Words similar to gpcrs
Example sentences for: gpcrs
How can you use “gpcrs” in a sentence? Here are some example sentences to help you improve your vocabulary:
With the first evidence that GPCRs could signal via the MAPK cascade, many investigators have looked for a common mechanism of activation that could be applied across receptor types.
These results, taken together, suggest that GPCRs and RTKs can act as independent regulators of MAP kinase cascades, although interactions between the two receptor types may exist in certain cases.
In this report, we questioned whether the EGFR acts as a surrogate scaffold during ERK activation through the δ-OR, as it appears to do for several other GPCRs [ 7 ] . To act as a surrogate-binding site for complex formation, the literature states that this protein must first become tyrosine-phosphorylated [ 7 ] . Tyrosine phosphorylation of the EGFR is apparent after agonist stimulation of the α 2 -AR (COS-7), β 2 -AR (COS-7), insulin-like growth factor (IGF-1; COS-7), substance P, and the lysophosphatidic acid receptor (LPAR) [ 7 ] . In addition, each of the aforementioned ligands also increases ERK phosphorylation when the proper receptor is expressed in these cell lines.
To interpret the results of the competition binding studies, we assume that the mutation in Smo act, like those in constitutively activate mutants of other GPCRs [ 29 ] , indirectly influences ligand binding by creating a change in the normal equilibrium between the different conformations of Smo.
As a receptor class, GPCRs are considered excellent drug targets because they are often regulated through interactions with small natural ligands [ 32 33 ] . Specifically, studies of classic GPCRs, such as the β-adrenergic receptors, show that in the absence of endogenous ligand (agonists) these receptors exist in multiple interconvertible conformations that are predominately inactive [ 34 ] . Upon exposure to their natural ligands, however, the active receptor forms are preferentially stabilized, allowing them to readily engage G-protein couplers and to create signaling-competent complexes.
Loading...