PEPTIDES

• Main Authors: CHAN, WENG, C, ATKINSON, GAIL, E, ZHELEVA, DANIELLA, I, MCINNES, CAMPBELL, ANDREWS, MARTIN, J., I, FISCHER, PETER, M
• Format: Patent
• Language: English; French
• Published: 06.05.2005
• Edition: 7
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; TESTING

The present invention relates to p2l derived peptides capable of inhibiting CDK/cyclin complexes, particularly cyclins A or E/CDK2, by modifying the interaction with their substrates. The peptides are derived from a C-terminal region of p2l. and display selectivity for cyclin/CDK2 inhibition over cyclin/CDK4 inhibition. Variants of such peptides particularly involving certain alanine replacements are shown to be particularly potent. L'invention concerne des peptides dérivés de p21, capables d'inhiber des complexes CDK/cycline, en particulier les cyclines A ou E/CDK2, par la modification de l'interaction avec leurs substrats. Ces peptides, qui sont dérivés d'une zone terminale C de p21, présentent une sélectivité d'inhibition de la cycline/CDK2 supérieure à l'inhibition de la cycline/CDK4. Des variantes de ces peptides comprenant notamment certaines substitutions d'alanine se sont avérées particulièrement efficaces.