Methods and compositions for bisubstrate inhibitors of acetyltransferases
AssigneeGovernment of the United States of America, Department of Health and Human Services
InventorsDavid C. Klein, M. A.A. Namboodiri, Joan L. Weller, Jeffrey A. Kowalak, Anthony K. Ho
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Abstract
The present invention provides a method of producing a bisubstrate inhibitor in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell. Further provided is a method of inhibiting the activity of an acetyltransferase in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell under conditions whereby a bisubstrate inhibitor will be produced, thereby inhibiting the activity of the acetyltransferase in the cell.
Claims20
A method of producing a bisubstrate inhibitor in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell.
A method of inhibiting the activity of an acetyltransferase in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell under conditions whereby a bisubstrate inhibitor will be produced, thereby inhibiting the activity of the acetyltransferase in the cell.
A method of inhibiting melatonin production in a cell which produces melatonin, comprising introducing into the cell an alkylating derivative of the acetyl acceptor substrate of AANAT which is selected from the group consisting of N-bromoacetyltryptamine, N-bromoacetylserotonin, N-bromoacetylphenylethylamine, N-bromo-acetyl-methoxytryptamine, N-bromoacetyltyramine, N-chloroacetyltryptamine, N-chloroacetylserotonin, N-chloroacetylphenylethylamine, N-chloro-acetyl-methoxytryptamine, N-chloroacetyltyramine, N-fluoroacetyltryptamine, N-fluoroacetylserotonin, N-fluoroacetylphenylethylamine, N-fluoro-acetyl-methoxytryptamine and N-fluoroacetyltyramine.
A method of increasing the amount of serotonin in a cell which produces serotonin, comprising introducing into the cell an alkylating derivative of the acetyl acceptor substrate of AANAT which is selected from the group consisting of N-bromoacetyltryptamine, N-bromoacetylserotonin, N-bromoacetylphenylethylamine, N-bromo-acetyl-methoxytryptamine, N-bromoacetyltyramine, N-chloroacetyltryptamine, N-chloroacetylserotonin, N-chloroacetylphenylethylamine, N-chloro-acetyl-methoxytryptamine, N-chloroacetyltyramine, N-fluoroacetyltryptamine, N-fluoroacetylserotonin, N-fluoroacetylphenylethylamine, N-fluoro-acetyl-methoxytryptamine and N-fluoroacetyltyramine.
A method of treating a subject for a disorder caused by a decreased amount of serotonin, comprising administering to the subject an alkylating derivative of the acetyl acceptor substrate of AANAT which is selected from the group consisting of N-bromoacetyltryptamine, N-bromoacetylserotonin, N-bromoacetylphenylethylamine, N-bromo-acetyl-methoxytryptamine, N-bromoacetyltyramine, N-chloroacetyltryptamine, N-chloroacetylserotonin, N-chloroacetylphenylethylamine, N-chloro-acetyl-methoxytryptamine, N-chloroacetyltyramine, N-fluoroacetyltryptamine, N-fluoroacetylserotonin, N-fluoroacetylphenylethylamine, N-fluoro-acetyl-methoxytryptamine and N-fluoroacetyltyramine.
A cell comprising a bisubstrate inhibitor, wherein the bisubstrate inhibitor comprises an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell and CoA.
Dependencies are inferred from the claim text.