Characterization of domain-selective inhibitor binding in angiotensin-converting enzyme using a novel derivative of lisinopril.

  title={Characterization of domain-selective inhibitor binding in angiotensin-converting enzyme using a novel derivative of lisinopril.},
  author={Jean M. Watermeyer and Wendy L. Kr{\"o}ger and Hester G. O’Neill and Bryan Trevor Sewell and Edward D. Sturrock},
  journal={The Biochemical journal},
  volume={428 1},
Human ACE (angiotensin-converting enzyme) (EC is an important drug target because of its role in the regulation of blood pressure via the renin-angiotensin-aldosterone system. Somatic ACE comprises two homologous domains, the differing substrate preferences of which present a new avenue for domain-selective inhibitor design. We have co-crystallized lisW-S, a C-domain-selective derivative of the drug lisinopril, with human testis ACE and determined a structure using X-ray… 

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