Author/Authors :
Bruce A. Lefker، نويسنده , , William A. Hada، نويسنده , , Ann S. Wright، نويسنده , , William H. Martin، نويسنده , , Ingrid A. Stock، نويسنده , , Gayle K. Schulte، نويسنده , , Jay Pandit، نويسنده , , Dennis E. Danley، نويسنده , , Mark J. Ammirati، نويسنده , , Scott F. Sneddon، نويسنده ,
Abstract :
Structural information from a complex of a tetrapeptide renin inhibitor, CP-85, 339, with human renin, led to the design of inhibitors with extended P1 groups that span the S1-S3 active site pocket. A m-biphenyl sidechain at P1 and glycine at P3 led to a 160X increase in potency over the analogous phenyl compound. A crystal structure of this compound in complex with recombinant human renin (rHR) was solved.
