Title of article
Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 sidechains
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 ,
Issue Information
روزنامه با شماره پیاپی سال 1995
Pages
4
From page
2623
To page
2626
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1995
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
787756
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