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.

Biomolecules
|April 25, 2020
PubMed

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.

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