Complex pharmacology of free fatty acid receptors
G protein-coupled receptors (GPCRs) are historically the most successful family of drug
targets. In recent times it has become clear that the pharmacology of these receptors is far …
targets. In recent times it has become clear that the pharmacology of these receptors is far …
Lifting the lid on GPCRs: the role of extracellular loops
GPCRs exhibit a common architecture of seven transmembrane helices (TMs) linked by
intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site …
intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site …
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
A Srivastava, J Yano, Y Hirozane, G Kefala, F Gruswitz… - Nature, 2014 - nature.com
Abstract Human GPR40 receptor (hGPR40), also known as free fatty-acid receptor 1
(FFAR1), is a G-protein-coupled receptor that binds long-chain free fatty acids to enhance …
(FFAR1), is a G-protein-coupled receptor that binds long-chain free fatty acids to enhance …
Pharmacology of free fatty acid receptors and their allosteric modulators
M Grundmann, E Bender, J Schamberger… - International journal of …, 2021 - mdpi.com
The physiological function of free fatty acids (FFAs) has long been regarded as indirect in
terms of their activities as educts and products in metabolic pathways. The observation that …
terms of their activities as educts and products in metabolic pathways. The observation that …
Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation
MC Peeters, GJP Van Westen, Q Li… - Trends in pharmacological …, 2011 - cell.com
G protein-coupled receptors (GPCRs) are the major drug target of medicines on the market
today. Therefore, much research is and has been devoted to the elucidation of the function …
today. Therefore, much research is and has been devoted to the elucidation of the function …
Free fatty acid receptors act as nutrient sensors to regulate energy homeostasis
Free fatty acids (FFAs) have been demonstrated to act as ligands of several G-protein-
coupled receptors (GPCRs)(FFAR1, FFAR2, FFAR3, GPR84, and GPR120). These fatty acid …
coupled receptors (GPCRs)(FFAR1, FFAR2, FFAR3, GPR84, and GPR120). These fatty acid …
Classification model for the second extracellular loop of class A GPCRs
A Nicoli, A Dunkel, T Giorgino, C de Graaf… - Journal of Chemical …, 2022 - ACS Publications
The extracellular loop 2 (ECL2) is the longest and the most diverse loop among class AG
protein-coupled receptors (GPCRs). It connects the transmembrane (TM) helices 4 and 5 …
protein-coupled receptors (GPCRs). It connects the transmembrane (TM) helices 4 and 5 …
The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?
AD Mancini, V Poitout - Trends in Endocrinology & Metabolism, 2013 - cell.com
Glucose homeostasis requires the highly coordinated regulation of insulin secretion by
pancreatic β cells. This is primarily mediated by glucose itself, but other nutrients, including …
pancreatic β cells. This is primarily mediated by glucose itself, but other nutrients, including …
Structure and activation of the visual pigment rhodopsin
SO Smith - Annual review of biophysics, 2010 - annualreviews.org
Rhodopsin is a specialized G protein–coupled receptor (GPCR) found in vertebrate rod
cells. Absorption of light by its 11-cis retinal chromophore leads to rapid photochemical …
cells. Absorption of light by its 11-cis retinal chromophore leads to rapid photochemical …
Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders
Free fatty acids (FFAs) are not only essential nutritional components, but they also act as
signaling molecules in various physiological processes. Recently, a G-protein-coupled …
signaling molecules in various physiological processes. Recently, a G-protein-coupled …