The endocannabinoid system as a target in cancer diseases: are we there yet?
The endocannabinoid system (ECS) has been placed in the anti-cancer spotlight in the last
decade. The immense data load published on its dual role in both tumorigenesis and …
decade. The immense data load published on its dual role in both tumorigenesis and …
Structural–functional features of the thyrotropin receptor: a class A G-protein-coupled receptor at work
G Kleinau, CL Worth, A Kreuchwig… - Frontiers in …, 2017 - frontiersin.org
The thyroid-stimulating hormone receptor (TSHR) is a member of the glycoprotein hormone
receptors, a sub-group of class A G-protein-coupled receptors (GPCRs). TSHR and its …
receptors, a sub-group of class A G-protein-coupled receptors (GPCRs). TSHR and its …
The transmembrane domains of GPCR dimers as targets for drug development
X Cai, D Wang, R Zhang, Y Chen, J Chen - Drug Discovery Today, 2023 - Elsevier
Highlights•GPCRs can form homodimers or heterodimers; these complexes regulate a wide
range of physiological and pathological functions and are emerging drug targets.•The …
range of physiological and pathological functions and are emerging drug targets.•The …
Interplay of G protein-coupled receptors with the membrane: insights from supra-atomic coarse grain molecular dynamics simulations
X Periole - Chemical reviews, 2017 - ACS Publications
G protein-coupled receptors (GPCRs) are central to many fundamental cellular signaling
pathways. They transduce signals from the outside to the inside of cells in physiological …
pathways. They transduce signals from the outside to the inside of cells in physiological …
Signal transduction and pathogenic modifications at the melanocortin-4 receptor: A structural perspective
The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of
melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast …
melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast …
Computational prediction of GPCR oligomerization
Highlights•GPCR dimers are a dynamic species with a changing dimerization interface that
shifts during receptor activation and inactivation.•Computational methodologies are a …
shifts during receptor activation and inactivation.•Computational methodologies are a …
Probing the cooperative mechanism of the μ–δ opioid receptor heterodimer by multiscale simulation
L Wang, Y Yuan, X Chen, J Chen, Y Guo… - Physical Chemistry …, 2018 - pubs.rsc.org
Accumulated experimental evidence indicated that G-protein coupled receptors (GPCRs)
could form biologically relevant oligomers and hetero-oligomers possess different functional …
could form biologically relevant oligomers and hetero-oligomers possess different functional …
FLIM–FRET-Based Structural Characterization of a Class-A GPCR Dimer in the Cell Membrane
J Yang, Z Gong, YB Lu, CJ Xu, TF Wei, MS Yang… - Journal of molecular …, 2020 - Elsevier
Class-A G protein-coupled receptors (GPCRs) are known to homo-dimerize in the
membrane. Yet, methods to characterize the structure of GPCR dimer in the native …
membrane. Yet, methods to characterize the structure of GPCR dimer in the native …
Prediction and targeting of GPCR oligomer interfaces
GPCR oligomerization has emerged as a hot topic in the GPCR field in the last years.
Receptors that are part of these oligomers can influence each other's function, although it is …
Receptors that are part of these oligomers can influence each other's function, although it is …
Oligomerization and cooperativity in GPCRs from the perspective of the angiotensin AT1 and dopamine D2 receptors
Abstract G Protein-Coupled Receptors (GPCRs) can form homo-and heterodimers or
constitute higher oligomeric clusters with other heptahelical GPCRs. In this article, multiscale …
constitute higher oligomeric clusters with other heptahelical GPCRs. In this article, multiscale …