[HTML][HTML] The world of protein acetylation

A Drazic, LM Myklebust, R Ree, T Arnesen - Biochimica et Biophysica Acta …, 2016 - Elsevier
Acetylation is one of the major post-translational protein modifications in the cell, with
manifold effects on the protein level as well as on the metabolome level. The acetyl group …

Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

Targeting the p300/CBP axis in lethal prostate cancer

J Welti, A Sharp, N Brooks, W Yuan, C McNair… - Cancer Discovery, 2021 - AACR
Resistance to androgen receptor (AR) blockade in castration-resistant prostate cancer
(CRPC) is associated with sustained AR signaling, including through alternative splicing of …

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

LM Lasko, CG Jakob, RP Edalji, W Qiu, D Montgomery… - Nature, 2017 - nature.com
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases
(HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of …

[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 …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012 - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

Metabolic regulation of histone post-translational modifications

J Fan, KA Krautkramer, JL Feldman… - ACS chemical …, 2015 - ACS Publications
Histone post-translational modifications regulate transcription and other DNA-templated
functions. This process is dynamically regulated by specific modifying enzymes whose …

Targeting CDK9 reactivates epigenetically silenced genes in cancer

H Zhang, S Pandey, M Travers, H Sun, G Morton… - Cell, 2018 - cell.com
Summary Cyclin-dependent kinase 9 (CDK9) promotes transcriptional elongation through
RNAPII pause release. We now report that CDK9 is also essential for maintaining gene …

Use of epigenetic drugs in disease: an overview

S Heerboth, K Lapinska, N Snyder… - Genetics & …, 2014 - journals.sagepub.com
Epigenetic changes such as DNA methylation and histone methylation and acetylation alter
gene expression at the level of transcription by upregulating, downregulating, or silencing …

Androgen receptor signaling in prostate cancer

Z Culig, FR Santer - Cancer and Metastasis Reviews, 2014 - Springer
The androgen receptor (AR), ligand-induced transcription factor, is expressed in primary
prostate cancer and in metastases. AR regulates multiple cellular events, proliferation …