PARP1

Overview

PARP1 (Poly ADP-Ribose Polymerase 1) is a key enzyme in the base excision repair pathway. The synthetic lethal interaction between BRCA1/2 deficiency and PARP1 inhibition is the paradigm for DNA damage response-based targeted therapy in oncology.

Alterations observed in the corpus

  • Screened as a DDR candidate in FBXO7 synthetic lethality study; BRCA1/2:PARP1 synthetic lethal interaction used as a conceptual parallel for the FBXO7:CHEK1 SL pair PMID:36334560
  • Identified as a synthetic lethal partner in ARID1A-mutant ovarian cancer cells, where PARP1 inhibition selectively impairs cell survival PMID:22037554
  • PARP inhibitors (niraparib, fuzuloparib, olaparib) tested in combination with ICI to exploit DNA repair deficiencies in NPC PMID:24952746
  • Direct target of olaparib/rucaparib/niraparib/talazoparib; PARP1 knockdown used as positive control for PARPi sensitivity in mCRPC cell lines; synergy with USP10 inhibitor spautin-1 demonstrated PMID:28068672

Cancer types (linked)

  • CRC: referenced in the context of DDR-based synthetic lethality screening PMID:36334560

Co-occurrence and mutual exclusivity

  • PARP1 inhibition is synthetically lethal with BRCA1/2 deficiency (established paradigm referenced in FBXO7 SL study) PMID:36334560

Therapeutic relevance

  • PARP inhibitors (e.g., olaparib) target BRCA1/2-deficient tumors via synthetic lethality; referenced as conceptual parallel for FBXO7:CHEK1 SL PMID:36334560

Open questions

Sources

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