A Src/Abl kinase inhibitor, bosutinib, downregulates and inhibits PARP enzyme and sensitizes cells to the DNA damaging agents


Kirmizibayrak P. , İLHAN R. , Yilmaz S. , GUNAL S., Tepedelen B. E.

TURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISI, vol.43, no.2, pp.101-109, 2018 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 43 Issue: 2
  • Publication Date: 2018
  • Doi Number: 10.1515/tjb-2017-0095
  • Title of Journal : TURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISI
  • Page Numbers: pp.101-109
  • Keywords: PARP inhibitor, PARylation, Bosutinib, Multi-kinase inhibitor, Chemosensitizer, POLY(ADP-RIBOSE) POLYMERASE-1 INHIBITOR, SKI-606 BOSUTINIB, BREAST-CANCER, GROWTH, DEATH, ACTIVATION, PROSTATE, INVASION, PATHWAY, STRESS

Abstract

Background: Poly(ADP-ribosyl)ation (PARylation) catalyzed mainly by PARP1 is a highly regulated posttranslational modification associated with several pathways in cellular physiology and genotoxic deoxyribonucleic acid (DNA) damage response. PAR polymers and PARP enzyme function in DNA integrity maintenance and several PARP inhibitors have entered clinical phase studies for cancer therapies.