Peptidomimetic inhibitors of stat3 activity and their...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/06 (2006.01) A61K 38/05 (2006.01) A61P 35/00 (2006.01) C07K 5/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2516685

The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include dipeptides of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position and L=Leu, Val, Ala or a non-polar amino acid. R is preferably aryl or heteroaryl, eventually substituted with halogens, amino and nitro groups. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.

L'invention concerne des compositions et des procédés permettant de bloquer la croissance ou prolifération des cellules cancéreuses et/ou d'induire la mort des cellules cancéreuses. Les compositions selon l'invention sont des peptidomimétiques inhibant la fonction de STAT. Les peptidomimétiques selon l'invention comprennent des composés de formule RY*L (dans laquelle Y* représente la phosphotyrosine), le groupe R étant au niveau de la position Y-1. Les peptidomimétiques selon l'invention interrompent l'activation et la fonction de Stat3, inhibent de manière importante la croissance des cellules tumorales et induisent la mort des cellules tumorales.

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