Significats de orthosteric en anglès

These compounds were confirmed to be potent and selective orthosteric FFA2 agonists.

It may be that many active and orthosteric sites can recognize topologically unrelated ligands.

The structure reveals an interesting N-terminus that could co-occupy the enlarged orthosteric binding site together with elagolix.

BMS-681 inhibits chemokine binding by occupying the orthosteric pocket of the receptor in a previously unseen binding mode.

Binding of 15 to the receptor cooperatively enhances orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists.

These results should facilitate the design of new therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family.

Mutations within the orthosteric binding site caused similar reductions in affinity and signaling efficacy for both selective and prototypical orthosteric ligands.

Mutation of amino acid residues that form the orthosteric binding pocket caused a loss of carbachol response that could be rescued by BQCA.

However, targeting the largely unexplored and evolutionarily unique allosteric sites has potential for developing more specific drugs with fewer side effects than orthosteric ligands.

Because allosteric modulation can vary depending on the orthosteric ligand it is important to study their function in a system that employs endogenous cannabinoids.

Our data show that both orthosteric and allosteric activation of a7 nAChR require cooperative activity at the interface between the subunits in the extracellular domain.

We also report the structure of the M2 receptor simultaneously bound to the orthosteric agonist iperoxo and the positive allosteric modulator LY2119620.

Our results suggest that the 3,4-methylenedioxyamphetamine analogs bind at the monoamine transporter orthosteric binding site by adopting one of two mutually exclusive binding modes.

These compounds were confirmed to be potent and selective orthosteric FFA2 agonists.

It may be that many active and orthosteric sites can recognize topologically unrelated ligands.

The structure reveals an interesting N-terminus that could co-occupy the enlarged orthosteric binding site together with elagolix.