A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias [PDF]
, 2017 Free Fatty Acid Receptor 2 is a GPCR activated by short chain fatty acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates.
Aoki, Junken +9 more
core +3 more sources
BIASED AGONISM OF THREE DIFFERENT CANNABINOID RECEPTOR AGONISTS IN MOUSE BRAIN CORTEX
Frontiers in Pharmacology, 2016 Cannabinoid receptors are able to couple to different families of G-proteins when activated by an agonist drug. It has been suggested that different intracellular responses may be activated depending on the ligand.
Rebeca Diez-Alarcia +12 more
doaj +1 more source
Does modulation of the endocannabinoid system have potential therapeutic utility in cerebellar ataxia? [PDF]
, 2016 Cerebellar ataxias represent a spectrum of disorders which are, however, linked by common symptoms of motor incoordination and are typically associated with deficient in Purkinje cell firing activity and, often, degeneration. Cerebellar ataxias currently
Stephens, G. J.
core +1 more source
Biased agonism in peptide-GPCRs: A structural perspective
Pharmacology & TherapeuticsG protein-coupled receptors (GPCRs) are dynamic membrane receptors that transduce extracellular signals to the cell interior by forming a ligand-receptor-effector (ternary) complex that functions via allosterism. Peptides constitute an important class of ligands that interact with their cognate GPCRs (peptide-GPCRs) to form the ternary complex. "Biased
Tharindunee, Jayakody +6 more
openaire +2 more sources
Novel mechanisms of G-protein-coupled receptors functions: AT1 angiotensin receptor acts as a signaling hub and focal point of receptor cross-talk [PDF]
, 2018 AT1 angiotensin receptor (AT1R), a prototypical G protein-coupled receptor (GPCR), is the main receptor, which mediates the effects of the renin-angiotensin system (RAS).
Balla, András +3 more
core +1 more source
The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120) [PDF]
, 2014 The long-chain fatty acid receptor FFA4(previously GPR120) is receiving substantial interest as a novel target for the treatment of metabolic and inflammatory disease.
Hudson, Brian D. +3 more
core +1 more source
Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors [PDF]
, 2015 Glycoprotein hormones, follicle-stimulating hormone (FSH), luteinizing hormone (LH), and thyroid stimulating hormone (TSH) are heterodimeric proteins with a common subunit and hormone-specific subunit.
Henry N. Yu +2 more
core +2 more sources
Emerging strategies targeting CB2 cannabinoid receptor: Biased agonism and allosterism
Biochemical Pharmacology, 2018 During these last years, the CB2 cannabinoid receptor has emerged as a potential anti-inflammatory target in diseases such as multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, ischemic stroke, autoimmune diseases, osteoporosis, and cancer.
Morales, Paula +2 more
openaire +3 more sources
Receptor activity modifying protein-directed G protein signaling specificity for the calcitonin gene-related peptide family of receptors [PDF]
, 2016 The calcitonin gene-related peptide (CGRP) family of G protein-coupled receptors (GPCRs) is formed through association of the calcitonin receptor-like receptor (CLR) and one of three receptor activitymodifying proteins (RAMPs).
Weston, Cathryn +11 more
core +1 more source
Acta Pharmaceutica Sinica BG protein-coupled receptors (GPCRs) represent key drug targets, with approximately 30%–40% of all medications acting on these receptors. Recent advancements have uncovered the complexity of GPCR signaling, including biased signaling, which allows ...
Michał K. Jastrzębski +11 more
doaj +1 more source