Serial femtosecond crystallography

TRM Barends, B Stauch, V Cherezov… - Nature Reviews …, 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 …

Angiotensin II signal transduction: an update on mechanisms of physiology and pathophysiology

SJ Forrester, GW Booz, CD Sigmund… - Physiological …, 2018 - journals.physiology.org
The renin-angiotensin-aldosterone system plays crucial roles in cardiovascular physiology
and pathophysiology. However, many of the signaling mechanisms have been unclear. The …

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 …

Deep docking: a deep learning platform for augmentation of structure based drug discovery

F Gentile, V Agrawal, M Hsing, AT Ton, F Ban… - ACS central …, 2020 - ACS Publications
Drug discovery is a rigorous process that requires billion dollars of investments and decades
of research to bring a molecule “from bench to a bedside”. While virtual docking can …

Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design

S Lu, X He, Z Yang, Z Chai, S Zhou, J Wang… - Nature …, 2021 - nature.com
G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Novel therapeutic approaches targeting the renin-angiotensin system and associated peptides in hypertension and heart failure

LB Arendse, AHJ Danser, M Poglitsch, RM Touyz… - Pharmacological …, 2019 - Elsevier
Despite the success of renin-angiotensin system (RAS) blockade by angiotensin-converting
enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT 1 R) blockers, current …

Advances in therapeutic peptides targeting G protein-coupled receptors

AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

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 …

Conformational basis of G protein-coupled receptor signaling versatility

LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …