Exact(1)
15, 16 However, recent in vitro and in vivo studies have shown that sunitinib can only effectively inhibit imatinib-resistant KIT mutants containing primary mutations in exon 9 or secondary mutations in the drug/ATP binding pocket (encoded by exons 13 and 14), but not those harboring secondary mutations in the activation loop (encoded by exon 17).
Similar(59)
Heinrich and co-workers showed that secondary point mutations located in the ATP-binding pocket of the KIT receptor (encoded by exons 13 and 14) are associated with resistance to imatinib, a KIT receptor tyrosine kinase inhibitor, in gastrointestinal stromal tumors (GISTs) [ 27].
EGF encodes a mitogenic factor that acts by binding to the EGFR, encoded by EGFR.
Three amino acid substitutions (Asn89His, Gln153Glu, and Leu205Arg), two of them are near the active site and substrate binding pocket, were identified by sequencing the genes encoding this evolved enzyme.
They are located in and near the binding pocket facilitated by crystal packing effects.
These drastic changes in measured TIF likely occur from slight changes in the binding pocket caused by different co-binding peptides P1, P2, and P3.
Especially, we observe a potential substrate binding pocket surrounded by hydrophobic residues upon NADPH binding and present evidences that this pocket is essential for BdcA binding NADPH and exerting its biological functions.
(B ) The binding pocket formed by hydrophobic residues (orange) that accommodate the crotonyl lysine.
Evolution of substrate and product specificities in these orthologous enzymes may involve keyhole surgery of binding pocket residues by Nature.
This short, modified helix results in an open binding pocket formed by the four-stranded β-sheet.
The deleted sequence comprises half of the active site binding pocket, identified by the citrate molecule shown in red.
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