Abstract
Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decade, considerable efforts have been devoted to the production of PTPs inhibitors by both academia and the pharmaceutical industry. However, there are only limited drug candidates in clinical trials and no commercial drugs have been approved, implying that further efficient discovery of novel chemical entities competent for inhibition of the specific PTP target in vivo remains yet a challenge. In light of the click-chemistry paradigm which advocates the utilization of concise and selective carbon-heteroatom ligation reactions for the modular construction of useful compound libraries, the Cu(I)-catalyzed azidealkyne 1,3-dipolar cycloaddition reaction (CuAAC) has fueled enormous energy into the modern drug discovery. Recently, this ingenious chemical ligation tool has also revealed efficacious and expeditious in establishing large combinatorial libraries for the acquisition of novel PTPs inhibitors with promising pharmacological profiles. We thus offer here a comprehensive review highlighting the development of PTPs inhibitors accelerated by the CuAAC click chemistry.
Keywords: Protein tyrosine phosphatase, click chemistry, in situ screening, drug discovery, CuAAC, tyrosine phosphorylation, dephosphorylation, carbohydrate, amino acid, salicylic acid, isoxazole acid, ketocarboxylic acid, competitive inhibitor, bidentate
Current Medicinal Chemistry
Title:CuAAC Click Chemistry Accelerates the Discovery of Novel Chemical Scaffolds as Promising Protein Tyrosine Phosphatases Inhibitors
Volume: 19 Issue: 15
Author(s): X. -P. He, J. Xie, Y. Tang, J. Li, G. -R. Chen
Affiliation:
Keywords: Protein tyrosine phosphatase, click chemistry, in situ screening, drug discovery, CuAAC, tyrosine phosphorylation, dephosphorylation, carbohydrate, amino acid, salicylic acid, isoxazole acid, ketocarboxylic acid, competitive inhibitor, bidentate
Abstract: Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decade, considerable efforts have been devoted to the production of PTPs inhibitors by both academia and the pharmaceutical industry. However, there are only limited drug candidates in clinical trials and no commercial drugs have been approved, implying that further efficient discovery of novel chemical entities competent for inhibition of the specific PTP target in vivo remains yet a challenge. In light of the click-chemistry paradigm which advocates the utilization of concise and selective carbon-heteroatom ligation reactions for the modular construction of useful compound libraries, the Cu(I)-catalyzed azidealkyne 1,3-dipolar cycloaddition reaction (CuAAC) has fueled enormous energy into the modern drug discovery. Recently, this ingenious chemical ligation tool has also revealed efficacious and expeditious in establishing large combinatorial libraries for the acquisition of novel PTPs inhibitors with promising pharmacological profiles. We thus offer here a comprehensive review highlighting the development of PTPs inhibitors accelerated by the CuAAC click chemistry.
Export Options
About this article
Cite this article as:
X. -P. He, J. Xie, Y. Tang, J. Li, G. -R. Chen , CuAAC Click Chemistry Accelerates the Discovery of Novel Chemical Scaffolds as Promising Protein Tyrosine Phosphatases Inhibitors, Current Medicinal Chemistry 2012; 19 (15) . https://dx.doi.org/10.2174/092986712800269245
DOI https://dx.doi.org/10.2174/092986712800269245 |
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
-
Pharmacological Activation of p53 in Cancer Cells
Current Pharmaceutical Design VEGF Promotes Glycolysis in Pancreatic Cancer via HIF1α Up-Regulation
Current Molecular Medicine Three Decades of P-gp Inhibitors: Skimming Through Several Generations and Scaffolds
Current Medicinal Chemistry Oxidative Stress and Cancer: The Role of Nrf2
Current Cancer Drug Targets Pharmacogenomics of Breast Cancer Targeted Therapy: Focus on Recent Patents
Recent Patents on DNA & Gene Sequences The Heme Oxygenase System: Its Role in Liver Inflammation
Current Drug Targets - Cardiovascular & Hematological Disorders Synthesis, Biological Evaluation and Docking Studies of 1,3,4-Oxadiazole Fused Benzothiazole Derivatives for Anticancer Drugs
Letters in Drug Design & Discovery Recent Advance in Drug Development of Squamous Cell Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Therapeutic Value of an Integrin Antagonist in Prostate Cancer
Current Drug Targets Editorial (Thematic Issue: Chemoresistance in Gynecologic Cancers)
Current Cancer Therapy Reviews Regulatory T Cells and Skin Tumors
Recent Patents on Inflammation & Allergy Drug Discovery Can We Predict the Sites of the Recurrence of Ovarian Cancer by F-18 FDG PET/CT Depending on CA-125 Level?
Current Medical Imaging Recent Development in [1,4]Benzodiazepines as Potent Anticancer Agents: A Review
Mini-Reviews in Medicinal Chemistry Genetics of Cancer Susceptibility
Current Genomics The Proteolytic Activation of Angiogenic and Lymphangiogenic Growth Factors in Cancer – Its Potential Relevance for Therapeutics and Diagnostics
Current Medicinal Chemistry Doxorubicin vs. ladirubicin: methods for improving osteosarcoma treatment
Mini-Reviews in Medicinal Chemistry CXCR4 Inhibitors: Tumor Vasculature and Therapeutic Challenges
Recent Patents on Anti-Cancer Drug Discovery Directed Differentiation of Pluripotent Cells Towards Therapeutic Stem Cells
Recent Patents on Regenerative Medicine Rapid Estrogen Signaling in Spermatogenesis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) ABCB1, SLCO1B1 and UGT1A1 Gene Polymorphisms Are Associated with Toxicity Line Irinotecan
Drug Metabolism Letters