[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 …

Lipotoxicity and β-cell failure in type 2 diabetes: Oxidative stress linked to NADPH oxidase and ER stress

EA Vilas-Boas, DC Almeida, LP Roma, F Ortis… - Cells, 2021 - mdpi.com
A high caloric intake, rich in saturated fats, greatly contributes to the development of obesity,
which is the leading risk factor for type 2 diabetes (T2D). A persistent caloric surplus …

Acetylene group, friend or foe in medicinal chemistry

TT Talele - Journal of medicinal chemistry, 2020 - ACS Publications
The use of an acetylene (ethynyl) group in medicinal chemistry coincides with the launch of
the Journal of Medicinal Chemistry in 1959. Since then, the acetylene group has been …

[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 …

Small molecule allosteric modulators of G-protein-coupled receptors: drug–target interactions

S Lu, J Zhang - Journal of medicinal chemistry, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …

Deconvolution of complex G protein–coupled receptor signaling in live cells using dynamic mass redistribution measurements

R Schröder, N Janssen, J Schmidt, A Kebig… - Nature …, 2010 - nature.com
Label-free biosensor technology based on dynamic mass redistribution (DMR) of cellular
constituents promises to translate GPCR signaling into complex optical'fingerprints' in real …

Free fatty acid (FFA) and hydroxy carboxylic acid (HCA) receptors

S Offermanns - Annual review of pharmacology and toxicology, 2014 - annualreviews.org
Saturated and unsaturated free fatty acids (FFAs), as well as hydroxy carboxylic acids
(HCAs) such as lactate and ketone bodies, are carriers of metabolic energy, precursors of …

Applying label-free dynamic mass redistribution technology to frame signaling of G protein–coupled receptors noninvasively in living cells

R Schröder, J Schmidt, S Blättermann, L Peters… - Nature protocols, 2011 - nature.com
Label-free dynamic mass redistribution (DMR) is a cutting-edge assay technology that
enables real-time detection of integrated cellular responses in living cells. It relies on …

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 …