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Related Experiment Video

Updated: Apr 30, 2026

Yeast As a Chassis for Developing Functional Assays to Study Human P53
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Small molecule compounds targeting the p53 pathway: are we finally making progress?

Xin Yu1, Sumana Narayanan, Alexei Vazquez

  • 1Rutgers Cancer Institute of New Jersey, Robert Wood Johnson Medical School, Rutgers-The State University of New Jersey, 195 Little Albany Street, New Brunswick, NJ, 08903, USA.

Apoptosis : an International Journal on Programmed Cell Death
|April 24, 2014
PubMed
Summary

Targeting the p53 tumor suppressor gene, the most frequently mutated gene in human cancers, is crucial. Researchers are developing small-molecule drugs to activate the p53 pathway, with several now in clinical trials.

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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The p53 tumor suppressor gene is the most frequently mutated gene in human cancers.
  • Loss of p53 function is critical for cancer development, making its pathway a key therapeutic target.

Purpose of the Study:

  • To review current literature on small-molecule drugs targeting wild-type and mutant p53.
  • To discuss drug discovery methods and mechanisms of action for p53-targeting agents.
  • To outline the developmental status of these drugs and identify future therapeutic avenues.

Main Methods:

  • Literature review of small-molecule compounds targeting p53.
  • Classification of drugs based on their mechanisms of action.
  • Analysis of current clinical trial data for p53-targeting therapeutics.

Main Results:

  • Significant progress has been made in discovering small molecules that target both wild-type and mutant p53.
  • The first in-human clinical trials for several p53-targeting drugs have been initiated and completed.
  • Various approaches are being explored to pharmacologically activate the p53 pathway.

Conclusions:

  • Pharmacologic activation of the p53 pathway represents a promising, yet challenging, therapeutic strategy in cancer treatment.
  • Small-molecule drugs targeting p53 are advancing through clinical development.
  • Emerging insights into p53 tumor biology may reveal novel therapeutic targets.