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The present invention provides the compound having the formula: ##STR00001## wherein each of R.sub.1 and R.sub.2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, --O--, --S--, --NH--, or --CH.sub.2--; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apopt...
The present invention discloses compositions and methods for enhancing the expression of major histocompatability complex (MHC) and costimulatory antigens on tumor cells. The method comprises exposing the tumor cells to inhibitors of histone deacetylation.
The present invention provides the compound having the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, --O--, --S--, --NH--, or --CH.sub.2 --; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosi...
Disclosed herein are carbonyl compounds of Formula I as described herein. ##STR00001## Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the ...
Methods of identifying agents which alter the NAD-dependent acetylation status and mono-ADP-ribosylation of nuclear proteins are disclosed. The methods further include identifying agents which alter the life span or aging of a cell or an organism by determining the level of NAD-dependent acetylation and/or ADP ribosylation of a nuclear protein. The invention also relates to a mammalian Sir2 protein which acetylates or deacetylates nuclear proteins in a NAD-dependent manner and has mono-ADP-ribos...
The present invention provides polypeptides with histone H3 lysine 79 methyltransferase activity as well as nucleic acids encoding the same. Also provided are methods of using the polypeptides and nucleic acids of the invention in screening assays to identify compounds of interest. Further provided are diagnostic methods for leukemia and prognostic methods to predict the course of the disease in a subject.
In this patent we describe the purification of prenylated benzophenones from the fruit rinds of Garcinia species and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC.sub.50-1 .mu.M) and pCAF (IC.sub.50-15 .mu.M). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. Th...
The present invention provides a reconstituted complex including EED, EZH2 and SUZ12 wherein the reconstituted complex has histone methyltransferase (HMTase) activity for lysine 27 of histone H3 (H3-K27). The reconstituted complex may further include RbAp48, AEBP2 or both. Also disclosed are methods of producing the reconstituted complex, methods of identifying compounds that inhibit the HTMase activity of the reconstituted complex and methods of identifying candidate compounds for treating canc...
The present invention provides the compound having the formula: ##STR00001## wherein each of R.sub.1 and R.sub.2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, --O--, --S--, --NH--, or --CH.sub.2--; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apopt...
The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis. ##STR00001##
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