Suggest an approach you would take to identify the pharmacophore in the following lead compound which inhibits poly(ADP-ribose) polymerase-1 (PARP-1).
Suggest an approach you would take to identify the pharmacophore in the following lead
compound which inhibits poly(ADP-ribose) polymerase-1 (PARP-1).
poly(ADP-ribose) polymerase-1 (PARP-1):
PARP-1) is a nuclear enzyme that plays an important role in DNA repair, transcriptional regulation, and cell death. It catalyzes the formation of poly(ADP-ribose) (PAR) chains from NAD+ molecules, which are then covalently attached to target proteins to modulate their activity or facilitate their repair.
PARP-1 is of particular interest in cancer research because it is overactivated in many types of cancer cells, leading to increased DNA damage repair and cell survival. Inhibition of PARP-1 can therefore sensitize cancer cells to chemotherapy or radiation therapy, making it a promising target for cancer treatment.
Several PARP-1 inhibitors have been developed and approved for the treatment of cancer, including Olaparib, Rucaparib, and Niraparib. These drugs selectively bind to the PARP-1 active site and prevent the formation of PAR chains, leading to accumulation of DNA damage and cell death.
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