Helper inducers for differentiation therapy and chemoprevention

Details Helper inducers for differentiation therapy and chemoprevention Helper inducers for differentiation therapy and chemoprevention

1996-10-15

1998-07-21

Krass, Frederick

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514415, 514418, 514419, 514544, 514570, A61K 3119

Patent

active

057836051

ABSTRACT:
Cancer cells are blocked from entering differentiation pathways because of abnormal methylation enzymes, which are responsible for keeping cancer cells in cycling state. Effective differentiation inducers are those capable of acting directly or indirectly to convert abnormal methylation enzymes into normal enzymes, thereby enabling cancer cells to undergo terminal differentiation. Differentiation employing inducer alone often can not reach completion because of the damage created by the inducer. Such damage can be prevented if differentiation is induced in the presence of helper inducers, which are basically inhibitors of the component enzymes of methylation. Thus, differentiation induced in the presence of helper inducers is more likely to reach completion. Therefore, helper inducers are essential components of differentiation therapy, not just merely to potentiate the activity of differentiation inducers. The present inventors discover that alkyl phenylacetamides, alkyl phenylacetate, 2,4-dichlorophenylacetate, and indole acetate are potent helper inducers.

REFERENCES:
patent: 4470970 (1984-09-01), Burzynski
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Chemical Abstracts 111:169028, "Urinary Metabolites of N,N-diethylphenylacetamide", Rao et al., Jan. 1989.
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