.beta.-sheet mimetics and use thereof as inhibitors of...

A - Human Necessities – 61 – K

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A61K 38/02 (2006.01) A61K 31/415 (2006.01) A61K 31/50 (2006.01) A61K 31/675 (2006.01) A61K 38/00 (2006.01) A61K 38/04 (2006.01) C07K 5/02 (2006.01)

Patent

CA 2215720

There are disclosed .beta.-sheet mimetics and methods relating to the same for imparting or stabilizing the .beta.-sheet structure of a peptide, protein or molecule. In one aspect, the .beta.-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The .beta.-sheet mimetics have utility as inhibitors of one or more of proteases, kinases, CAAX, peptides binding to SH2 domains and MHC-I and/or MHC-II presentation of peptides to T cell receptors in warm-blooded animals.

La présente invention concerne des mimétiques de feuillets .beta. et des procédés s'y rapportant permettant de communiquer ou stabiliser la structure en feuillets .beta. d'un peptide, d'une protéine ou d'une molécule. Dans l'une des variantes, les mimétiques de feuillets .beta. sont fixés par covalence à l'extrémité du peptide ou de la protéine, ou entre ses extrémités. Ces imitateurs de feuillets .beta. conviennent comme inhibiteurs d'une ou plusieurs protéases, kinases, CAAX, de peptides se liant à des domaines SH2 et de la présentation MHC-I et/ou MHC-II de peptides à des récepteurs de cellules T chez les animaux à sang chaud.

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