Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors

Name: Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors
Uploaded: 1994-01-01
Description: A series of non-macrocyclic pipecolyl α-ketoamides were prepared and evaluated as FKBP cis-trans peptidyl-prolyl isomerase inhibitors. These compounds exhibited inhibition constants as low as 2 nM. Their design was based on a consideration of the common FKBP-binding elements of FK506 and rapamycin. Structure-activity relationships are discussed.
Dennis A. Holt; Arda Konialian-Beck; Hye-Ja Oh; Hwa-Kwo Yen; Leonard W. Rozamus; Arnold J. Krog; Karl F. Erhard; Elizabeth Ortiz; Mark A. Levy; Martín Brandt; Mary J. Bossard; Juan I. Luengo
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