Substrates and inhibitors for cysteine protease ich-1

Details Substrates and inhibitors for cysteine protease ich-1 Substrates and inhibitors for cysteine protease ich-1

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 38/07 (2006.01) A61K 38/08 (2006.01) C07K 5/103 (2006.01) C07K 5/113 (2006.01) C07K 14/81 (2006.01) C12N 9/64 (2006.01) C12N 9/99 (2006.01) C12Q 1/37 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2243497

Substrates and inhibitors for the cysteine protease Ich-1 are disclosed. These compounds are designed based on an optimal minimal substrate for Ich-1 and include reversible inhibitors, irreversible inhibitors, selectively reversible inhibitors, chromogenic substrates, fluorogenic substrates and radiolabeled substrates/inhibitors. Pharmaceutical compositions comprising the compounds of the invention are also provided. Methods for inhibiting the proteolytic activity of Ich-1, methods for detecting the presence of Ich-1 and methods for isolating Ich-1 using the compounds of the invention are also disclosed.

L'invention concerne des substrats et des inhibiteurs de la cystéine protéase Ich-1. Ces composés sont basés sur un substrat minimum optimal pour Ich-1 et englobent des inhibiteurs réversibles, des inhibiteurs irréversibles, des inhibiteurs sélectivement réversibles, des substrats chromogènes, des substrats fluorogènes et des substrats/inhibiteurs portant un marqueur radioactif. L'invention concerne également des compositions pharmaceutiques comprenant des composés de l'invention, ainsi que des méthodes pour bloquer l'activité protéolytique d'Ich-1, des méthodes pour détecter la présence d'Ich-1 et des méthodes pour isoler Ich-1, en utilisant les composés de l'invention.

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