Human pak65

Details Human pak65 Human pak65

C - Chemistry, Metallurgy

12

N

C12N 15/54 (2006.01) C07H 21/00 (2006.01) C07K 7/06 (2006.01) C07K 19/00 (2006.01) C12N 9/12 (2006.01) C12P 21/02 (2006.01) C12Q 1/48 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2209426

A novel humain serine protein kinase, human p21-protein activated serine kinase p65 protein referred to as hPAK65, and methods for its preparation and use are provided. Nucleic acids encoding hPAK65 and methods for their use in preparing hPAK65 as well as in preparing and identifying hPAK65 analogs are provided. Methods provided for the use of hPAK65 protein and its protein fragments, such as those that retain at least one hPAK65 activity, that include screening libraries of agents for candidates that modulate hPAK65 activity. Methods are provided to identify agents that modulate the interaction of hPAK65 with rho-like p21 GTPases, particularly rac1 and CDC42Hs binding to hPAK65 and subsequent activation of hPAK65 serine protein kinase activity, that modulate hPAK65 serine protein kinase activity, and that modulate hPAK65 effect on p21 protein GTPase activity. Such modulating agents can provide novel chemotherapeutic agents for treatment of neoplasia, lymphoproliferative conditions, arthritis, inflammation, autoimmune diseases, apoptosis, and the like, that are related to hPAK65 and p21 protein signal transduction pathways.

L'invention concerne une nouvelle sérine protéine kinase humaine, la sérine protéine kinase p65 humaine activée par la protéine p21, dite hPAK65, et ses procédés de préparation et d'utilisation; des acides nucléiques codant la hPAK65 et des procédés permettant de les utiliser pour produire la hPAK65 et pour produire et identifier des analogues de la hPAK65; des procédés permettant d'utiliser la protéine hPAK65 et ses fragments, tels que ceux qui retiennent au moins une activité de la hPAK65, et comprenant le criblage de banques d'agents afin de détecter des candidats modulant l'acitivité de la hPAK65; des procédés d'identification d'agents qui modulent l'interaction de la hPAK65 avec des GTPases p21 du type rho, en particulier rac1 et CDC42H se liant à la hPAK65, et l'activation ultérieure de la sérine protéine kinase hPAK65, et qui modulent également l'activité de la sérine protéine kinase hPAK65 ainsi que l'effet de la hPAK21 sur l'activité GTPase de la protéine p21. De tels agents de modulation permettent d'obtenir des agents chimiothérapeutiques pour le traitement de la néoplasie, des états lymphoprolifératifs, de l'arthrite, des inflammations, des maladies autoimmunes, de l'apoptose et autres, qui sont associés aux voies de transduction de signaux de la hPAK65 et de la protéine p21.

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