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 …

G protein-coupled receptors (GPCRs) are seven transmembrane proteins that form the
largest single family of integral membrane receptors. GPCRs transduce information provided …

Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …

The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century,
yet recent data have revealed that many ligands can differentially activate signaling …

It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …

G protein-coupled receptors (GPCRs) represent the largest family of cell-surface receptors.
These receptors are natural allosteric proteins because agonist-mediated signaling by …

Targeting neuroendocrine tumors expressing somatostatin receptor subtypes (sst) with
radiolabeled somatostatin agonists is an established diagnostic and therapeutic approach in …

It is becoming increasingly clear that signaling via G protein-coupled receptors is a diverse
phenomenon involving receptor interaction with a variety of signaling partners. Despite this …

Cholecystokinin and gastrin receptors (CCK1R and CCK2R) are G protein-coupled
receptors that have been the subject of intensive research in the last 10 years with …

The efficacy of a drug is generally determined by the drug's ability to promote a quantifiable
biological response. In the context of the classical receptor-occupancy theory, the efficacy is …