G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Serial femtosecond crystallography

TRM Barends, B Stauch, V Cherezov… - Nature reviews Methods …, 2022 - nature.com
With the advent of X-ray free-electron lasers (XFELs), new, high-throughput serial
crystallography techniques for macromolecular structure determination have emerged …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

[HTML][HTML] A condensate-hardening drug blocks RSV replication in vivo

J Risso-Ballester, M Galloux, J Cao, R Le Goffic… - Nature, 2021 - nature.com
Biomolecular condensates have emerged as an important subcellular organizing principle.
Replication of many viruses, including human respiratory syncytial virus (RSV), occurs in …

Advances and challenges in time-resolved macromolecular crystallography

G Brändén, R Neutze - Science, 2021 - science.org
BACKGROUND Conformational changes are essential for the correct functioning of
biological macromolecules. Time-resolved x-ray crystallography extends an extremely …

Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?

F Ballante, AJ Kooistra, S Kampen, C de Graaf… - Pharmacological …, 2021 - ASPET
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

Retinal isomerization in bacteriorhodopsin captured by a femtosecond x-ray laser

P Nogly, T Weinert, D James, S Carbajo, D Ozerov… - Science, 2018 - science.org
INTRODUCTION Retinal is a light-sensitive protein ligand that is used by all domains of life
to process the information and energy content of light. Retinal-binding proteins are integral …

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

Y Kang, XE Zhou, X Gao, Y He, W Liu, A Ishchenko… - Nature, 2015 - nature.com
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins.
Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous …

Linac coherent light source: The first five years

C Bostedt, S Boutet, DM Fritz, Z Huang, HJ Lee… - Reviews of Modern …, 2016 - APS
A new scientific frontier opened in 2009 with the start of operations of the world's first x-ray
free-electron laser (FEL), the Linac Coherent Light Source (LCLS), at SLAC National …

SwissFEL: the Swiss X-ray free electron laser

CJ Milne, T Schietinger, M Aiba, A Alarcon, J Alex… - Applied Sciences, 2017 - mdpi.com
The SwissFEL X-ray Free Electron Laser (XFEL) facility started construction at the Paul
Scherrer Institute (Villigen, Switzerland) in 2013 and will be ready to accept its first users in …