Method of treating cancer
OwnerStanley F Barnett, Deborah DeFeo-Jones +3inventors
InventorsStanley F Barnett, Deborah DeFeo-Jones, Kathleen M Haskell, Hans E Huber, Deborah D Nahas
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Abstract
The present invention is directed to a method of treating cancer which comprises administration of a compound which selectively inhibits the activity of one or two of the isoforms of Akt, a serine/threonine protein kinase. The invention is particularly directed to the method wherein the compound is dependent on the presence of the plestrin homology domain of Akt for its inhibitory activity.
Claims34
A method for treating cancer in a mammal in need thereof which comprises administering to said mammal amounts of a selective inhibitor of the activity of one or more of the isoforms of Akt.
A method for treating cancer in a mammal in need thereof which comprises administering to said mammal amounts of an inhibitor of the activity of one or more of the isoforms of Akt wherein the inhibition by the inhibitor is dependent on the presence of the pleckstrin homology domain of the isoforms of Akt.
A method for treating cancer in a mammal in need thereof which comprises administering to said mammal amounts of an inhibitor of the activity of one or more of the isoforms of Akt wherein the inhibition by the inhibitor is dependent on the presence of the hinge region of the isoforms of Akt.
A method for treating cancer in a mammal in need thereof which comprises administering to said mammal amounts of an inhibitor of the activity of one or more of the isoforms of Akt wherein the inhibition by the inhibitor is dependent on the presence of the pleckstrin homology domain and the hinge region of the isoforms of Akt.
A method for identifying a compound that is a selective inhibitor of one, two or three of the Akt isoforms, whose inhibitory efficacy is dependent on the pleckstrin homology domain, that comprises the steps of:
- a) determining the efficacy of a test compound in inhibiting the activity of an Akt isoform;
- b) determining the efficacy of the test compound in inhibiting the activity of the Akt isoform that has been modified to delete the pleckstrin homology domain;
- and
- c) comparing the activity of the test compound against the Akt isoform with the activity of the test compound against the modified Akt isoform lacking the pleckstrin homology domain.
A method for identifying a compound that is a selective inhibitor of one, two or three of the Akt isoforms, whose inhibitory efficacy is dependent on the hinge region of Akt, that comprises the steps of:
- a) determining the efficacy of a test compound in inhibiting the activity of an Akt isoform;
- b) determining the efficacy of the test compound in inhibiting the activity of the Akt isoform that has been modified to delete the pleckstrin homology domain;
- c) determining the efficacy of the test compound in inhibiting the activity of the Akt isoform that has been modified to delete the pleckstrin homology domain and the hinge region;
- and
- d) comparing the activity of the test compound against the Akt isoform, the activity of the test compound against the modified Akt isoform lacking the PH domain, and the activity of the test compound against the modified Akt isoform lacking the pleckstrin homology domain and the hinge region.
A modified Akt isoform lacking only the pleckstrin homology domain.
A modified Akt isoform lacking only the hinge region.
A modified Akt isoform lacking the full pleckstrin homology domain and the full hinge region.
Dependencies are inferred from the claim text.