Significats de biased agonism en anglès

Some terms for this phenomenon include functional selectivity, agonist-directed trafficking, and biased agonism.

Binding and signaling kinetics have previously proven important in validation of biased agonism at GPCRs.

This relationship unifies different definitions of efficacy and provides a rational basis for quantifying biased agonism.

Mechanisms behind such biased agonism are largely unknown for RTKs, especially at the level of receptor-ligand complex structure.

We propose that kinetic context must be acknowledged in the design and interpretation of studies of biased agonism.

As such, it is of great importance to gain insight into the SAR of biased agonism at this receptor.

However, the medicinal chemist faces numerous challenges to develop biased ligands, including the detection and quantification of biased agonism.

However, proof that cognate conformations of receptors display structural differences within their binding site where biased agonism initiates, are still lacking.

Ligand-directed signaling, biased agonism, and functional selectivity are terms that describe the propensity of a ligand to drive signaling toward one GPCR pathway over another.

Biased agonism offers an opportunity for the medicinal chemist to discover pathway-selective ligands for GPCRs.

Biased agonism arises when the ligand induces the receptor to engage distinct transduction proteins with different efficacies.

Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets.