• Corpus ID: 34488651

The PARP inhibitor AZD 2461 is differentiated from olaparib for both PARP 3 activity and drug resistance

  title={The PARP inhibitor AZD 2461 is differentiated from olaparib for both PARP 3 activity and drug resistance},
  author={Lenka Oplustil O’Connor and Stuart L. Rulten and Aaron N. Cranston and Rajesh Odedra and Henry Brown and Janneke E. Jaspers and Louise A Jones and Charlotte Knights and Bastiaan Evers and Attilla Ting and Robert Hugh Bradbury and Marina Pajic and Sven Rottenberg and Jos Jonkers and David Alan Rudge and Niall M. B. Martin and Keith W. Caldecott and Alan Lau and Mark J. O’Connor},


High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs
In vivo efficacy of AZD2281 against BRCA1-deficient breast cancer is demonstrated and how GEMMs of cancer can be used for preclinical evaluation of novel therapeutics and for testing ways to overcome or circumvent therapy resistance is illustrated.
Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Rationale for PARP inhibitors in combination therapy with camptothecins or temozolomide based on PARP trapping versus catalytic inhibition
This work presents a novel and scalable approach called JPET Fast Forward that allows for real-time decision-making in the development of novel targets for cancer treatment and its application in clinical practice.
Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.
This study shows that PARP inhibitors trap the PARP1 and PARP2 enzymes at damaged DNA, providing a new mechanistic foundation for the rational application ofPARP inhibitors in cancer therapy.
The role of PARP in DNA repair and its therapeutic exploitation
Recent studies indicate that tumour cells with defective homologous recombination (HR) repair pathways are exquisitely sensitive to PARPi, and the identification of predictive markers for sensitivity to PARP inhibition is a priority area for research.
PARP-3 and APLF function together to accelerate nonhomologous end-joining.
Post-translational modification of poly(ADP-ribose) polymerase induced by DNA strand breaks.