Chemistry: molecular biology and microbiology – Enzyme – proenzyme; compositions thereof; process for... – Transferase other than ribonuclease
Patent
1995-01-06
1996-05-21
Wax, Robert A.
Chemistry: molecular biology and microbiology
Enzyme , proenzyme; compositions thereof; process for...
Transferase other than ribonuclease
435 691, 4352523, 4353201, 536 232, C12N 912, C12N 120, C12P 2106, C07H 2104
Patent
active
055189113
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 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.
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. (1994) Nature 367: 40-46.
Abo Arie
Martin George A.
Giotta Greg
Hobbs Lisa J.
Mendlein John D.
ONYX Pharmaceuticals, Inc.
Torchia Timothy E.
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