Protein acylation: mechanisms, biological functions and therapeutic targets

S Shang, J Liu, F Hua - Signal transduction and targeted therapy, 2022 - nature.com
Metabolic reprogramming is involved in the pathogenesis of not only cancers but also
neurodegenerative diseases, cardiovascular diseases, and infectious diseases. With the …

Targeting signaling pathways in prostate cancer: mechanisms and clinical trials

Y He, W Xu, YT **ao, H Huang, D Gu… - Signal transduction and …, 2022 - nature.com
Prostate cancer (PCa) affects millions of men globally. Due to advances in understanding
genomic landscapes and biological functions, the treatment of PCa continues to improve …

Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents

Q Chen, B Yang, X Liu, XD Zhang, L Zhang… - Theranostics, 2022 - pmc.ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …

Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies

L Nicosia, GJ Spencer, N Brooks, FMR Amaral… - Cancer Cell, 2023 - cell.com
CCS1477 (inobrodib) is a potent, selective EP300/CBP bromodomain inhibitor which
induces cell-cycle arrest and differentiation in hematologic malignancy model systems. In …

Epigenetics-targeted drugs: Current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

[HTML][HTML] Loss of SYNCRIP unleashes APOBEC-driven mutagenesis, tumor heterogeneity, and AR-targeted therapy resistance in prostate cancer

X Li, Y Wang, S Deng, G Zhu, C Wang, NA Johnson… - Cancer Cell, 2023 - cell.com
Tumor mutational burden and heterogeneity has been suggested to fuel resistance to many
targeted therapies. The cytosine deaminase APOBEC proteins have been implicated in the …

Discovery of CBPD-268 as an exceptionally potent and orally efficacious CBP/p300 PROTAC degrader capable of achieving tumor regression

Z Chen, M Wang, D Wu, L Bai, T Xu… - Journal of Medicinal …, 2024 - ACS Publications
CBP/p300 proteins are key epigenetic regulators and promising targets for the treatment of
castration-resistant prostate cancer and other types of human cancers. Herein, we report the …

A new old target: androgen receptor signaling and advanced prostate cancer

D Westaby, MLD Fenor de La Maza… - Annual review of …, 2022 - annualreviews.org
Owing to the development of multiple novel therapies, there has been major progress in the
treatment of advanced prostate cancer over the last two decades; however, the disease …

[HTML][HTML] Histone lysine acetyltransferase inhibitors: an emerging class of drugs for cancer therapy

J White, FA Derheimer, K Jensen-Pergakes… - Trends in …, 2024 - cell.com
Lysine acetyltransferases (KATs) are a family of epigenetic enzymes involved in the
regulation of gene expression; they represent a promising class of emerging drug targets …