Recent advances in dual PROTACs degrader strategies for disease treatment

J Liu, Y Liu, J Tang, Q Gong, G Yan, H Fan… - European Journal of …, 2024‏ - Elsevier
Proteolysis-targeting chimeras (PROTACs) is regarded as an emerging therapeutic strategy
with unlimited potential because of its mechanism of inducing target protein degradation …

Discovery of CW-3308 as a Potent, Selective, and Orally Efficacious PROTAC Degrader of BRD9

C Wang, M Wang, Y Wang, RK Rej… - Journal of Medicinal …, 2024‏ - ACS Publications
The bromodomain-containing protein BRD9 has emerged as an attractive therapeutic target.
In the present study, we successfully identified a number of highly potent BRD9 degraders …

[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 …

Discovery of sd-436: a potent, highly selective and efficacious stat3 protac degrader capable of achieving complete and long-lasting tumor regression

R Xu, H Zhou, L Bai, D McEachern, D Wu… - Journal of Medicinal …, 2024‏ - ACS Publications
STAT3 is an attractive therapeutic target for cancer and other human diseases. We have
previously reported the discovery of potent, selective, and efficacious PROTAC STAT3 …

Discovery of a Highly Potent PROTAC Degrader of p300/CBP Proteins for the Treatment of Enzalutamide-Resistant Prostate Cancer

M Ma, M Li, C Zhang, Z Yang, X Chen… - Journal of Medicinal …, 2024‏ - ACS Publications
Prostate cancer therapies against androgen receptor (AR) eventually develop lethal
resistance; thus, exploring new therapeutic approaches is urgent for prostate cancer …

Dysregulation of the p300/CBP histone acetyltransferases in human cancer

L Xu, H Xuan, X Shi - Epigenomics, 2025‏ - Taylor & Francis
ABSTRACT p300 (E1A binding protein 300) and CBP (CREB-binding protein) are critical
regulators of chromatin dynamics and gene expression, playing essential roles in various …

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

J Luo, Z Chen, Y Qiao, JCY Tien, E Young… - …, 2024‏ - pmc.ncbi.nlm.nih.gov
Prostate cancer is an exemplar of an enhancer-binding transcription factor-driven disease.
The androgen receptor (AR) enhanceosome complex comprised of chromatin and …

Paralogue-selective degradation of the lysine acetyltransferase EP300

X Chen, MKC Crawford, Y **ong, 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 …

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 …

Discovery of an EP300 Inhibitor using Structure-based Virtual Screening and Bioactivity Evaluation

D Pan, Y Huang, D Jiang, Y Zhang… - Current …, 2024‏ - benthamdirect.com
Background: EP300 (E1A binding protein p300) played a significant role in serial diseases
such as cancer, neurodegenerative disease. Therefore, it became a significant target …