Molecular insights into GPCR mechanisms for drugs of abuse

OB Sanchez-Reyes, G Zilberg, JD McCorvy… - Journal of biological …, 2023 - ASBMB
Substance abuse is on the rise, and while many people may use illicit drugs mainly due to
their rewarding effects, their societal impact can range from severe, as is the case for …

Genetic and biased agonist-mediated reductions in β-arrestin recruitment prolong cAMP signaling at glucagon family receptors

B Jones, ER McGlone, Z Fang, P Pickford… - Journal of Biological …, 2021 - ASBMB
Receptors for the peptide hormones glucagon-like peptide-1 (GLP-1R), glucose-dependent
insulinotropic polypeptide (GIPR), and glucagon (GCGR) are important regulators of insulin …

Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor

V Burghi, JS Paradis, A Officer… - Journal of Biological …, 2023 - ASBMB
β-arrestins play a key role in G protein–coupled receptor (GPCR) internalization, trafficking,
and signaling. Whether β-arrestins act independently of G protein–mediated signaling has …

Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu5a receptor internalization

JR van Senten, TC Møller, E Von Moo… - Journal of Biological …, 2022 - ASBMB
The internalization of G protein–coupled receptors (GPCRs) can be regulated by PKC.
However, most tools available to study the contribution of PKC isozymes have considerable …

G protein βγ translocation to the Golgi apparatus activates MAPK via p110γ-p101 heterodimers

M Khater, Z Wei, X Xu, W Huang, BL Lokeshwar… - Journal of Biological …, 2021 - ASBMB
The Golgi apparatus (GA) is a cellular organelle that plays a critical role in the processing of
proteins for secretion. Activation of G protein–coupled receptors at the plasma membrane …

A single phenylalanine residue in β-arrestin2 critically regulates its binding to G protein–coupled receptors

PY Jean-Charles, V Rajiv, S Sarker, S Han… - Journal of Biological …, 2022 - ASBMB
Arrestins and their yeast homologs, arrestin-related trafficking adaptors (ARTs), share a
stretch of 29 amino acids called the ART motif. However, the functionality of that motif is …

The ubiquitination status of the glucagon receptor determines signal bias

S Kaur, B Sokrat, ME Capozzi, K El, Y Bai… - Journal of Biological …, 2023 - ASBMB
The pancreatic hormone glucagon activates the glucagon receptor (GCGR), a class B seven-
transmembrane G protein-coupled receptor that couples to the stimulatory heterotrimeric G …