Structural analysis of the inhibition of thermolysin by an active-site-directed irreversible inhibitor.

@article{Holmes1983StructuralAO,
  title={Structural analysis of the inhibition of thermolysin by an active-site-directed irreversible inhibitor.},
  author={M. Holmes and D. Tronrud and B. Matthews},
  journal={Biochemistry},
  year={1983},
  volume={22 1},
  pages={
          236-40
        }
}
The mode of binding of the irreversible thermolysin inhibitor ClCH2CO-DL-(N-OH)Leu-OCH3 [Rasnick, D., & Powers, J.C. (1978) Biochemistry 17, 4363-4369] has been determined by X-ray crystallography at a resolution of 2.3 A and the structure of the covalent complex refined to give a crystallographic residual of 17.0%. This is the first such structural study of an active-site-directed covalent complex of a zinc protease. As anticipated by Rasnick and Powers, the inhibitor alkylates Glu-143 in the… Expand
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