PARP Inhibitors for Cancer Therapy

PARP Inhibitors for Cancer Therapy

Sharma, Ricky A.; Curtin, Nicola J.

Birkhauser Verlag AG

02/2018

591

Mole

Inglês

9783319344898

15 a 20 dias

926

Descrição não disponível.
History of the discovery of poly (ADP-ribose).- Discovery of the PARP superfamily and focus on the lesser exhibited but not lesser talented members.- The role of PARPs in DNA Strand Break Repair.- TIPs: Tankyrase Interacting Proteins.- PARP and Carcinogenesis.- Multitasking roles for poly(ADP-ribosyl)ation in aging and longevity.- Overview of PARP Inhibitor Design and Optimization.- Structure Based Design of PARP Inhibitors.- Preclinical chemosensitization by PARP inhibitors.- Classification of PARP inhibitors based on PARP trapping and catalytic inhibition, and rationale for combinations with topoisomerase I inhibitors and alkylating agents.- Radiosensitisation by poly(ADP-ribose) polymerase inhibition.- The vasoactivity of PARP inhibitors.- Synthetic lethality with Homologous Recombination Repair defects.- Targeting tumour hypoxia with PARP Inhibitors: Contextual synthetic lethality.- Other determinants of sensitivity.- Synthetic sickness with molecularly targeted agents against the EGFR pathway.- Disruption of DNA repair by cell cycle and transcriptional CDK inhibition.- Resistance to PARP Inhibitors Mediated by Secondary BRCA1/2 Mutations.- PARP inhibitor resistance - what is beyond BRCA1 or BRCA2 restoration.- Introduction to PARPi clinical trials and future directions.- Clinical trials investigating PARP inhibitors as single agents.- Clinical trials of PARP inhibitors with chemotherapy.- Combination of PARP inhibitors with clinical radiotherapy.- Biomarkers for PARP Inhibitors.
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DNA repair;PARP;cancer;carcinogenesis;drug resistance;inhibitors;antibacterial drug resistance