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 …
Biased ligands at G-protein-coupled receptors: promise and progress
JD Violin, AL Crombie, DG Soergel, MW Lark - Trends in pharmacological …, 2014 - cell.com
Drug discovery targeting G protein-coupled receptors (GPCRs) is no longer limited to
seeking agonists or antagonists to stimulate or block cellular responses associated with a …
seeking agonists or antagonists to stimulate or block cellular responses associated with a …
Bias factor and therapeutic window correlate to predict safer opioid analgesics
Biased agonism has been proposed as a means to separate desirable and adverse drug
responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe …
responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe …
The role of kinetic context in apparent biased agonism at GPCRs
Biased agonism describes the ability of ligands to stabilize different conformations of a
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway …
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway …
Combinatorial expression of GPCR isoforms affects signalling and drug responses
G-protein-coupled receptors (GPCRs) are membrane proteins that modulate physiology
across human tissues in response to extracellular signals. GPCR-mediated signalling can …
across human tissues in response to extracellular signals. GPCR-mediated signalling can …
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 …
Biased agonism: An emerging paradigm in GPCR drug discovery
G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors …
cellular proteins. The members of this large receptor gene family couple to primary effectors …
Synthesis, chemical characterization, and μ-opioid receptor activity assessment of the emerging group of “nitazene” 2-benzylbenzimidazole synthetic opioids
MM Vandeputte, K Van Uytfanghe… - ACS chemical …, 2021 - ACS Publications
Several 2-benzylbenzimidazole opioids (also referred to as “nitazenes”) recently emerged
on the illicit market. The most frequently encountered member, isotonitazene, has been …
on the illicit market. The most frequently encountered member, isotonitazene, has been …
Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors
Members of the heterotrimeric guanine nucleotide–binding protein (G protein)–coupled
receptor (GPCR) family play key roles in many physiological functions and are extensively …
receptor (GPCR) family play key roles in many physiological functions and are extensively …
Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential
G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …
G proteins. Originally, an individual GPCR was thought to signal through one G protein …