[HTML][HTML] The world of protein acetylation
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 …
manifold effects on the protein level as well as on the metabolome level. The acetyl group …
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 …
(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 …
(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
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 …
targeted therapies. The cytosine deaminase APOBEC proteins have been implicated in the …
Epigenetic protein families: a new frontier for drug discovery
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …
establishes normal cellular phenotypes but also contributes to human diseases. At the …
Metabolic regulation of histone post-translational modifications
Histone post-translational modifications regulate transcription and other DNA-templated
functions. This process is dynamically regulated by specific modifying enzymes whose …
functions. This process is dynamically regulated by specific modifying enzymes whose …
Targeting CDK9 reactivates epigenetically silenced genes in cancer
Summary Cyclin-dependent kinase 9 (CDK9) promotes transcriptional elongation through
RNAPII pause release. We now report that CDK9 is also essential for maintaining gene …
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 …
gene expression at the level of transcription by upregulating, downregulating, or silencing …
Androgen receptor signaling in prostate cancer
The androgen receptor (AR), ligand-induced transcription factor, is expressed in primary
prostate cancer and in metastases. AR regulates multiple cellular events, proliferation …
prostate cancer and in metastases. AR regulates multiple cellular events, proliferation …