Emerging targets in type 2 diabetes and diabetic complications
S Demir, PP Nawroth, S Herzig… - Advanced …, 2021 - Wiley Online Library
Type 2 diabetes is a metabolic, chronic disorder characterized by insulin resistance and
elevated blood glucose levels. Although a large drug portfolio exists to keep the blood …
elevated blood glucose levels. Although a large drug portfolio exists to keep the blood …
Biased ligands at opioid receptors: Current status and future directions
The opioid crisis represents a major worldwide public health crisis that has accelerated the
search for safer and more effective opioids. Over the past few years, the identification of …
search for safer and more effective opioids. Over the past few years, the identification of …
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD
Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …
GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation
G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …
[HTML][HTML] Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics
Binding of arrestin to phosphorylated G protein-coupled receptors (GPCRs) is crucial for
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …
How Carvedilol activates β2-adrenoceptors
T Benkel, M Zimmermann, J Zeiner, S Bravo… - Nature …, 2022 - nature.com
Carvedilol is among the most effective β-blockers for improving survival after myocardial
infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are …
infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are …
Structure of the vasopressin hormone–V2 receptor–β-arrestin1 ternary complex
J Bous, A Fouillen, H Orcel, S Trapani, X Cong… - Science …, 2022 - science.org
Arrestins interact with G protein–coupled receptors (GPCRs) to stop G protein activation and
to initiate key signaling pathways. Recent structural studies shed light on the molecular …
to initiate key signaling pathways. Recent structural studies shed light on the molecular …
β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells
Abstract β-arrestins mediate regulatory processes for over 800 different G protein-coupled
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …
receptors (GPCRs) by adopting specific conformations that result from the geometry of 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 …
physiology in response to a wide array of different extracellular stimuli and thus represent …
Autoantibody mimicry of hormone action at the thyrotropin receptor
Thyroid hormones are vital in metabolism, growth and development. Thyroid hormone
synthesis is controlled by thyrotropin (TSH), which acts at the thyrotropin receptor (TSHR). In …
synthesis is controlled by thyrotropin (TSH), which acts at the thyrotropin receptor (TSHR). In …