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Serial femtosecond crystallography
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 …
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 …
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 …
Novel therapeutic approaches targeting the renin-angiotensin system and associated peptides in hypertension and heart failure
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 …
enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT 1 R) blockers, current …
Advances in therapeutic peptides targeting G protein-coupled receptors
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
Linac coherent light source: The first five years
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 …
free-electron laser (FEL), the Linac Coherent Light Source (LCLS), at SLAC National …
Conformational basis of G protein-coupled receptor signaling versatility
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 …