Highlights • Biased MOR ligands discovered using empirical, rational and natural product
approaches. • Biased MOR ligands produce analgesia with fewer side effects in mice and …

The concept of ligand bias at G protein-coupled receptors broadens the possibilities for
agonist activities and provides the opportunity to develop safer, more selective therapeutics. …

Biased G protein-coupled receptor ligands engage subsets of the receptor signals normally
stimulated by unbiased agonists. However, it is unclear whether ligand bias can elicit …

Seven transmembrane receptors (7TMRs), commonly referred to as G protein-coupled
receptors, form a large part of the “druggable” genome. 7TMRs can signal through parallel …

Presenilins are integral membrane protein involved in the production of amyloid β-protein.
Mutations of the presenilin-1 and -2 gene are associated with familial Alzheimer's disease …

Background: Myelosuppression has been observed with several multikinase angiogenesis
inhibitors in clinical studies, although the frequency and severity varies among the different …

The concept of “ligand bias” at G protein coupled receptors has been introduced to describe
ligands which preferentially stimulate one intracellular signaling pathway over another. …

Linopirdine (3,3-bis(4-pyridinylmethyl)-1-phenylindolin-2-one, DUP996) is an extensively
studied representative of a class of cognition enhancing compounds that increase the evoked …

The concept of "biased agonism" arises from the recognition that the ability of an agonist to
induce a receptor-mediated response (ie "efficacy") can differ across the multiple signal …

The Smoothened receptor (Smo) mediates hedgehog (Hh) signaling critical for development,
cell growth, and migration, as well as stem cell maintenance. Aberrant Hh signaling …