Inhibitors of phosphoserine and phosphothreonine-proline-specific isomerases

US6462173B1 · kind B1 · utility

Assignees

• Max-Planck-Gesellschaft zur Föderung der Wissenschaften e.V. · US
• Beth Israel Deaconess Medical Center, Inc. · US

Inventors

• Kun Ping Lu · Newton, US
• Lewis C. Cantley · Belmont, US
• Michael B. Yaffe · Dedham, US
• Gunter Fischer · Hamburg, DE

Key dates

• Filing date: Dec 11, 1997
• Grant date: Oct 8, 2002
• Expiry date: Dec 11, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Inhibitors of phosphoserine- or posphothreonine-specific peptidyl prolyl isomerases are described. Such inhibitors include molecules that mimic the structure and conformation of the pSer/pThr-Pro peptide moiety of the isomerase substrate when the substrate is bound into the active site of the isomerase. For example, a protein, peptide or peptide mimetic including xSer/ThrY where x is a negatively charged tetra or pentavalent moiety and Y is a Pro or a Pro analog. Methods of inhibiting cell growth and methods of identifying phosphoserine- or phosphothreonine-proline specific peptidyl-prolyl isomerase inhibitors are also included in the invention.