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US 2001/0041337 A1Published application
Specific inhibitors of DNA methyltransferase
OwnerMoshe Szyf, Pascal Bigeyinventors
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Abstract
The invention provides novel mechanism-based inhibitors of DNA methyltransferase enzyme, and diagnostic and therapeutic uses for the same. The novel inhibitors according to the invention form stable, noncovalent complexes with DNA methyltransferase enzyme in a manner which is independent of S-adenosylmethionine.
Claims10
An inhibitor of DNA methytransferase enzyme having the general structure:
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- wherein each N is independently any nucleotide, n is a number from 0-20, C is 5-methylcytidine, G is guanidine, y is a number from 0-20, L is a linker, each D is a nucleotide that is complementary to an N such that Watson-Crick base pairing takes place between that D and the N such that the Nn—C—G—Ny and the Dn—G—B—Dy form a double helix, B is cytosine, inosine, uridine, 5-bromocytosine or 5-fluorocytosine, orabasic deoxyribose, the linkage between B and G is a phosphorothioate or phosphorodithioate linkage, dotted lines between nucleotides represent hydrogen bonding between the nucleotides, and the total number of nucleotides ranges from about 10 to about 50.
An inhibitor of DNA methytransferase enzyme having the general structure
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- wherein each N is independently any nucleotide, n is a number from 0-20, C is 5-methylcytidine, G is guanidine, y is a number from 0-20, L is a linker, each D is a nucleotide that is complementary to an N such that Watson-Crick base pairing takes place between that D and the N such that the Nn—C—G—Ny and the Dn—G—B—Dy form a double helix, B is cytosine, inosine, uridine, 5-bromocytosine, abasic deoxyribose, or 5-fluorocytosine, dotted lines between nucleotides represent hydrogen bonding between the nucleotides, B and G are linked by a phosphorothioate or phosphorodithioate linkage and the total number of nucleotides ranges from about 10 to about 50, X is an antisense oligonucleotide of from about 10 to about 50 nucleotides in length, which is complementary to a portion of an RNA encoding DNA MTase enzyme, and L can optionally be X.
Dependencies are inferred from the claim text.