Cripto antagonism of activin and tgf-b signaling

A - Human Necessities – 61 – K

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A61K 39/395 (2006.01)

Patent

CA 2539116

Cripto, a developmental oncoprotein, antagonizes activin and TGF-b signaling by forming a complex with activin and TGF-b and their type II receptors. This complex precludes the formation of a functional activin/TGF-b-type II-type I complex, thereby blocking the signaling of activin and TGF-b. Cripto may be generally capable of blocking antiproliferative Smad2/3 signals and provides a novel mechanism of oncogenic action with multiple therapeutic implications. Inhibiting the formation of Cripto and activin/TGF-b complex may enhance antiproliferative effects of activin and TGF-b.

Pour antagoniser l'activine et la signalisation TGF-b, Cripto, qui est une oncoprotéine issue de la recherche, forme un complexe avec l'activine et le TGF-b et leurs récepteurs de type II. Ce complexe interdit la formation d'un complexe fonctionnel entre l'activine et le TGF-b de type II ou de type I, ce qui bloque la signalisation de l'activine et du TGF-b. Cripto, qui peut être généralement capable de bloquer les signaux d'antiprolifération Smad2/3, vient constituer un nouveau mécanisme d'action oncogène aux multiples implications thérapeutiques. En empêchant la formation du complexe entre Cripto et l'activine ou le TGF-b, on est susceptible de renforcer l'action antiproliférante de l'activine et du TGF-b.

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