[HTML][HTML] Free fatty acid receptors in health and disease

I Kimura, A Ichimura, R Ohue-Kitano… - Physiological …, 2019 - journals.physiology.org
Fatty acids are metabolized and synthesized as energy substrates during biological
responses. Long-and medium-chain fatty acids derived mainly from dietary triglycerides, and …

Complex pharmacology of free fatty acid receptors

G Milligan, B Shimpukade, T Ulven… - Chemical …, 2017 - ACS Publications
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 …

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 …

[PDF][PDF] Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets

T Ulven - Frontiers in endocrinology, 2012 - frontiersin.org
The deorphanization of the free fatty acid (FFA) receptors FFA1 (GPR40), FFA2 (GPR43),
FFA3 (GPR41), GPR84, and GPR120 has made clear that the body is capable of …

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

J Lu, N Byrne, J Wang, G Bricogne, FK Brown… - Nature structural & …, 2017 - nature.com
Clinical studies indicate that partial agonists of the G-protein-coupled, free fatty acid receptor
1 GPR40 enhance glucose-dependent insulin secretion and represent a potential …

Fatty acid signaling mechanisms in neural cells: fatty acid receptors

LJ Falomir-Lockhart, GF Cavazzutti… - Frontiers in cellular …, 2019 - frontiersin.org
Fatty acids (FAs) are typically associated with structural and metabolic roles, as they can be
stored as triglycerides, degraded by β-oxidation or used in phospholipids' synthesis, the …

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 …

Discovery of TAK-875: a potent, selective, and orally bioavailable GPR40 agonist

N Negoro, S Sasaki, S Mikami, M Ito… - ACS medicinal …, 2010 - ACS Publications
GPR40, one of the G protein-coupled receptors predominantly expressed in pancreatic β-
cells, mediates enhancement of glucose-stimulated insulin secretion by free fatty acids. A …

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 …

Free fatty acid receptors and their role in regulation of energy metabolism

T Hara, I Kimura, D Inoue, A Ichimura… - Reviews of Physiology …, 2013 - Springer
The free fatty acid receptor (FFAR) is a G protein-coupled receptor (GPCR) activated by free
fatty acids (FFAs), which play important roles not only as essential nutritional components …