Abstract
Poly(ADP-ribose) polymerase 1 (PARP1) inhibition, increasing chemosensitization and conferring independent antiproliferation against defective homologous recombination cells, has provided a unique opportunity for anticancer therapeutic intervention. Therefore, PARP1, the best characterized enzyme among PARP family, is presently serving as a well-established target for the treatment of oncology attributed to its intimate role in DNA repair. Nowadays, intensified medicinal chemistry efforts have led to the discovery of 12 PARP1 inhibitors that have been advanced into clinical trial. In this article, we classify these candidates as three categories based on the chemical structure, including lactam type, pseudo ring type and untypical PARP1 inhibitors, for a sequential overview of them. In particular, the development of some candidates will serve the purpose for the future exploration of PARP1 inhibitors.
Keywords: Anticancer, clinical trial, PARP1 inhibitors, PARPs, structure-activity relationship (SAR).
Current Medicinal Chemistry
Title:PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention
Volume: 23 Issue: 17
Author(s): Xiaolei Zhu, Xiaodong Ma and Yongzhou Hu
Affiliation:
Keywords: Anticancer, clinical trial, PARP1 inhibitors, PARPs, structure-activity relationship (SAR).
Abstract: Poly(ADP-ribose) polymerase 1 (PARP1) inhibition, increasing chemosensitization and conferring independent antiproliferation against defective homologous recombination cells, has provided a unique opportunity for anticancer therapeutic intervention. Therefore, PARP1, the best characterized enzyme among PARP family, is presently serving as a well-established target for the treatment of oncology attributed to its intimate role in DNA repair. Nowadays, intensified medicinal chemistry efforts have led to the discovery of 12 PARP1 inhibitors that have been advanced into clinical trial. In this article, we classify these candidates as three categories based on the chemical structure, including lactam type, pseudo ring type and untypical PARP1 inhibitors, for a sequential overview of them. In particular, the development of some candidates will serve the purpose for the future exploration of PARP1 inhibitors.
Export Options
About this article
Cite this article as:
Zhu Xiaolei, Ma Xiaodong and Hu Yongzhou, PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention, Current Medicinal Chemistry 2016; 23 (17) . https://dx.doi.org/10.2174/0929867321666140915143516
DOI https://dx.doi.org/10.2174/0929867321666140915143516 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Extracellular Citrate in Health and Disease
Current Molecular Medicine Exosomes Harnessed as Nanocarriers for Cancer Therapy - Current Status and Potential for Future Clinical Applications
Current Molecular Medicine Lipid-based Nanoplatforms in Cancer Therapy: Recent Advances and Applications
Current Cancer Drug Targets Recent Advancements in Liposome-Based Strategies for Effective Drug Delivery to the Brain
Current Medicinal Chemistry Therapeutic Strategies to Target Multiple Kinases in Glioblastoma
Anti-Cancer Agents in Medicinal Chemistry Peptidyl Prolyl Isomerase, Pin1 is a Potential Target for Enhancing the Therapeutic Efficacy of Etoposide
Current Cancer Drug Targets Recent Development of Peptide Drugs and Advance on Theory and Methodology of Peptide Inhibitor Design
Medicinal Chemistry Thiopurine Biotransformation and Pharmacological Effects: Contribution of Oxidative Stress
Current Drug Metabolism Potentials and Challenges of Active Targeting at the Tumor Cells by Engineered Polymeric Nanoparticles
Current Pharmaceutical Biotechnology Phagoptosis - Cell Death By Phagocytosis - Plays Central Roles in Physiology, Host Defense and Pathology
Current Molecular Medicine Pharmacological Activation of p53 in Cancer Cells
Current Pharmaceutical Design Ubiquitin-Protein Ligases - Novel Therapeutic Targets?
Current Protein & Peptide Science Nanotheranostics in Evidence Based Personalized Medicine
Current Drug Targets Recent Patents in Circulating Cell-Free Tumor DNA as Biomarker in Cancer
Recent Patents on Biomarkers Malignant Mesothelioma Resistance to Apoptosis: Recent Discoveries and their Implication for Effective Therapeutic Strategies
Current Medicinal Chemistry Production and Application of Copper Radiopharmaceuticals
Current Radiopharmaceuticals Insights on the Neuromodulatory Propensity of Selaginella (Sanjeevani) and its Potential Pharmacological Applications
CNS & Neurological Disorders - Drug Targets Modified cAMP Derivatives: Powerful Tools in Heart Research
Current Medicinal Chemistry Ganglioside GD3 as a Raft Component in Cell Death Regulation
Anti-Cancer Agents in Medicinal Chemistry Quantum Dot-Based Nanoprobes for In Vivo Targeted Imaging
Current Molecular Medicine