Words similar to gpcrs
Example sentences for: gpcrs
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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.
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.
The two Hh-signaling antagonists, KAAD-cyclopamine and Cur61414, have shown decreased potency on Smo act-expressing cells, leading to the speculation that they may bind this mutant form of Smo less well than the wild-type form [ 11 17 ] . We sought to determine whether the Hh agonist binds Smo actwith a higher affinity, an observation seen with certain ligands and constitutively active mutants of GPCRs [ 29 ] . To perform this experiment, we isolated membranes from cells transfected with a cDNA construct encoding a tryptophan-to-leucine mutation at residue 539 (W539L) of murine Smo.
Despite numerous reported differences, it does appear that diverse GPCRs share common mechanistic themes during ERK stimulation, including the tyrosine-phosphorylation of Shc and its complexing with Grb2, mSOS recruitment, the GTP-loading of Ras, and Raf-1 activation leading to MEK-1 phosphorylation [ 1 ] . However, the progression of each of these downstream events after GPCR stimulation depends first on the tyrosine phosphorylation of a membrane-bound protein that will be used as a scaffold, which will bind the other proteins (e.g.
For example the cone rod homeobox (Crx) binds and transactivates the rhodopsin promoter [ 26 ] . However, it has not been determined whether other rhodopsin GPCRs are also regulated by homeobox proteins.
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