G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Structure, function and drug discovery of GPCR signaling

L Cheng, F Xia, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …

[HTML][HTML] Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors

MK Yadav, J Maharana, R Yadav, S Saha, P Sarma… - Cell, 2023 - cell.com
The complement system is a critical part of our innate immune response, and the terminal
products of this cascade, anaphylatoxins C3a and C5a, exert their physiological and …

A key GPCR phosphorylation motif discovered in arrestin2⋅ CCR5 phosphopeptide complexes

P Isaikina, I Petrovic, RP Jakob, P Sarma, A Ranjan… - Molecular cell, 2023 - cell.com
The two non-visual arrestins, arrestin2 and arrestin3, bind hundreds of GPCRs with different
phosphorylation patterns, leading to distinct functional outcomes. Structural information on …

Molecular insights into atypical modes of β-arrestin interaction with seven transmembrane receptors

J Maharana, FK Sano, P Sarma, MK Yadav, L Duan… - Science, 2024 - science.org
β-arrestins (βarrs) are multifunctional proteins involved in signaling and regulation of seven
transmembrane receptors (7TMRs), and their interaction is driven primarily by agonist …

Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system

P Sarma, CMC Carino, D Seetharama… - Nature …, 2023 - nature.com
Chemokine receptors constitute an important subfamily of G protein-coupled receptors
(GPCRs), and they are critically involved in a broad range of immune response …

Molecular mechanism of β-arrestin-2 pre-activation by phosphatidylinositol 4, 5-bisphosphate

K Kim, KY Chung - EMBO reports, 2024 - embopress.org
Phosphorylated residues of G protein-coupled receptors bind to the N-domain of arrestin,
resulting in the release of its C-terminus. This induces further allosteric conformational …

Arrestin‐centred interactions at the membrane and their conformational determinants

O Underwood, RS Haider, J Sanchez… - British Journal of …, 2024 - Wiley Online Library
More than 30 years after their discovery, arrestins are recognised multiprotein scaffolds that
play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling …

[HTML][HTML] ACKR3–arrestin2/3 complexes reveal molecular consequences of GRK-dependent barcoding

Q Chen, CT Schafer, S Mukherjee, M Gustavsson… - bioRxiv, 2023 - ncbi.nlm.nih.gov
SUMMARY Atypical chemokine receptor 3 (ACKR3, also known as CXCR7) is a scavenger
receptor that regulates extracellular levels of the chemokine CXCL12 to maintain …

Basal interaction of the orphan receptor GPR101 with arrestins leads to constitutive internalization

D Abboud, C Abboud, A Inoue, JC Twizere… - Biochemical …, 2024 - Elsevier
GPR101 is an orphan G protein-coupled receptor that promotes growth hormone secretion
in the pituitary. The microduplication of the GPR101 gene has been linked with the X-linked …