PARP1

Poly(ADP-ribose) polymerase 1 (PARP1) is a crucial DNA repair enzyme that plays a key role in the cellular response to DNA damage. It catalyzes poly(ADP-ribosyl)ation (PARylation), a post-translational modification that regulates DNA repair, gene expression, and cell survival. DNA Damage-Dependent PARylation Process by PARP1 The activation of PARP1 and its PARylation reaction is a multi-step process, which includes: DNA Damage Recognition Upon single-strand breaks (SSBs) or double-strand breaks (DSBs), PARP1 binds to damaged DNA via its zinc finger domains (Zn fingers). This binding induces a conformational change that activates its catalytic domain. NAD⁺ Binding and Hydrolysis Activated PARP1 utilizes NAD⁺ (nicotinamide adenine dinucleotide) as a substrate. It cleaves NAD⁺ to release nicotinamide and generate an ADP-ribose unit. Attachment of ADP-Ribose Monomers The initial ADP-ribose unit is covalently attached to PARP1 itself or other target proteins, such as histones and DNA repair factors. Poly(ADP-Ribose) Chain Elongation PARP1 continues to catalyze the transfer of multiple ADP-ribose units, forming linear or branched poly(ADP-ribose) (PAR) chains. This modification recruits DNA repair complexes, facilitating base excision repair (BER) and homologous recombination (HR). Regulation of Target Proteins PAR chains act as a platform for protein-protein interactions, modulating DNA repair, chromatin remodeling, and transcriptional regulation. PARP1 Auto-Regulation and PAR Degradation Once DNA repair is complete, poly(ADP-ribose) glycohydrolase (PARG) degrades PAR chains. This restores cellular homeostasis and prevents excessive PARP1 activity.

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A10111

Olaparib (AZD2281)

PARP inhibitor

Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
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