Structure-Activity Relationship of Fluorine-Containing Renin Inhibitory Peptides Based upon the Tertiary Structure of Human Renin

Abstract

The structure-activity relationship of acyl-His-trifluorinated leucinol derivatives as inhibitors of human renal renin is discussed based upon the tertiary structure of human renin, which was deduced from the crystal structure of penicillopepsin by assuming structural similarity. The structural requirements for the inhibitors and possible interactions at the renin binding site are discussed.