Abstract
Recently identified novel agents that disrupt tubulin polymerization include synthetic spiroketal pyrans (SPIKET) targeting the spongistatin binding site of beta tubulin. These agents exhibit anticancer activity by disrupting normal mitotic spindle assembly and cell division as well as inducing apoptosis. At nanomolar concentrations, the SPIKET compound SPIKET-P caused tubulin depolymerization in cell-free turbidity assays and exhibited potent cytotoxic activity against cancer cells as evidenced by destruction of microtubule organization, and prevention of mitotic spindle formation in human breast cancer cells. SPIKET compounds represent a new class of tubulin targeting agents that show promise as anti-cancer drugs.
Keywords: Spongistatins, Tubulin Targeting Agents, spiroketal pyrans (SPIKET), anticancer activity, SPIKET, SPIKET-P, anti-cancer drugs, Spiroketal Pyrans (SPIKET-P), Beta Tubulin, colchicine
Current Pharmaceutical Design
Title: Spongistatins as Tubulin Targeting Agents
Volume: 7 Issue: 13
Author(s): F. M. Uckun, C. Mao, S. -T. jan, H. Huang, A. O. Vassilev, C. S. Navara and R. K. Narla
Affiliation:
Keywords: Spongistatins, Tubulin Targeting Agents, spiroketal pyrans (SPIKET), anticancer activity, SPIKET, SPIKET-P, anti-cancer drugs, Spiroketal Pyrans (SPIKET-P), Beta Tubulin, colchicine
Abstract: Recently identified novel agents that disrupt tubulin polymerization include synthetic spiroketal pyrans (SPIKET) targeting the spongistatin binding site of beta tubulin. These agents exhibit anticancer activity by disrupting normal mitotic spindle assembly and cell division as well as inducing apoptosis. At nanomolar concentrations, the SPIKET compound SPIKET-P caused tubulin depolymerization in cell-free turbidity assays and exhibited potent cytotoxic activity against cancer cells as evidenced by destruction of microtubule organization, and prevention of mitotic spindle formation in human breast cancer cells. SPIKET compounds represent a new class of tubulin targeting agents that show promise as anti-cancer drugs.
Export Options
About this article
Cite this article as:
Uckun M. F., Mao C., jan -T. S., Huang H., Vassilev O. A., Navara S. C. and Narla K. R., Spongistatins as Tubulin Targeting Agents, Current Pharmaceutical Design 2001; 7 (13) . https://dx.doi.org/10.2174/1381612013397492
DOI https://dx.doi.org/10.2174/1381612013397492 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Design, Synthesis and Antitumor Activity of Quinazoline Derivatives Bearing 2,3-Dihydro-indole or 1,2,3,4-Tetrahydroquinoline
Letters in Drug Design & Discovery Inhibition of Hedgehog/Gli Signaling by Botanicals: A Review of Compounds with Potential Hedgehog Pathway Inhibitory Activities
Current Cancer Drug Targets Neuronal Death in Amyotrophic Lateral Sclerosis (ALS): What Can We Learn from Genetics?
CNS & Neurological Disorders - Drug Targets Enhanced Biocatalytic Activity of Recombinant Lipase Immobilized on Gold Nanoparticles
Current Pharmaceutical Biotechnology Editorial (Thematic Issue: "Discovery and Development of New Anticancer Drugs Inspired from Natural Product Leads" Part 1)
Anti-Cancer Agents in Medicinal Chemistry Cyclophosphamide and/or Anthracyclines Induced Epiphora in Breast Cancer Patients: A Rare Side-effect
Current Drug Safety Adenoviral Vectors for Cancer Gene Therapy
Current Genomics Patent Selections
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Anti-Cancer Drug Design Using Natural and Synthetic Pharmacophores
Current Organic Chemistry The Role of Epithelial-Mesenchymal Interactions in Tissue Repair, Fibrogenesis and Carcinogenesis
Current Signal Transduction Therapy Wheel of Fortune – Cyclic Peptides Hit the Mimetic Jackpot: Current Syntheses, Uses and Roles for Cyclic Peptide Mimetics
Current Chemical Biology Extracellular Vesicles in the Treatment of Parkinson’s Disease: A Review
Current Medicinal Chemistry Gold Nanostructure: Fabrication, Surface Modification, Targeting Imaging, and Enhanced Radiotherapy
Current Nanoscience Patent Selections
Recent Patents on Anti-Cancer Drug Discovery Dendritic Cell Vaccine and Cancer Treatment: New Patents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Targeting Microtubules to Inhibit Angiogenesis and Disrupt Tumour Vasculature:Implications for Cancer Treatment
Current Cancer Drug Targets Serum miRNAs Signature Plays an Important Role in Keloid Disease
Current Molecular Medicine Diazine Analogues of the Pyridocarbazole Alkaloids
Current Organic Chemistry Discovery of Potent Natural-Product-Derived SIRT2 Inhibitors Using Structure- Based Exploration of SIRT2 Pharmacophoric Space Coupled With QSAR Analyses
Anti-Cancer Agents in Medicinal Chemistry Advances in Human Cytochrome P450 and Personalized Medicine
Current Drug Metabolism