[1] The major obstacle for the design of selective inhibitors of PSTPs lies in the similarity of the catalytic pocket, which so far has not allowed the development of selective, high-affinity active-site binders.
After reviewing the article, the curator chose the more specific GO term 'high affinity secondary active ammonium transmembrane transporter activity' (GO 0015398), a child term of GO 0008519.
But according to fluoride speciation, neutral hydrofluoride which has less affinity towards active carbon adsorbents is predominant in the pH at less than 3 (Lagergren 1898), and so, less adsorption is observed at low pH conditions.
Similar study conducted that revealed benzofuran having high affinity for active site of COX-2 receptor showing it to be a good anti-inflammatory compound (Yadav et al. 2014).
In the current work, 55 tyrosine structural analogues on docking with COX-2, COX-1 and hERG revealed that 35 molecules have more affinity at active site residues of COX-2 enzyme and less interaction with the other two proteins (COX-1, hERG) than standard celecoxib.
This in vitro binding data provides an explanation for our finding that isoform 2 has higher affinity for active Rac1 than does isoform 3 (Fig. 4B).
This assay takes advantage of a nucleotide-free single amino acid mutation in RhoA (G17A) that binds with high affinity to active RhoA-specific GEFs [12].
Besides, higher frequencies of smaller Km18 values indicate that the affinity of active Raf to its specific enzyme PP2A is far more stable and stronger, resulting in a much faster Raf inactivation in the transient as compared to the sustained case.
TrkA is the high affinity catalytically active receptor for NGF.
An analogue internal standard might fail to compensate because it might have higher/lower affinity for active sites than the drug of interest.
Inside-out activation of αIIbβ3 integrin was detected using JON/A antibody binding, which only recognizes the high affinity or active conformation of the integrin.
