Dissecting the role of protein phosphorylation: a chemical biology toolbox

T Bilbrough, E Piemontese, O Seitz - Chemical Society Reviews, 2022 - pubs.rsc.org
Protein phosphorylation is a crucial regulator of protein and cellular function, yet, despite
identifying an enormous number of phosphorylation sites, the role of most is still unclear …

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 …

Conserved class B GPCR activation by a biased intracellular agonist

LH Zhao, Q He, Q Yuan, Y Gu, X He, H Shan, J Li… - Nature, 2023 - nature.com
Class B G-protein-coupled receptors (GPCRs), including glucagon-like peptide 1 receptor
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …

Structural insights into CXCR4 modulation and oligomerization

K Saotome, LL McGoldrick, JH Ho, TF Ramlall… - Nature Structural & …, 2024 - nature.com
Activation of the chemokine receptor CXCR4 by its chemokine ligand CXCL12 regulates
diverse cellular processes. Previously reported crystal structures of CXCR4 revealed the …

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 …

Applications and prospects of cryo-EM in drug discovery

KF Zhu, C Yuan, YM Du, KL Sun, XK Zhang… - Military Medical …, 2023 - Springer
Drug discovery is a crucial part of human healthcare and has dramatically benefited human
lifespan and life quality in recent centuries, however, it is usually time-and effort-consuming …

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 …

High-resolution cryo-EM performance comparison of two latest-generation cryo electron microscopes on the human ribosome

L Fréchin, S Holvec, O von Loeffelholz… - Journal of Structural …, 2023 - Elsevier
Recent technological advances in cryo electron microscopy (cryo-EM) have led to new
opportunities in the structural biology field. Here we benchmark the performance of two 300 …

Classification model for the second extracellular loop of class A GPCRs

A Nicoli, A Dunkel, T Giorgino, C de Graaf… - Journal of Chemical …, 2022 - ACS Publications
The extracellular loop 2 (ECL2) is the longest and the most diverse loop among class AG
protein-coupled receptors (GPCRs). It connects the transmembrane (TM) helices 4 and 5 …

Targeting VIP and PACAP receptor signaling: new insights into designing drugs for the PACAP subfamily of receptors

J Lu, SJ Piper, P Zhao, LJ Miller, D Wootten… - International journal of …, 2022 - mdpi.com
Pituitary Adenylate Cyclase-Activating Peptide (PACAP) and Vasoactive Intestinal Peptide
(VIP) are neuropeptides involved in a diverse array of physiological and pathological …