PARP Inhibitors for Cancer Therapy [electronic resource] / edited by Nicola J. Curtin, Ricky A. Sharma.

1st ed. 2015.
Cham : Springer International Publishing : Imprint: Humana, 2015.
Cancer Drug Discovery and Development, 2196-9906
Cancer Drug Discovery and Development, 2196-9906
1 online resource (590 p.)
Cancer research.
Drug resistance.
Molecular biology.
Local subjects:
Cancer Research. (search)
Drug Resistance. (search)
Molecular Medicine. (search)
PARP Inhibitors for Cancer Therapy provides a comprehensive overview of the role of PARP—poly ADP ribose polymerase—in cancer therapy. The volume covers the history of the discovery of PARP and its role in DNA repair. Additionally, it describes the discovery of the PARP family, and includes a discussion of other DNA maintenance-associated PARPs. As well, the volume features a section on the accessible chemistry behind the development of inhibitors. PARP inhibitors—PARPi—are a group of pharmacological inhibitors that are particularly good targets for cancer therapy. PARP plays a pivotal role in DNA repair and may contribute to the therapeutic resistance to DNA-damaging agents used to treat cancer. Researchers have learned a great deal about the biology of PARP and how tumor-specific defects in DNA repair can be exploited by PARPi. The “synthetic lethality” of PARPi is an exciting concept for cancer therapy, and has led to heightened activity in this area.
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.
Description based upon print version of record.
Includes bibliographical references and index.
Curtin, Nicola J. editor., Editor,
Sharma, Ricky A. editor., Editor,
Publisher Number:
10.1007/978-3-319-14151-0 doi
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