Related Experiment Video

Updated: May 28, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
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Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

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Dysregulation of the p300/CBP histone acetyltransferases in human cancer

Longxia Xu1, Hongwen Xuan1, Xiaobing Shi1

  • 1Department of Epigenetics, Van Andel Institute, Grand Rapids, MI, USA.

Epigenomics
|February 10, 2025
PubMed

Insights

p300 and CREB-binding protein (CBP) are crucial for gene expression and development. Their dysregulation in cancer, through mutations, drives tumor progression, highlighting their therapeutic potential.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Cancer Biology

Background:

  • p300 (E1A binding protein 300) and CBP (CREB-binding protein) are homologous histone acetyltransferases (HATs).
  • They act as transcriptional co-activators, regulating gene expression and cellular processes like proliferation and differentiation.
  • p300/CBP function is vital for normal development.

Purpose of the Study:

  • To review the regulatory mechanisms of p300/CBP HAT activity.
  • To discuss the role of p300/CBP dysregulation in cancer development.
  • To explore the therapeutic potential of p300/CBP inhibitors in cancer treatment.

Main Methods:

  • Review of existing literature on p300/CBP function, regulation, and involvement in cancer.
  • Analysis of somatic mutations affecting p300/CBP activity in various cancer types.
  • Discussion of emerging therapeutic strategies targeting p300/CBP.

Main Results:

  • Somatic mutations inactivating p300/CBP are common in cancers.
  • Translocations or truncations can lead to gain-of-function mutations, promoting tumor progression.
  • p300/CBP HAT activity is tightly regulated, and its dysregulation contributes to oncogenesis.

Conclusions:

  • p300/CBP are critical regulators whose dysregulation is implicated in cancer.
  • Understanding p300/CBP mechanisms offers insights into cancer development.
  • Inhibitors targeting p300/CBP represent a promising avenue for cancer therapy.
Keywords:
CBPP300TAZ2cancerhistone acetyltransferaseinhibitorsomatic mutationtruncation

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