Abstract
In 1977 an unknown natural product was isolated from Streptomyces staurosporeus by Omura et al. during a search for new alkaloids present in actinomycetes and was given the name AM-2282. Later, the structure of AM-2282 was elucidated by single crystal X-ray analysis and renamed as staurosporine. It has been published that staurosporine and its analogues display strong inhibitory effect against a variety of kinases and a number of biological properties such as antifungal, antibacterial, and immunosuppressive activities. Despite strong inhibitory activity of staurosporine, a very high level of cross-reactivity makes it impossible to use staurosporine as a therapeutic agent. In the course of searching for other staurosporine-related compounds, a number of staurosporine analogues have been isolated from different microorganisms. In addition, a number of staurosporine analogues have been synthesized to improve the poor selectivity and target specificity of staurosporine which limited its clinical effectiveness. The review addresses staurosporine analogues from both microbial and synthetic sources and their biological activities.
Keywords: Staurosporine analogues, cancer, kinase inhibitor, phosphorylation, biological activity.
Current Medicinal Chemistry
Title:Staurosporine Analogues from Microbial and Synthetic Sources and Their Biological Activities
Volume: 20 Issue: 31
Author(s): B. S. Park, A. Z. Abdel-Azeem, M. M. Al-Sanea, K. H. Yoo, J. S. Tae and S. H. Lee
Affiliation:
Keywords: Staurosporine analogues, cancer, kinase inhibitor, phosphorylation, biological activity.
Abstract: In 1977 an unknown natural product was isolated from Streptomyces staurosporeus by Omura et al. during a search for new alkaloids present in actinomycetes and was given the name AM-2282. Later, the structure of AM-2282 was elucidated by single crystal X-ray analysis and renamed as staurosporine. It has been published that staurosporine and its analogues display strong inhibitory effect against a variety of kinases and a number of biological properties such as antifungal, antibacterial, and immunosuppressive activities. Despite strong inhibitory activity of staurosporine, a very high level of cross-reactivity makes it impossible to use staurosporine as a therapeutic agent. In the course of searching for other staurosporine-related compounds, a number of staurosporine analogues have been isolated from different microorganisms. In addition, a number of staurosporine analogues have been synthesized to improve the poor selectivity and target specificity of staurosporine which limited its clinical effectiveness. The review addresses staurosporine analogues from both microbial and synthetic sources and their biological activities.
Export Options
About this article
Cite this article as:
Park S. B., Abdel-Azeem Z. A., Al-Sanea M. M., Yoo H. K., Tae S. J. and Lee H. S., Staurosporine Analogues from Microbial and Synthetic Sources and Their Biological Activities, Current Medicinal Chemistry 2013; 20 (31) . https://dx.doi.org/10.2174/09298673113209990176
DOI https://dx.doi.org/10.2174/09298673113209990176 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Synthesis and Hypoxia Selective Radiosensitization Potential of β-2-FAZA and β-3-FAZL: Fluorinated Azomycin β-Nucleosides
Medicinal Chemistry Immunossupressant and Organ Transplantation: Immunophilins Targeting Agent and Alternative Therapies
Current Medicinal Chemistry Prophylactic Vaccine Strategies and the Potential of Therapeutic Vaccines Against Herpes Simplex Virus
Current Pharmaceutical Design Novel Therapeutic Strategies for Dementia
CNS & Neurological Disorders - Drug Targets Cancer Therapy: Targeting Mitochondria and other Sub-cellular Organelles
Current Pharmaceutical Design Advances in the Management of Brain Tumors in Infants
Current Cancer Therapy Reviews Small Ruminant Lentiviruses and Human Immunodeficiency Virus: Cousins that Take a Long View
Current HIV Research Molecular Mechanisms and Targeted Therapies Including Immunotherapy for Non-Small Cell Lung Cancer
Current Cancer Drug Targets Recent Nanocarrier Approaches for Targeted Drug Delivery in Cancer Therapy
Current Molecular Pharmacology 3D Culture Modelling: An Emerging Approach for Translational Cancer Research in Sarcomas
Current Medicinal Chemistry Gene Therapy: The First Approved Gene-Based Medicines, Molecular Mechanisms and Clinical Indications
Current Molecular Pharmacology A Review of Natural and Modified Betulinic, Ursolic and Echinocystic Acid Derivatives as Potential Antitumor and Anti-HIV Agents
Mini-Reviews in Medicinal Chemistry A Natural Membrane Vesicle Exosome-based Sinomenine Delivery Platform for Hepatic Carcinoma Therapy
Current Topics in Medicinal Chemistry Adverse Drug Reactions in the Oral Cavity
Current Pharmaceutical Design VEGF Inhibitors in Cancer Therapy
Current Pharmaceutical Design Small Molecular Inhibitors of p-STAT3: Novel Agents for Treatment of Primary and Metastatic CNS Cancers
Recent Patents on CNS Drug Discovery (Discontinued) Cytokines and their Antagonists as Therapeutic Agents
Current Medicinal Chemistry Outcome Measures Following Sonodynamic Photodynamic Therapy – A Case Series
Current Drug Therapy Neuropeptides as Autocrine Growth Factors in Cancer Cells
Current Pharmaceutical Design CAM Use in Pediatric Oncology
Current Pediatric Reviews