Related Experiment Video
Updated: Sep 26, 2025
08:49
Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
9.2K
A Comprehensive Overview of the Developments of Cdc25 Phosphatase Inhibitors
Ahmed Bakr Abdelwahab1, Eslam Reda El-Sawy2, Atef G Hanna2
1Plant Advanced Technologies (PAT), 54500 Vandoeuvre-les-Nancy, France.
Molecules (Basel, Switzerland)
|April 23, 2022
Summary
Cdc25 phosphatases are key targets for cancer drug development. This review analyzes chemical structures of Cdc25 inhibitors to guide the design of more effective and less toxic anticancer therapies.
Area of Science:
- Oncology
- Medicinal Chemistry
- Biochemistry
Background:
- Cdc25 phosphatases are frequently overexpressed in various cancers.
- This overexpression links Cdc25 phosphatases to cancer development, making them attractive therapeutic targets.
- Research interest in Cdc25 phosphatases as anticancer targets has surged over the past two decades.
Purpose of the Study:
- To review and present the chemical structures of known Cdc25 inhibitors.
- To provide insights into designing novel Cdc25 inhibitors with improved efficacy.
- To address strategies for reducing toxicity in Cdc25-targeted anticancer agents.
Main Methods:
- Comprehensive literature review of publications from 1992 to 2021.
- Data analysis of reported Cdc25 inhibitor structures and their properties.
- Synthesis of information to identify structure-activity relationships.
Main Results:
- Detailed compilation of diverse chemical scaffolds targeting Cdc25 phosphatases.
- Identification of key structural features associated with Cdc25 inhibitory activity.
- Analysis of existing inhibitors' efficacy and toxicity profiles.
Conclusions:
- Cdc25 phosphatases represent a validated target class for anticancer drug discovery.
- Understanding inhibitor chemical structures is crucial for rational drug design.
- Future efforts should focus on optimizing Cdc25 inhibitors for enhanced potency and reduced side effects.
More Related Videos
10:33Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
Published on: October 26, 2015
11.4K
12:26Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
Published on: May 3, 2018
18.8K
Related Concept Videos
02:34Inhibition of Cdk Activity
5.0K
The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
5.0K
00:50Anaphase Promoting Complex
3.0K
The stepwise destruction of specific proteins is necessary for the progression and completion of the cell cycle. Such proteins are ubiquitinated by ubiquitin ligases and then subsequently destroyed by the proteasome. The SCF (Skp1/Cullin/F-box) and the anaphase-promoting complex (APC) are two important ubiquitin ligases involved in cell cycle progression. While SCF is active throughout the cell cycle, APC gets activated during metaphase to anaphase transition. Cdc20 or Cdh1 binds to APC and...
3.0K
02:15M-Cdk Drives Transition Into Mitosis
5.7K
Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
5.7K
02:54Protein Kinases and Phosphatases
13.5K
Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
13.5K
01:10Drugs that Destabilize Microtubules
2.1K
Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
2.1K
02:39Positive Regulator Molecules
5.7K
Mitotic cell division results in daughter cells that exactly resemble the parent cell. However, errors in the DNA replication or distribution of genetic material may lead to genetic mutations that may be passed down to every new cell formed from the resulting abnormal cell. Propagation of such mutant cells is restricted through checkpoint mechanisms present at different stages of the cell cycle. These checkpoints involve regulator molecules that either promote or demote cell cycle events.
5.7K