Related Experiment Video
Updated: Dec 23, 2025

Yeast As a Chassis for Developing Functional Assays to Study Human P53
Published on: August 4, 2019
Recent Synthetic Approaches towards Small Molecule Reactivators of p53
Jerson L Silva1, Carolina G S Lima2, Luciana P Rangel3
1Programa de Biologia Estrutural, Instituto de Bioquímica Médica Leopoldo de Meis, Instituto Nacional de Ciência e Tecnologia de Biologia Estrutural e Bioimagem, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21941-902, Brazil.
Abstract:
The tumor suppressor protein p53 is often called "the genome guardian" and controls the cell cycle and the integrity of DNA, as well as other important cellular functions. Its main function is to trigger the process of apoptosis in tumor cells, and approximately 50% of all cancers are related to the inactivation of the p53 protein through mutations in the TP53 gene. Due to the association of mutant p53 with cancer therapy resistance, different forms of restoration of p53 have been subject of intense research in recent years. In this sense, this review focus on the main currently adopted approaches for activation and reactivation of p53 tumor suppressor function, focusing on the synthetic approaches that are involved in the development and preparation of such small molecules.
Insights
The tumor suppressor protein p53 guards the genome by controlling cell cycle and DNA integrity. Reactivating p53 is crucial for overcoming cancer therapy resistance.
Area of Science:
- Molecular Biology
- Oncology
- Drug Discovery
Background:
- The tumor suppressor protein p53, known as the "genome guardian", regulates cell cycle, DNA integrity, and apoptosis.
- Mutations in the TP53 gene inactivate p53 in about 50% of human cancers, often leading to therapy resistance.
- Restoring p53 function is a key strategy in cancer treatment research.
Purpose of the Study:
- To review current approaches for activating and reactivating the tumor suppressor function of p53.
- To focus on synthetic strategies for developing small molecules that restore p53 activity.
Main Methods:
- Literature review of synthetic approaches for p53 reactivation.
- Analysis of small molecule development and preparation methods.
Main Results:
- Identification of various synthetic strategies aimed at restoring p53 tumor suppressor function.
- Overview of small molecules designed to activate or reactivate p53.
Conclusions:
- Synthetic approaches are central to developing novel therapeutics targeting p53.
- Restoring p53 function holds significant promise for overcoming cancer therapy resistance.
Related Concept Videos
Abnormal Proliferation
Conservative Site-specific Recombination and Phase Variation
The recognition sites for Cre recombinase called LoxP...
Covalently Linked Protein Regulators
These groups modify specific amino acids in a protein....
Negative Regulator Molecules
DNA Damage Can Stall the Cell Cycle
DNA Damage can Stall the Cell Cycle

