P300 histone acetylase inhibitor

Details P300 histone acetylase inhibitor P300 histone acetylase inhibitor

C - Chemistry, Metallurgy

12

N

C12N 15/09 (2006.01) C07K 14/47 (2006.01) C07K 16/18 (2006.01) C12N 15/11 (2006.01) G01N 33/15 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2461094

An inhibitor of p300 histone acetylase is isolated and identified from a human cDNA library. This inhibitor is a nuclear protein consisting of 855 amino acid residues. This inhibitor binds to the cysteine/histidine rich domain of p300 and thus inhibits the transcriptional activation by p300. Moreover, it inhibits the transcriptional activity of p53, which is coactivated by p300, to thereby inhibit the cell cycle arrest depending on p53.

L'invention concerne un inhibiteur de l'histone acétylase de p300 isolé et identifié à partir d'une banque d'ADNc humain. Cet inhibiteur est une protéine nucléaire comprenant 855 résidus d'acide aminé et se liant à un domaine riche en cystéine/histidine de p300 et inhibe, par conséquent, l'activation transcriptionnelle par p300. De plus, l'inhibiteur inhibe l'activité transcriptionnelle de p53 co-activée par p300, inhibant ainsi l'arrêt du cycle cellulaire dépendant de p53.

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