Related Experiment Video
Updated: Jul 11, 2026
10:44
Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Improved low molecular weight Myc-Max inhibitors
Huabo Wang1, Dalia I Hammoudeh, Ariele Viacava Follis
1Section of Hematology/Oncology, Children's Hospital of Pittsburgh, Pittsburgh, PA 15213, USA.
Molecular Cancer Therapeutics
|September 19, 2007
Summary
Researchers improved Myc-Max compounds to better inhibit cancer cell growth. These modified compounds effectively disrupt the c-Myc oncoprotein
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- Myc-Max compounds inhibit c-Myc oncoprotein activity.
- Existing compounds have low potency, limiting clinical use.
Purpose of the Study:
- To improve the efficacy of Myc-Max compounds.
- To develop more potent inhibitors of c-Myc-Max association.
Main Methods:
- Chemical modification of the 10058-F4 compound.
- Assessing cell growth inhibition in c-Myc-expressing cells.
- Using fluorescence polarization assays to study compound binding to c-Myc.
Main Results:
- Modified analogues showed enhanced growth inhibition.
- Improved compounds effectively disrupted c-Myc-Max association and DNA binding.
- Active analogues specifically bind to monomeric c-Myc.
Conclusions:
- Directed chemical modification can generate improved Myc-Max compounds.
- These compounds specifically target the c-Myc oncoprotein.
- Understanding c-Myc's dynamic structure aids drug development.
Related Concept Videos
02:23Abnormal Proliferation
Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the daughter...
02:57Targeted Cancer Therapies
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
There are several types of targeted therapies against specific...
01:30Inhibitors of Viral Protein Synthesis
Protein synthesis is indispensable for viral replication, as viruses lack the cellular machinery required for this process and must hijack the host's translational apparatus. In response, host cells deploy a critical innate immune defense involving interferons, specialized cytokines that play a central role in inhibiting viral propagation.Upon viral detection, infected cells release interferons that bind to receptors on adjacent uninfected cells, activating the JAK-STAT signaling pathway and...
02:50Combination Therapies and Personalized Medicine
Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
02:34Inhibition of Cdk Activity
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...
01:06Induced Pluripotent Stem Cells
Stem cells are undifferentiated cells that divide and produce different cell types. Ordinarily, cells that have differentiated into a specific cell type are terminally differentiated; however, scientists have found a way to reprogram these mature cells so that they dedifferentiate and return to an unspecialized, proliferative state. These cells are pluripotent like embryonic stem cells—able to produce all cell types—and are called induced pluripotent stem cells (iPSCs).
Somatic cells are...
Somatic cells are...