Abstract
The Cdc25 phosphatases (Cdc25A, Cdc25B, and Cdc25C in humans), which are responsible for dephosphorylating specific tyrosine/ threonine residues on cyclin dependent kinases (CDKs), function as essential regulators of cell cycle control during normal eukaryotic cell division and as mediators of the checkpoint response in cells with DNA damage. Because overexpression of Cdc25A and Cdc25B has been linked to numerous cancers and often correlates with a poor clinical outcome, both academia and industry have devoted substantial research effort in establishing the basic underlying molecular mechanisms and in identifying novel, specific and potentially useful inhibitors of Cdc25 as potential anticancer drugs. Over the past year, dozens of research papers and patent applications describing new Cdc25 inhibitors belonging to different structural classes have been disclosed. In this review, we give an overview on the current status in the field of medicinal chemistry of Cdc25B inhibitors. In addition, molecular modeling studies aimed to clarify the molecular mechanism of inhibition as well as the pharmacophoric features critical for design of new and selective Cdc25B inhibitors are also discussed.
Keywords: Cancer, phosphatases, Cdc25 inhibitors, cell cycle, antiproliferative agents, docking, molecular modeling
Anti-Cancer Agents in Medicinal Chemistry
Title: Cdc25B Phosphatase Inhibitors in Cancer Therapy: Latest Developments, Trends and Medicinal Chemistry Perspective
Volume: 8 Issue: 8
Author(s): Antonio Lavecchia, Antonio Coluccia, Carmen Di Giovanni and Ettore Novellino
Affiliation:
Keywords: Cancer, phosphatases, Cdc25 inhibitors, cell cycle, antiproliferative agents, docking, molecular modeling
Abstract: The Cdc25 phosphatases (Cdc25A, Cdc25B, and Cdc25C in humans), which are responsible for dephosphorylating specific tyrosine/ threonine residues on cyclin dependent kinases (CDKs), function as essential regulators of cell cycle control during normal eukaryotic cell division and as mediators of the checkpoint response in cells with DNA damage. Because overexpression of Cdc25A and Cdc25B has been linked to numerous cancers and often correlates with a poor clinical outcome, both academia and industry have devoted substantial research effort in establishing the basic underlying molecular mechanisms and in identifying novel, specific and potentially useful inhibitors of Cdc25 as potential anticancer drugs. Over the past year, dozens of research papers and patent applications describing new Cdc25 inhibitors belonging to different structural classes have been disclosed. In this review, we give an overview on the current status in the field of medicinal chemistry of Cdc25B inhibitors. In addition, molecular modeling studies aimed to clarify the molecular mechanism of inhibition as well as the pharmacophoric features critical for design of new and selective Cdc25B inhibitors are also discussed.
Export Options
About this article
Cite this article as:
Lavecchia Antonio, Coluccia Antonio, Di Giovanni Carmen and Novellino Ettore, Cdc25B Phosphatase Inhibitors in Cancer Therapy: Latest Developments, Trends and Medicinal Chemistry Perspective, Anti-Cancer Agents in Medicinal Chemistry 2008; 8 (8) . https://dx.doi.org/10.2174/187152008786847783
DOI https://dx.doi.org/10.2174/187152008786847783 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Magnetic Hydrogel Nanocomposites and Composite Nanoparticles – a Review of Recent Patented Works
Recent Patents on Nanotechnology Stress Relaxation Testing of Non-Small Lung Cancer Cells Using Atomic Force Microscopy
Current Nanoscience Piperine and Derivatives: Trends in Structure-Activity Relationships
Current Topics in Medicinal Chemistry Impact of Viscosity and Refractive Index on Droplet Size and Zeta Potential of Model O/W and W/O Nanoemulsion
Current Nanoscience Backbone-Cyclized Peptides: A Critical Review
Current Topics in Medicinal Chemistry Investigating the Therapeutic Effects of Alginate Nanogel Co-loaded with Gold Nanoparticles and Cisplatin on U87-MG Human Glioblastoma Cells
Anti-Cancer Agents in Medicinal Chemistry Biological Activities and Corresponding SARs of Andrographolide and Its Derivatives
Mini-Reviews in Medicinal Chemistry The Role of PPARβ/δ in the Management of Metabolic Syndrome and its Associated Cardiovascular Complications
Endocrine, Metabolic & Immune Disorders - Drug Targets Pharmacological Applications of Antioxidants: Lights and Shadows
Current Drug Targets Nanopotentiation of Propolis for Revocation of Enzyme Imbalance in UVB Induced Cutaneous Toxicity in Murine Model: a Preliminary Study for Chemoprotection of Skin Cancer
Drug Delivery Letters Nitric Oxide and Dietary Factors: Part IV Traditional Japanese Food (Soy Products, Fish and Tea)
Vascular Disease Prevention (Discontinued) Regulation of Mammalian UDP-Glucuronosyltransferases
Current Drug Metabolism Bergamot Juice Extract Inhibits Proliferation by Inducing Apoptosis in Human Colon Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Meet Our Editorial Board Member
Current Cancer Drug Targets Cdc42 Signaling Pathway Inhibition as a Therapeutic Target in Ras- Related Cancers
Current Medicinal Chemistry Allosteric Inhibitors of Bcr-Abl: Towards Novel Myristate-Pocket Binders
Current Pharmaceutical Biotechnology Polymer-based Nanodevices for Effective Antimicrobial Therapy: Synthetic Strategies and Applications
Current Applied Polymer Science Molecular Classification of Breast Carcinoma In Situ
Current Genomics Role of Antioxidants for the Treatment of Cardiovascular Diseases: Challenges and Opportunities
Current Pharmaceutical Design Bone Morphogenetic Proteins and its Receptors; Therapeutic Targets in Cancer Progression and Bone Metastasis?
Current Pharmaceutical Design