[HTML][HTML] Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy

D Zhang, B Ma, D Liu, W Wu, T Zhou, Y Gao, C Yang… - …, 2024 - thelancet.com
Summary Background The E1A-associated protein p300 (p300) has emerged as a
promising target for cancer therapy due to its crucial role in promoting oncogenic signaling …

Paralogue-selective degradation of the lysine acetyltransferase EP300

X Chen, MKC Crawford, Y Xiong, AB Shaik, KF Suazo… - JACS Au, 2024 - ACS Publications
The transcriptional coactivators EP300 and CREBBP are critical regulators of gene
expression that share high sequence identity but exhibit nonredundant functions in basal …

p300/CBP degradation is required to disable the active AR enhanceosome in prostate cancer

J Luo, Z Chen, Y Qiao, JCY Tien, E Young, R Mannan… - bioRxiv, 2024 - biorxiv.org
Prostate cancer is an exemplar of an enhancer-binding transcription factor-driven disease.
The androgen receptor (AR) enhanceosome complex comprised of chromatin and …

CBP/p300 Degrader: A Promising Therapeutic Strategy for Treatment of Prostate Cancer and Beyond

J Hu, Y Xu - Journal of Medicinal Chemistry, 2024 - ACS Publications
Transcriptional coactivators CBP/p300 have emerged as potential targets for cancer
therapeutics. This Viewpoint discusses recent results that demonstrate an exceptionally …