Protein surface-assisted enhancement in the binding affinity of an inhibitor for recombinant human carbonic anhydrase-II.

@article{Banerjee2004ProteinSE,
  title={Protein surface-assisted enhancement in the binding affinity of an inhibitor for recombinant human carbonic anhydrase-II.},
  author={Abir L Banerjee and Michael P. Swanson and Bidhan Ch Roy and Xiao G Jia and Manas K. Haldar and Sanku Mallik and Dharmendra K. Srivastava},
  journal={Journal of the American Chemical Society},
  year={2004},
  volume={126 35},
  pages={
          10875-83
        }
}
We elaborate on a novel strategy for enhancing the binding affinity of an active-site directed inhibitor by attaching a tether group, designed to interact with the surface-exposed histidine residue(s) of enzymes. In this approach, we have utilized the recombinant form of human carbonic anhydrase-II (hCA-II) as the enzyme source and benzenesulfonamide and its derivatives as inhibitors. The steady-state kinetic and the ligand binding data revealed that the attachment of iminodiacetate (IDA)-Cu(2… CONTINUE READING
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