A tremendous research on Poly (ADP-ribose) polymerase (PARP) pertaining to cancer and ischemia is in very
rapid progress. PARP’s are a specific class of enzymes that repairs the damaged DNA. Recent findings suggest also that
PARP-1 is the most abundantly expressed nuclear enzyme which involves in various therapeutic areas like inflammation,
stroke, cardiac ischemia, cancer and diabetes. The current review describes the overview on clinical candidates of PARP1
and its current status in clinical trials. This paper also covers identification of potent PARP1 inhibitors using structure and
ligand based pharmacophore models. Finally 36 potential hits were identified from the virtual screening of pharmacophore
models and screened for PARP1 activity. 15 actives were identified as potent PARP1 inhibitors and further optimization
of these analogues are in progress.
Keywords: Cancer, docking, glide, PARP1, pharmacophore, virtual screening.
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