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AssigneeThe Regents of the University of California
InventorsNorbert O. Reich, James Flynn
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A synthetic oligonucleotide comprising a C-5 methylcytosine and which recognizes and binds an allosteric site on DNA methyltransferase thereby inhibiting DNA methyltransferase activity is disclosed. Also disclosed is a composition comprising a synthetic oligonucleotide of the invention. The composition is useful for inhibiting DNA methyltransferase activity, thereby inhibiting the methylation of DNA. The composition can be a pharmaceutical composition useful for treating disorders associated with methylation defects, such as cancer and certain developmental disorders. Also disclosed is a method of inhibiting methylation of DNA. The method involves contacting a DCMTase with a synthetic oligonucleotide of the invention in the presence of the DNA, thereby resulting in an enzyme/synthetic oligonucleotide complex. The presence of the complex prevents catalysis, thereby inhibiting DNA methyltransferase activity. Also disclosed is a method of treating a disorder of cell proliferation or development by administering to a subject a synthetic oligonucleotide of the invention. The inhibition of DNA methyltransferase prevents the methylation of DNA thereby treating the disorder of cell proliferation or development.
A synthetic oligonucleotide comprising a C-5 methylcytosine and which recognizes and binds an allosteric site on DNA cytosine methyltransferase (DCMTase) thereby modulating DCMTase activity associated with the allosteric site.
A method of inhibiting methylation of DNA comprising contacting a DCMTase with a synthetic inhibitor molecule so as to form an enzyme/synthetic inhibitor molecule complex in the presence of the DNA, wherein the synthetic inhibitor molecule comprises a C-5 methylcytosine which recognizes and binds an allosteric site on DCMTase, thereby inhibiting DNA methyltransferase activity.
A method of inhibiting proliferation of cancer cells comprising administering to a subject a synthetic inhibitor molecule which recognizes and binds an allosteric site on DCMTase thereby resulting in an enzyme/synthetic inhibitor molecule complex, the presence of the complex inhibiting DCMTase-mediated methylation of DNA, thereby inhibiting proliferation of the cancer cells.
A method of identifying a molecule which recognizes and binds an allosteric site on DCMTase comprising:
Dependencies are inferred from the claim text.