Structure determination of GPCRs: cryo-EM compared with X-ray crystallography

J García-Nafría, CG Tate - Biochemical Society Transactions, 2021 - portlandpress.com
G protein-coupled receptors (GPCRs) are the largest single family of cell surface receptors
encoded by the human genome and they play pivotal roles in co-ordinating cellular systems …

Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM

SJ Piper, RM Johnson, D Wootten, PM Sexton - Chemical reviews, 2022 - ACS Publications
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …

Molecular basis for selective activation of DREADD-based chemogenetics

S Zhang, RH Gumpper, XP Huang, Y Liu, BE Krumm… - Nature, 2022 - nature.com
Designer receptors exclusively activated by designer drugs (DREADDs) represent a
powerful chemogenetic technology for the remote control of neuronal activity and cellular …

[HTML][HTML] Structures of signaling complexes of lipid receptors S1PR1 and S1PR5 reveal mechanisms of activation and drug recognition

Y Yuan, G Jia, C Wu, W Wang, L Cheng, Q Li, Z Li… - Cell research, 2021 - nature.com
Abstract Sphingosine-1-phosphate (S1P) is an important bioactive lipid molecule in cell
membrane metabolism and binds to G protein-coupled S1P receptors (S1PRs) to regulate …

[HTML][HTML] Specific binding of GPR174 by endogenous lysophosphatidylserine leads to high constitutive Gs signaling

Y Nie, Z Qiu, S Chen, Z Chen, X Song, Y Ma… - Nature …, 2023 - nature.com
Many orphan G protein-coupled receptors (GPCRs) remain understudied because their
endogenous ligands are unknown. Here, we show that a group of class A/rhodopsin-like …

New insights into the structure and function of class B1 GPCRs

BP Cary, X Zhang, J Cao, RM Johnson… - Endocrine …, 2023 - academic.oup.com
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

[HTML][HTML] Molecular insights into the regulation of constitutive activity by RNA editing of 5HT2C serotonin receptors

RH Gumpper, JF Fay, BL Roth - Cell reports, 2022 - cell.com
RNA editing is a process by which post-transcriptional changes of mRNA nucleotides alter
protein function through modification of the amino acid content. The 5HT 2C serotonin …

The role of G protein conformation in receptor–G protein selectivity

W Jang, S Lu, X Xu, G Wu, NA Lambert - Nature chemical biology, 2023 - nature.com
G protein-coupled receptors (GPCRs) selectively activate at least one of the four families of
heterotrimeric G proteins, but the mechanism of coupling selectivity remains unclear …

[HTML][HTML] Routine sub-2.5 Å cryo-EM structure determination of GPCRs

R Danev, M Belousoff, YL Liang, X Zhang… - Nature …, 2021 - nature.com
Cryo-electron microscopy (cryo-EM) of small membrane proteins, such as G protein-coupled
receptors (GPCRs), remains challenging. Pushing the performance boundaries of the …

[HTML][HTML] Structural basis of neuropeptide Y signaling through Y1 receptor

C Park, J Kim, SB Ko, YK Choi, H Jeong, H Woo… - Nature …, 2022 - nature.com
Neuropeptide Y (NPY) is highly abundant in the brain and involved in various physiological
processes related to food intake and anxiety, as well as human diseases such as obesity …