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Here, the three most promising candidates: R28K, R201A and R201K and an additional one previously described in literature, K27A, were compared with the wild-type protein for binding activity and affinity to target cells and serum stability of the protein.
Mutants of CXCR4 lacking N-glycosylation sites g1 and/or g2, which were expressed by insect cells, exhibited a decreased binding activity and affinity for the natural CXCR4 ligand SDF-1α [ 21].
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Free energy value is an important parameter for evaluation of docking affinity, binding activity and stability of receptor and ligand, and it can be used to judge the interaction of ligand and receptor.
In addition to LigBCen2R, other variable regions of Ig-like domains of LigA and LigB were also found to possess GBD binding activity but with different binding affinity.
The data are consistent with an independent acquisition of high affinity ankyrin binding activity for the anion exchanger and Na+K-ATPase proteins through a convergent evolutionary process.
A number of variants with enhanced catalytic activity and binding affinity were obtained.
The C3=O/D angle of the ligands was correlated with both Na+-retaining activity and binding affinity for the mineralocorticoid receptor.
Highly predictive 3D-QSAR models, with Pearson-R values of 0.86 and 0.90, were obtained for the transactivation activity and binding affinity of PPARγ, respectively.
However, Drosocin containing either L or D enantiomeric sugar, displayed antimicrobial activity and binding affinity to bacterial heat shock protein, DnaK.
This peptide was shown to possess increased in vitro serum stability compared to native H2 relaxin whilst retaining relaxin-like binding affinity, activity, and structural integrity in vitro.
This approach allows comparative studies of drug binding affinity, activity and delivery and may serve as a first-line tool for evaluation of new vitamin D3 analogues and as a transgenic marker for drug delivery in sensor-transgenic animals.
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