Fundamentals and emerging frontiers in p53-targeted drug development

Hui-Deng Long1,2, Ning Zhang3, Wen-Er Wang4

  • 1Department of Pathology, The Affiliated Taizhou People's Hospital of Nanjing Medical University, Taizhou School of Clinical Medicine, Nanjing Medical University, Taizhou, Jiangsu, 225300, China.

Insights

The p53 tumor suppressor is crucial for preventing cancer, but its mutations drive over half of human cancers. This review explores novel p53-targeted therapies, including small molecules, gene therapy, and emerging technologies, to overcome drug resistance.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The p53 protein is a critical tumor suppressor involved in cell cycle regulation, DNA repair, and apoptosis.
  • Mutations or inactivation of the p53 gene occur in over 50% of human cancers, promoting tumorigenesis and drug resistance.
  • Targeting p53 is a key strategy in anticancer drug development, but faces challenges like diverse mutation types and resistance.

Purpose of the Study:

  • To systematically review the fundamental theories and cutting-edge advances in p53-targeted drug development.
  • To analyze the research history and clinical translation of small-molecule drugs targeting p53.
  • To discuss the prospects of gene therapy, immunotherapy, CRISPR, and PROTAC technologies for p53-targeted cancer treatment.

Main Methods:

  • Literature review of p53 structure, function, and mutation-induced carcinogenesis.
  • Analysis of small-molecule drugs (e.g., APR-246) and their clinical status.
  • Exploration of gene therapy, immunotherapy, CRISPR, and PROTAC technologies for p53-targeted therapies.

Main Results:

  • p53 mutations are a significant driver of cancer development and drug resistance.
  • Various therapeutic strategies are being developed to target p53, including small molecules, gene therapy, and novel technologies.
  • Emerging approaches like CRISPR and PROTAC offer new avenues for precise p53-targeted drug development.

Conclusions:

  • Developing effective p53-targeted drugs requires addressing diverse mutation types and overcoming drug resistance.
  • Gene therapy, immunotherapy, CRISPR, and PROTAC technologies show promise for future p53-targeted cancer treatments.
  • This review provides a theoretical basis and guidance for precise p53-targeted drug development and clinical translation.

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