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We found that since vemurafenib binds to the drug binding site of human ABCG2 with relatively high affinity, it effectively inhibited ABCG2-mediated transport of other drug substrates.
Steady-state kinetic data showed that, at high concentrations, tryptophan can bind to the inhibitory substrate binding site of human IDO in addition to the active site, thereby accounting for the substrate inhibition behaviour of the enzyme [50].
Nuclear proteins from 2008 ovarian cancer cell line treated with TNF-α were able to shift (bind) oligonucleotide sequences containing the predicted NF-κB binding site of human PIK3CA promoter, but were not able to shift either mutant or mock oligonucleotide sequences (Figure 8 D).
Pantophlet, R. et al. Fine mapping of the interaction of neutralizing and nonneutralizing monoclonal antibodies with the CD4 binding site of human immunodeficiency virus type 1 gp120.
Chaudhary, A. et al. Probing the phosphoinositide 4,5-bisphosphate binding site of human profilin I. Chem Biol 5, 273 281 (1998).
In the previous work, we reported compounds I and II as novel topoisomerase IIα catalytic inhibitors targeting for ATP binding site of human topoisomerase IIα ATP-binding domain.
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Previously, we have shown that amino-acid sequence changes in the antigen binding sites of human monoclonal aPL are important in determining their ability to bind procoagulant and anticoagulant/fibrinolytic SP, with binding to Thr predicting pathogenicity in mice [ 14].
Aoki, D., Appert, H. E., Johnson, D., Wong, S. S. & Fukuda, M. N. Analysis of the substrate binding sites of human galactosyltransferase by protein engineering.
This study was undertaken to synthesize peptides that are partially similar to the binding sites of human olfactory receptor protein.
An X-ray crystallographic study revealed that 8l bound at AMP binding sites of human liver FBPase with hydrogen bonding interactions similar to AMP.
Molecular dockings of synthesized compounds into the binding sites of human pancreatic α-amylase, intestinal maltase-glucoamylase and neuronal α-butrylcholinesterase allowed to shed light on the affinity and binding mode of these novel inhibitors.
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