Chemistry: molecular biology and microbiology – Enzyme – proenzyme; compositions thereof; process for... – Transferase other than ribonuclease
Patent
1995-06-07
1997-02-25
Wax, Robert A.
Chemistry: molecular biology and microbiology
Enzyme , proenzyme; compositions thereof; process for...
Transferase other than ribonuclease
435 697, 530324, 530350, C12N 912, C12P 2104, A61K 3800, C07K 100
Patent
active
056058250
ABSTRACT:
A novel human 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 racl 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.
REFERENCES:
Knaus et al. (1995) Science 269: 221-223.
Leberer et al. (1992) EMBO J. 11(13): 4815-4824.
Manser et al. (1992) J. Biol. Chem. 267(23): 16025-16028.
Manser et al. (1995) Nature 367: 40-46.
Abo Arie
Martin George A.
Hobbs Lisa J.
ONYX Pharmaceuticals, Inc.
Wax Robert A.
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