Abstract
Tankyrase 1 and 2 belonging to the family of poly(ADP-ribosyl)ases play an important role in PARsylation by utilizing NAD+ as a substrate in order to generate ADP-ribose polymers. Tankyrases are involved in a number of cellular functions, that includes telomere homeostasis, mitotic spindle formation, vesicle transport linked to glucose metabolism, Wnt/β-catenin signalling, and viral replication. These roles of tankyrases in disease-relevant cellular processes have made them attractive drug targets. Recently, several inhibitors have been identified as potential clinical leads. The current review covers the progress, mechanism and binding modes of recently known Tankyrase inhibitors and discusses the rational approaches that were used to identify the tankyrase inhibitors.
Keywords: Cancer, glucose metabolism, inhibitors, PARsylation, PARP, tankyrase.
Current Topics in Medicinal Chemistry
Title:Tankyrase Inhibitors as Therapeutic Targets for Cancer
Volume: 14 Issue: 17
Author(s): Ahmed Kamal, Sd. Riyaz, Ajay Kumar Srivastava and Abdul Rahim
Affiliation:
Keywords: Cancer, glucose metabolism, inhibitors, PARsylation, PARP, tankyrase.
Abstract: Tankyrase 1 and 2 belonging to the family of poly(ADP-ribosyl)ases play an important role in PARsylation by utilizing NAD+ as a substrate in order to generate ADP-ribose polymers. Tankyrases are involved in a number of cellular functions, that includes telomere homeostasis, mitotic spindle formation, vesicle transport linked to glucose metabolism, Wnt/β-catenin signalling, and viral replication. These roles of tankyrases in disease-relevant cellular processes have made them attractive drug targets. Recently, several inhibitors have been identified as potential clinical leads. The current review covers the progress, mechanism and binding modes of recently known Tankyrase inhibitors and discusses the rational approaches that were used to identify the tankyrase inhibitors.
Export Options
About this article
Cite this article as:
Kamal Ahmed, Riyaz Sd., Srivastava Kumar Ajay and Rahim Abdul, Tankyrase Inhibitors as Therapeutic Targets for Cancer, Current Topics in Medicinal Chemistry 2014; 14 (17) . https://dx.doi.org/10.2174/1568026614666140929115831
DOI https://dx.doi.org/10.2174/1568026614666140929115831 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
DLEU2: A Meaningful Long Noncoding RNA in Oncogenesis
Current Pharmaceutical Design Resveratrol Counteracts Hypoxia-Induced Gastric Cancer Invasion and EMT through Hedgehog Pathway Suppression
Anti-Cancer Agents in Medicinal Chemistry Coupling of Conjugating Enzymes and Efflux Transporters: Impact on Bioavailability and Drug Interactions
Current Drug Metabolism Editorial (Hot Topic: TRP Channels as Therapeutic Targets)
Current Topics in Medicinal Chemistry Quantum Dots in the Therapy: Current Trends and Perspectives
Mini-Reviews in Medicinal Chemistry MicroRNA in the Pathogenesis and Prognosis of Esophageal Cancer
Current Pharmaceutical Design Efficacy and Safety of the Combination of Docetaxel (Taxotere®) with Targeted Therapies in the Treatment of Solid Malignancies
Current Drug Targets Recent Advances in T Cell Adoptive Immunotherapy of Cancer
Current Cancer Therapy Reviews Diastereoselective Synthesis of Dispiropseudoindoxyls and Preparation of 9-Oxopyrrolo[ 1,2-α]Indoles
Current Organic Synthesis Dietary Phytochemicals in Chemoprevention of Cancer: An Update
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Viral-Mediated Gene Transfer for Cancer Treatment
Current Pharmaceutical Biotechnology Natural Sourced Inhibitors of EGFR, PDGFR, FGFR and VEGFRMediated Signaling Pathways as Potential Anticancer Agents
Current Medicinal Chemistry Bioinorganic Chemistry: The Study of the Fate of Platinum-Based Antitumour Drugs
Current Chemical Biology The Synthesis of Nano-Doxorubicin and its Anticancer Effect
Anti-Cancer Agents in Medicinal Chemistry Gene Electrotransfer: A Mechanistic Perspective
Current Gene Therapy Recent Development of Copolymeric Delivery System for Anticancer Agents Based on Cyclodextrin Derivatives
Anti-Cancer Agents in Medicinal Chemistry In Vitro Screening of an FDA-Approved Library Against ESKAPE Pathogens
Current Pharmaceutical Design Patent Selections:
Recent Patents on Anti-Cancer Drug Discovery Intracellular Trafficking of MDR Transporters and Relevance of SNPs
Current Topics in Medicinal Chemistry Effects of Edible Algae Polysaccharides on Allergic, Inflammatory, and Anti-Tumor Responses Through Toll-Like Receptor 4
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry