G protein–coupled receptor oligomerization revisited: functional and pharmacological perspectives

S Ferré, V Casadó, LA Devi, M Filizola, R Jockers… - Pharmacological …, 2014 - Elsevier
Most evidence indicates that, as for family CG protein–coupled receptors (GPCRs), family A
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …

Protease-activated receptors in hemostasis

MT Nieman - Blood, The Journal of the American Society of …, 2016 - ashpublications.org
Protease signaling in cells elicits multiple physiologically important responses via protease-
activated receptors (PARs). There are 4 members of this family of G-protein–coupled …

The GPCR heterotetramer: challenging classical pharmacology

S Ferré - Trends in pharmacological sciences, 2015 - cell.com
Two concepts are gaining increasing acceptance in G protein-coupled receptor (GPCR)
pharmacology:(i) pre-coupling of GPCRs with their preferred signaling molecules, and (ii) …

The sigma-1 receptors are present in monomeric and oligomeric forms in living cells in the presence and absence of ligands

AK Mishra, T Mavlyutov, DR Singh, G Biener… - Biochemical …, 2015 - portlandpress.com
The sigma-1 receptor (S1R) is a 223-amino-acid membrane protein that resides in the
endoplasmic reticulum and the plasma membrane of some mammalian cells. The S1R is …

Structural mechanism of G protein activation by G protein-coupled receptor

NM Duc, HR Kim, KY Chung - European journal of pharmacology, 2015 - Elsevier
G protein-coupled receptors (GPCRs) are a family of membrane receptors that regulate
physiology and pathology of various organs. Consequently, about 40% of drugs in the …

Structure and function of adenosine receptor heteromers

R Franco, A Cordomí, C Llinas del Torrent… - Cellular and Molecular …, 2021 - Springer
Adenosine is one of the most ancient signaling molecules and has receptors in both animals
and plants. In mammals there are four specific receptors, A 1, A 2A, A 2B, and A 3, which …

Methods used to study the oligomeric structure of G-protein-coupled receptors

H Guo, S An, R Ward, Y Yang, Y Liu, XX Guo… - Bioscience …, 2017 - portlandpress.com
G-protein-coupled receptors (GPCRs), which constitute the largest family of cell surface
receptors, were originally thought to function as monomers, but are now recognized as …

Protease-activated receptor 1 (PAR1) and PAR4 heterodimers are required for PAR1-enhanced cleavage of PAR4 by α-thrombin

A Arachiche, MM Mumaw, M de la Fuente… - Journal of Biological …, 2013 - ASBMB
Thrombin is a potent platelet agonist that activates platelets and other cells of the
cardiovascular system by cleaving its G-protein-coupled receptors, protease-activated …

Understanding the FRET signatures of interacting membrane proteins

C King, V Raicu, K Hristova - Journal of Biological Chemistry, 2017 - ASBMB
FRET is an indispensable experimental tool for studying membrane proteins. Currently, two
models are available for researchers to determine the oligomerization state of membrane …

Site-directed fluorescence approaches for dynamic structural biology of membrane peptides and proteins

H Raghuraman, S Chatterjee, A Das - Frontiers in Molecular …, 2019 - frontiersin.org
Membrane proteins mediate a number of cellular functions and are associated with several
diseases and also play a crucial role in pathogenicity. Due to their importance in cellular …