Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In our database we have the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors.
Source: Use of Epigenetic Drugs in Disease: An Overview, Sarah Heerboth et al.,2016
A poly (ADP-ribose) polymerase type 1 (PARP1) fluorescence imaging agent based on the PARP1 inhibitor olaparib, in which the cyclopropane group of olaparib is replaced by the green fluorescent dye boron-dipyrromethene (BODIPY) fluorophore (FL), with potential fluorescent imaging activity. Upon administration of the fluorescent PARP1 inhibitor PARPi-FL, the olaparib binding moiety specifically targets and binds to PARP1, which is often overexpressed on cancer cells. Upon fluorescent imaging, the PARP1-expressing cancer cells can be visualized. PARP1, the nuclear enzyme that catalyzes post-translational ADP-ribosylation of nuclear proteins, is activated by single-strand (SS) DNA breaks and overexpressed in certain tumor cells; it plays a key role in DNA repair, tumor cell resistance and survival. (Source : NIH-National Cancer Institute, Drug dictionary)
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