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
-
Breast Cancer and Anesthesia
Current Pharmaceutical Design A Functional Scaffold in Marine Alkaloid: An Anticancer Moiety for Human
Current Medicinal Chemistry Hepatitis C Virus NS3/4A Protease Inhibitors
Recent Patents on Anti-Infective Drug Discovery Editorial [Hot Topic: Lipids in Cancer Cell Biology and Therapy Guest Editor: Jose C. Fernandez-Checa)]
Anti-Cancer Agents in Medicinal Chemistry Novel Anti-Cancer Strategy in Bone Tumors by Targeting Molecular and Cellular Modulators of Bone Resorption
Recent Patents on Anti-Cancer Drug Discovery Recent Advances in the Probe Development of Technetium-99m Molecular Imaging Agents
Current Organic Synthesis Copper Compounds in Cancer Chemotherapy
Current Medicinal Chemistry Mucoadhesive Polymers for Delivery of Drugs to the Oral Cavity
Recent Patents on Drug Delivery & Formulation Editorial (End of the Beginning and Public Health Pharmacogenomics: Knowledge in ‘Mode 2’ and P5 Medicine)
Current Pharmacogenomics and Personalized Medicine Subject Index to Volume 4
Current Drug Targets Biological and Chemical Diversity of Coral-Derived Microorganisms
Current Medicinal Chemistry Phospholipid Nanosomes
Current Drug Delivery Editorial (Thematic Issue: Green Anti-Cancer Agents and Ayur-Biotechnology: A smart approach towards improving R&D productivity.)
Anti-Cancer Agents in Medicinal Chemistry Programmed Cell Death Mechanisms in Neurological Disease
Current Molecular Medicine Identify DNA-Binding Proteins with Optimal Chou’s Amino Acid Composition
Protein & Peptide Letters Effect of Hyperthermia and Triblock Copolymeric Nanoparticles as Quercetin Carrier on DU145 Prostate Cancer Cells
Current Nanoscience Long Non-coding RNA and microRNAs as Novel Potential Biomarker and Therapeutic Target in the Treatment of Gastrointestinal Cancers
Current Pharmaceutical Design Histone Deacetylase 2 in the Mouse Hippocampus: Attenuation of Age- Related Increase by Caloric Restriction
Current Alzheimer Research TRPV1 Function in Health and Disease
Current Pharmaceutical Biotechnology Tumor Initiating Cells
Current Pharmaceutical Biotechnology