Drug intelligence / Profile preview

Zebularine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Intraperitoneal
01

Overview

Zebularine is a chemically stable nucleoside analog of cytidine that acts as a transition state analog inhibitor of cytidine deaminase and an inhibitor of DNA methyltransferase. It forms covalent complexes with DNA methyltransferases (DNMTs), thereby inhibiting their activity, which leads to the demethylation and reactivation of silenced genes, particularly tumor suppressor genes in cancer cells. Zebularine displays anti-tumor properties both in vitro and in vivo, including inhibition of cell proliferation, induction of apoptosis, antiangiogenic effects, and potential for epigenetic therapy in cancer chemoprevention. It has also been shown to potentiate the effects of other epigenetic therapeutics such as vorinostat[1][2][3][5][7].

Other names
1-beta-D-ribofuranosyl-2(1H)-pyrimidinone1-beta-D-ribofuranosylpyrimidin-2(1H)-one4-deoxyuridinepyrimidin-2-one beta-D-ribofuranosidepyrimidin2-one beta-D-ribofuranosidepyrimidin 2-one beta-D-ribofuranosidepyrimidin-2-one beta-ribofuranosidepyrimidin2-one beta-ribofuranosidepyrimidin 2-one beta-ribofuranosidePyrimidin-2-one ribonucleosidePyrimidin2-one ribonucleosidePyrimidin 2-one ribonucleoside
02

Targets

CDA (Cytidine deaminase)DNMT (DNA methyltransferase)

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