Peptide antiestrogen compositions and methods for treating...

A - Human Necessities – 61 – K

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A61K 38/08 (2006.01) A61K 38/16 (2006.01) C07K 1/10 (2006.01) C07K 14/705 (2006.01) A61K 38/00 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2286877

Disclosed are methods and compositions comprising native, site-specifically mutagenized, and synthetic peptides comprising portions of the human estrogen receptor, or estrogen receptor co-activator, and nucleic acid compositions encoding these polypeptide compositions. Also disclosed are methods for synthesizing phosphotyrosyl and malonyltyrosyl peptide derivatives and their use as antiestrogen compositions in the treatment of breast cancers, the preparation of pharmaceutical compositions, diagnostic kits, and the development of related assays for use in antitumor therapies.

L'invention concerne des procédés et des compositions renfermant des peptides synthétiques, à l'état naturel, et à mutagénèse dirigée, comprenant des parties du récepteur des oestrogènes humain, ou du co-activateur du récepteur des oestrogènes, ainsi que des compositions d'acides nucléiques codant ces compositions peptidiques. L'invention concerne également des procédés de synthétisation des dérivés peptidiques de phosphotyrosyle et de malonyltyrosyle, ainsi que leur utilisation en tant que compositions antioestrogéniques dans le traitement du cancer du sein, dans la préparation de compositions pharmaceutiques, dans des kits de diagnostic, et dans le développement d'analyses destinées à être utilisées dans des thérapies antitumorales.

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