Cyclic GMP dependent protien kinase as a chemotherapeutic target for antiprotozoal agents
AssigneeMerck & Co., Inc.
InventorsAnne Gurnett, Robert Donald, Georgianna Harris, Paul A. Liberator, Dennis Schmatz, Sandra J. Rattray
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Abstract
Protozoal cyclic GMP dependent protein kinases have been isolated and cloned. These enzymes may be used in screening assays to identify potential antiprotozoal agents.
Claims15
A cGMP dependent protein kinase of a protozoan.
A cGMP dependent protein kinase of a protozoan of the family Apicomplexan.
A cGMP dependent protein kinase of an Eimeria species.
A cGMP dependent protein kinase of Einieria tenellla.
A cGMP dependent protein kinase of Toxoplasma gondii.
A polynucleotide encoding a cGMP dependent protein kinase of SEQ ID NO:
- 11.
A polynucleotide having SEQ ID NO:
- 10.
A polynucleotide having SEQ ID NO:
- 12.
A polypeptide having SEQ ID NO:
- 11.
A polypeptide having SEQ ID NO:
- 13.
A method for identifying compounds having antiprotozoal activity comprising:
- (a) contacting protozoal PKG with (i) a known amount of a labeled compound that interacts with a PKG and (ii) a known dilution of a test compound or a natural product extract;
- and
- (b) quantitating the percent inhibition of interaction of said labeled compound induced by said test compound.
A polynucleotide encoding a cGMP dependent protein kinase of SEQ ID NO:
- 13.
method for identifying compounds having antiprotozoal activity comprises:
- (a) contacting an intact host or protozoal cell with a test compound or a natural product extract;
- (b) disrupting said cell to obtain a biochemical fraction possessing PKG catalytic activity;
- and
- (c) determining the level of PKG activity in said biochemical fraction.
Dependencies are inferred from the claim text.