Related Experiment Video

Updated: Sep 26, 2026

Yeast As a Chassis for Developing Functional Assays to Study Human P53
14:57

Yeast As a Chassis for Developing Functional Assays to Study Human P53

Published on: August 4, 2019

Drug discovery and p53

David P Lane1, Ted R Hupp

  • 1Cancer Research UK Laboratories, Department of Surgery and Molecular Oncology, University of Dundee, Dundee, Scotland DD1 9SY, UK. d.p.lane@dundee.ac.uk

Drug Discovery Today
|April 12, 2003
PubMed

Insights

Restoring tumor suppressor gene activity, like p53, is a novel cancer drug target. These proteins are intrinsically disordered, enabling small molecules to restore their function and halt cancer cell proliferation.

Area of Science:

  • Oncology
  • Molecular Biology
  • Genetics

Background:

  • Cancer research has advanced significantly due to identifying mutated oncogenes and tumor suppressor genes.
  • Targeting oncogenes with small molecules is established, but restoring tumor suppressor gene function is challenging.

Purpose of the Study:

  • To explore the potential of targeting intrinsically disordered tumor suppressor proteins with small molecules.
  • To investigate the molecular characteristics of p53 that enable therapeutic intervention.

Main Methods:

  • Review of recent advancements in cancer genetics and drug discovery.
  • Molecular characterization of the p53 protein, focusing on its structural and dynamic properties.

Main Results:

  • Many eukaryotic regulatory proteins, including tumor suppressors, are intrinsically disordered.
  • The p53 protein's conformational flexibility and instability are key to its function and post-translational modification.

Conclusions:

  • Intrinsically disordered proteins represent a viable, albeit unconventional, class of drug targets in cancer therapy.
  • Understanding the dynamic nature of proteins like p53 opens new avenues for developing small molecule therapeutics to restore their function.

More Related Videos

Detection of Aggregation-Prone Behavior in Mutant P53 V157F Breast Cancer Cells Using Multipoint Thioflavin T Fluorescence04:56

Detection of Aggregation-Prone Behavior in Mutant P53 V157F Breast Cancer Cells Using Multipoint Thioflavin T Fluorescence

Published on: December 30, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Related Concept Videos

Abnormal Proliferation02:23

Abnormal 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...
DNA Damage Can Stall the Cell Cycle02:36

DNA Damage Can Stall the Cell Cycle

In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...
DNA Damage can Stall the Cell Cycle02:36

DNA Damage can Stall the Cell Cycle

In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...
Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein.