Enzyme inhibitors and methods therefor
AssigneeVDF Futureceuticals, Inc.
InventorsDusan Miljkovic, Pietrzkowski Zbigniew
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Abstract
An enzyme is inhibited by presenting the enzyme with a boron containing structure having a tetrahedral boron atom covalently bound to four ligands. Particularly preferred enzymes include prostaglandin endoperoxide synthase (COX-1 and COX-2), and particularly preferred structures include a ligand that confers at least 80-fold selectivity of COX-2 inhibition over COX-1 inhibition. Consequently, further methods are directed towards induction of apoptosis in a cell and methods of reducing pain.
Claims27
A method of inhibiting an enzyme, comprising presenting the enzyme with a boron containing structure having a tetrahedral boron atom covalently bound to four ligands at a concentration effective to inhibit the enzyme.
A method of inducing apoptosis in a cell, comprising presenting the cell with a boron containing structure having a tetrahedral boron atom covalently bound to four ligands at a concentration effective to induce apoptosis.
A method of reducing pain in a patient, comprising administering to patient a boron containing structure having a tetrahedral boron atom covalently bound to four ligands at a dosage effective to reduce pain.
A method of reducing inflammation in a patient, comprising administering to the patient a composition comprising a boron containing structure having a tetrahedral boron atom covalently bound to four ligands at a concentration effective to inhibit the enzyme.
The use of a composition comprising a boron containing structure having a tetrahedral boron atom covalently bound to four ligands in the manufacture of a medicament to treat an inflammation.
Dependencies are inferred from the claim text.