Trends in GPCR drug discovery: new agents, targets and indications
G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …
due to their substantial involvement in human pathophysiology and their pharmacological …
Therapeutically exploiting STAT3 activity in cancer—using tissue repair as a road map
The tightly orchestrated temporal and spatial control of signal transducer and activator of
transcription 3 (STAT3) activity in epithelial, immune and stromal cells is critical for wound …
transcription 3 (STAT3) activity in epithelial, immune and stromal cells is critical for wound …
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 …
GPCR dynamics: structures in motion
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …
both human membrane proteins and drug targets depends critically on their ability to …
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 …
Lack of beta-arrestin signaling in the absence of active G proteins
M Grundmann, N Merten, D Malfacini, A Inoue… - Nature …, 2018 - nature.com
G protein-independent, arrestin-dependent signaling is a paradigm that broadens the
signaling scope of G protein-coupled receptors (GPCRs) beyond G proteins for numerous …
signaling scope of G protein-coupled receptors (GPCRs) beyond G proteins for numerous …
β− Arrestins: structure, function, physiology, and pharmacological perspectives
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …
are multifunctional intracellular proteins that regulate the activity of a very large number of …
G-protein–coupled receptors in heart disease
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central
physiological role in the regulation of cardiac function in both health and disease and thus …
physiological role in the regulation of cardiac function in both health and disease and thus …
Biased allosteric modulators: new frontiers in GPCR drug discovery
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
Molecular signatures of G-protein-coupled receptors
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …