GPR120/FFAR4 pharmacology: focus on agonists in type 2 diabetes mellitus drug discovery
The G-protein coupled receptors (GPCRs) activated by free fatty acids (FFAs) have emerged
as new and exciting drug targets, due to their plausible translation from pharmacology to …
as new and exciting drug targets, due to their plausible translation from pharmacology to …
Discovery of a potent and selective GPR120 agonist
B Shimpukade, BD Hudson, CK Hovgaard… - Journal of medicinal …, 2012 - ACS Publications
GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1
secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore …
secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore …
Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 …
SB Bharate, KVS Nemmani… - Expert opinion on …, 2009 - Taylor & Francis
Background: The family of G-protein-coupled receptors (GPCRs) serves as the target for
almost a third of currently marketed drugs and provides the predominant mechanism …
almost a third of currently marketed drugs and provides the predominant mechanism …
FFA4/GPR120: pharmacology and therapeutic opportunities
G Milligan, E Alvarez-Curto, BD Hudson… - Trends in …, 2017 - cell.com
Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor
(GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a …
(GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a …
The discovery, preclinical, and early clinical development of potent and selective GPR40 agonists for the treatment of type 2 diabetes mellitus (LY2881835 …
C Hamdouchi, SD Kahl, A Patel Lewis, GR Cardona… - 2016 - ACS Publications
The G protein-coupled receptor 40 (GPR40) also known as free fatty acid receptor 1
(FFAR1) is highly expressed in pancreatic, islet β-cells and responds to endogenous fatty …
(FFAR1) is highly expressed in pancreatic, islet β-cells and responds to endogenous fatty …
Bidirectional, iterative approach to the structural delineation of the functional “chemoprint” in GPR40 for agonist recognition
IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2007 - ACS Publications
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 …
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …
Structure− activity study of dihydrocinnamic acids and discovery of the potent FFA1 (GPR40) agonist TUG-469
E Christiansen, ME Due-Hansen, C Urban… - ACS Medicinal …, 2010 - ACS Publications
The free fatty acid 1 receptor (FFA1 or GPR40), which is highly expressed on pancreatic β-
cells and amplifies glucose-stimulated insulin secretion, has emerged as an attractive target …
cells and amplifies glucose-stimulated insulin secretion, has emerged as an attractive target …
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents
GPR120 (FFAR4) is a fatty acid sensing G protein coupled receptor (GPCR) that has been
identified as a target for possible treatment of type 2 diabetes. A selective activator of …
identified as a target for possible treatment of type 2 diabetes. A selective activator of …
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties
E Christiansen, ME Due-Hansen, C Urban… - Journal of medicinal …, 2012 - ACS Publications
FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the
potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored …
potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored …
GPR40 agonists for the treatment of type 2 diabetes mellitus: benefits and challenges
S Mohammad - Current Drug Targets, 2016 - ingentaconnect.com
Apart from functioning as an energy source and important structural components of
biological membranes, Free Fatty acids (FFAs) play a key role in the regulation of metabolic …
biological membranes, Free Fatty acids (FFAs) play a key role in the regulation of metabolic …