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
-
A Review of the Effects of Gold, Silver, Selenium, and Zinc Nanoparticles on Diabetes Mellitus in Murine Models
Mini-Reviews in Medicinal Chemistry Diversity-Oriented Synthetic Approaches for Furoindoline: A Review
Current Organic Synthesis Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 2. Structural Analogues and Derivatives
Current Drug Targets Gene and Stem Cell Therapy in the Treatment of Erectile Dysfunction and Pulmonary Hypertension; Potential Treatments for the Common Problem of Endothelial Dysfunction
Current Gene Therapy Retinoids as Differentiating Agents in Oncology: A Network of Interactions with Intracellular Pathways as the Basis for Rational Therapeutic Combinations
Current Pharmaceutical Design The Pim Kinases: New Targets for Drug Development
Current Drug Targets TRICOM Vector Based Cancer Vaccines
Current Pharmaceutical Design Impact of p53 arg72pro SNP on Breast Cancer Risk in North Indian Population
Current Genomics Target-oriented Mechanisms of Novel Herbal Therapeutics in the Chemotherapy of Gastrointestinal Cancer and Inflammation
Current Pharmaceutical Design Implications of Fibroblast Growth Factors (FGFs) in Cancer: From Prognostic to Therapeutic Applications
Current Drug Targets Role of Mechanoinsensitive Nociceptors in Painful Diabetic Peripheral Neuropathy
Current Diabetes Reviews Trends in Utilization of the Pharmacological Potential of Chalcones
Current Clinical Pharmacology Modulation of Carbonic Anhydrase 9 (CA9) in Human Brain Cancer
Current Pharmaceutical Design CEACAM1 in Malignant Melanoma: A Diagnostic and Therapeutic Target
Current Topics in Medicinal Chemistry Gene Electrotransfer to Skin; Review of Existing Literature and Clinical Perspectives
Current Gene Therapy Difluorinated Curcumin: A Promising Curcumin Analogue with Improved Anti-Tumor Activity and Pharmacokinetic Profile
Current Pharmaceutical Design Current State of the Art of New Tubulin Inhibitors in the Clinic
Current Clinical Pharmacology Obesity and Arterial Compliance Alterations
Current Vascular Pharmacology RNAi in Clinical Studies
Current Medicinal Chemistry Laminin-332-Integrin Interaction: A Target For Cancer Therapy?
Current Medicinal Chemistry