Cancer inhibitory peptides

Details Cancer inhibitory peptides Cancer inhibitory peptides

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01) C07K 5/027 (2006.01)

Patent

CA 2203694

The sea hare Dolabella auricularia has yielded many structurally distinct peptides which possess antineoplastic activity. Presently the compound denominated "dolastatin 10" represents the most important of such peptides because of its demonstrated potential as an anticancer drug. The present invention relates to the systematic creation of seven unique pentapeptides by selectively coupling a tripeptide-trifluoroacetate salt with a preselected dipeptide trifluoroacetate salt which provide active molecules capable of emulating the measured therapeutic effect of dolastatin 10.

Le lièvre de mer, Dolabella auricularia, a déjà produit de nombreux peptides distincts du point de vue structural doués d'une activité antinéoplasique. Dans le cadre de cette invention, le composé appelé "dolastatine 10" apparaît comme le plus significatif de ces peptides en raison de son potentiel avéré comme médicament anticancéreux. La présente invention a trait à l'élaboration systématique de sept pentapeptides uniques, obtenus par couplage sélectif d'un sel de tripeptide-trifluoroacétate avec un sel de dipeptide trifluoroacétate sélectionné à l'avance, qui fournissent des molécules actives capables d'émuler l'effet thérapeutique mesuré de la dolastatine 10.

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