Regulation and dysregulation of endothelial permeability during systemic inflammation

KEM Hellenthal, L Brabenec, NM Wagner - Cells, 2022 - mdpi.com
Systemic inflammation can be triggered by infection, surgery, trauma or burns. During
systemic inflammation, an overshooting immune response induces tissue damage resulting …

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 …

Sampling alternative conformational states of transporters and receptors with AlphaFold2

D Del Alamo, D Sala, HS Mchaourab, J Meiler - Elife, 2022 - elifesciences.org
Equilibrium fluctuations and triggered conformational changes often underlie the functional
cycles of membrane proteins. For example, transporters mediate the passage of molecules …

3D variability analysis: Resolving continuous flexibility and discrete heterogeneity from single particle cryo-EM

A Punjani, DJ Fleet - Journal of structural biology, 2021 - Elsevier
Single particle cryo-EM excels in determining static structures of protein molecules, but
existing 3D reconstruction methods have been ineffective in modelling flexible proteins. We …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

Differential GLP-1R binding and activation by peptide and non-peptide agonists

X Zhang, MJ Belousoff, P Zhao, AJ Kooistra, TT Truong… - Molecular Cell, 2020 - cell.com
Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple
diseases; however, there remains substantial interest in the development of orally delivered …

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 …

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 …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - ASPET
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …

The role of structural dynamics in GPCR‐mediated signaling

D Hilger - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …