Methods and compositions for specific modulation of mcl-1

C - Chemistry – Metallurgy – 07 – K

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C07K 14/47 (2006.01) A61K 38/17 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2746256

A series of stapled BCL-2 family peptide helices were identified as able to target the survival protein MCL-I with high affinity and a subset with unprecedented selectivity. Agents and methods for selective pharmacologic neutralization of MCL-I are provided for drug discovery and therapeutic uses, including use in overcoming the apoptotic resistance of cancer and other diseases associated with impaired cell death.

L'invention concerne une série d'hélices peptidiques agrafées de la famille BCL-2, qui ont été identifiées comme étant capables de cibler la protéine de survie MCL-I avec une grande affinité et un sous-ensemble avec une sélectivité sans précédent. L'invention concerne également des agents et des procédés permettant la neutralisation pharmacologique sélective de MCL-I pour la découverte de médicaments et d'utilisations thérapeutiques, y compris l'utilisation pour surmonter la résistance apoptotique du cancer et d'autres maladies associées à une mort cellulaire altérée.

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