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 …
crystallography techniques for macromolecular structure determination have emerged …
Angiotensin II signal transduction: an update on mechanisms of physiology and pathophysiology
The renin-angiotensin-aldosterone system plays crucial roles in cardiovascular physiology
and pathophysiology. However, many of the signaling mechanisms have been unclear. The …
and pathophysiology. However, many of the signaling mechanisms have been unclear. The …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
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 …
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
Biased signalling: from simple switches to allosteric microprocessors
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 …
genome and some of the most common drug targets. It is now well established that GPCRs …
Deep docking: a deep learning platform for augmentation of structure based drug discovery
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 …
of research to bring a molecule “from bench to a bedside”. While virtual docking can …
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 …
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
The angiotensin AT2 receptor: from a binding site to a novel therapeutic target
UM Steckelings, RE Widdop, ED Sturrock… - Pharmacological …, 2022 - ASPET
Discovered more than 30 years ago, the angiotensin AT2 receptor (AT2R) has evolved from
a binding site with unknown function to a firmly established major effector within the …
a binding site with unknown function to a firmly established major effector within the …
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 - ASPET
Despite the success of renin-angiotensin system (RAS) blockade by angiotensin-converting
enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT1R) blockers, current …
enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT1R) blockers, current …
Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser
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 …
Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous …