GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
G protein-coupled receptors are important drug targets that engage and activate signaling
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
[HTML][HTML] Diffusive intracellular interactions: On the role of protein net charge and functional adaptation
EV Estrada, N Zhang, H Wennerström… - Current opinion in …, 2023 - Elsevier
A striking feature of nucleic acids and lipid membranes is that they all carry net negative
charge and so is true for the majority of intracellular proteins. It is suggested that the role of …
charge and so is true for the majority of intracellular proteins. It is suggested that the role of …
GPCRome-wide analysis of G-protein-coupling diversity using a computational biology approach
GPCRs are master regulators of cell signaling by transducing extracellular stimuli into the
cell via selective coupling to intracellular G-proteins. Here we present a computational …
cell via selective coupling to intracellular G-proteins. Here we present a computational …
The dark sides of the GPCR tree‐research progress on understudied GPCRs
MM Scharf, LJ Humphrys, S Berndt… - British Journal of …, 2024 - Wiley Online Library
A large portion of the human GPCRome is still in the dark and understudied, consisting even
of entire subfamilies of GPCRs such as odorant receptors, class A and C orphans, adhesion …
of entire subfamilies of GPCRs such as odorant receptors, class A and C orphans, adhesion …
Time-resolved cryo-EM of G-protein activation by a GPCR
MM Papasergi-Scott, G Pérez-Hernández, H Batebi… - Nature, 2024 - nature.com
G-protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by stimulating
guanine nucleotide exchange in the Gα subunit. To visualize this mechanism, we developed …
guanine nucleotide exchange in the Gα subunit. To visualize this mechanism, we developed …
[HTML][HTML] Sequence-directed concentration of G protein-coupled receptors in COPII vesicles
G protein-coupled receptors (GPCRs) constitute the largest superfamily of plasma
membrane signaling proteins. However, virtually nothing is known about their recruitment to …
membrane signaling proteins. However, virtually nothing is known about their recruitment to …
Structures of Ric-8B in complex with Gα protein folding clients reveal isoform specificity mechanisms
MM Papasergi-Scott, FE Kwarcinski, M Yu, O Panova… - Structure, 2023 - cell.com
Mammalian Ric-8 proteins act as chaperones to regulate the cellular abundance of
heterotrimeric G protein α subunits. The Ric-8A isoform chaperones Gαi/o, Gα12/13, and …
heterotrimeric G protein α subunits. The Ric-8A isoform chaperones Gαi/o, Gα12/13, and …
Binding kinetics drive G protein subtype selectivity at the β1-adrenergic receptor
G protein-coupled receptors (GPCRs) bind to different G protein α-subtypes with varying
degrees of selectivity. The mechanism by which GPCRs achieve this selectivity is still …
degrees of selectivity. The mechanism by which GPCRs achieve this selectivity is still …
A neurodevelopmental disorder mutation locks G proteins in the transitory pre-activated state
Many neurotransmitter receptors activate G proteins through exchange of GDP for GTP. The
intermediate nucleotide-free state has eluded characterization, due largely to its inherent …
intermediate nucleotide-free state has eluded characterization, due largely to its inherent …
Conformation-and activation-based BRET sensors differentially report on GPCR–G protein coupling
SC Wright, C Avet, SA Gaitonde, I Muneta-Arrate… - Science …, 2024 - science.org
G protein–coupled receptors (GPCRs) regulate cellular signaling processes by coupling to
diverse combinations of heterotrimeric G proteins composed of Gα, Gβ, and Gγ subunits …
diverse combinations of heterotrimeric G proteins composed of Gα, Gβ, and Gγ subunits …