic Publication: 2012 Nov 21.