Isozyme-specific antagonists of protein kinase c

Details Isozyme-specific antagonists of protein kinase c Isozyme-specific antagonists of protein kinase c

C - Chemistry, Metallurgy

07

K

C07K 7/00 (2006.01) C07K 14/705 (2006.01) C12N 9/12 (2006.01)

Patent

CA 2549052

A method of changing or otherwise converting the biological activity of a PKC peptide agonist to a peptide antagonist is described. The method involves substituting one or more amino acid residues so as to effect a change in charge in the peptide and/or to otherwise make the sequence similar to a sequence derived from the PKC binding site on the RACK protein for the respective PKC enzyme. Methods of inhibiting the activity of a PKC enzyme, and various peptide antagonists of .epsilon.PKC are also disclosed.

Cette invention se rapporte à un procédé servant à modifier ou, sinon, à convertir l'activité biologique d'un agoniste peptidique de la protéine-kinase C (PKC) en un antagoniste peptidique. Ce procédé consiste à substituer un ou plusieurs résidus d'acide aminé pour réaliser une modification dans le peptide et/ou, sinon, pour rendre la séquence similaire à une séquence dérivée du site de liaison de PKC sur la protéine RACK pour l'enzyme PKC respective. Des procédés servant à inhiber l'activité d'une enzyme PKC et divers antagonistes peptidiques de l'enzyme .epsilon.PKC sont également décrits.

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