Bromodomains: a new target class for drug development
AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
Therapeutic targets for cardiac fibrosis: from old school to next-gen
Cardiovascular diseases remain the leading cause of death worldwide, with pathological
fibrotic remodeling mediated by activated cardiac myofibroblasts representing a unifying …
fibrotic remodeling mediated by activated cardiac myofibroblasts representing a unifying …
Epigenetics of aging and aging-associated diseases
D Saul, RL Kosinsky - International journal of molecular sciences, 2021 - mdpi.com
Aging represents the multifactorial decline in physiological function of every living organism.
Over the past decades, several hallmarks of aging have been defined, including epigenetic …
Over the past decades, several hallmarks of aging have been defined, including epigenetic …
[HTML][HTML] 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, T Liu - Theranostics, 2022 - 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 …
sequence homology and functional overlap and co-operation, are emerging as critical …
Time-resolved analysis reveals rapid dynamics and broad scope of the CBP/p300 acetylome
The acetyltransferases CBP and p300 are multifunctional transcriptional co-activators. Here,
we combined quantitative proteomics with CBP/p300-specific catalytic inhibitors …
we combined quantitative proteomics with CBP/p300-specific catalytic inhibitors …
[HTML][HTML] Enhancer activity requires CBP/P300 bromodomain-dependent histone H3K27 acetylation
R Raisner, S Kharbanda, L Jin, E Jeng, E Chan… - Cell reports, 2018 - cell.com
Acetylation of histone H3 at lysine 27 is a well-defined marker of enhancer activity. However,
the functional impact of this modification at enhancers is poorly understood. Here, we use a …
the functional impact of this modification at enhancers is poorly understood. Here, we use a …
MLL-rearranged leukemias—an update on science and clinical approaches
AC Winters, KM Bernt - Frontiers in pediatrics, 2017 - frontiersin.org
The mixed-lineage leukemia 1 (MLL1) gene (now renamed Lysine [K]-specific
MethylTransferase 2A or KMT2A) on chromosome 11q23 is disrupted in a unique group of …
MethylTransferase 2A or KMT2A) on chromosome 11q23 is disrupted in a unique group of …
Transcriptional dependencies in diffuse intrinsic pontine glioma
S Nagaraja, NA Vitanza, PJ Woo, KR Taylor, F Liu… - Cancer cell, 2017 - cell.com
Diffuse intrinsic pontine glioma (DIPG) is a fatal pediatric cancer with limited therapeutic
options. The majority of cases of DIPG exhibit a mutation in histone-3 (H3K27M) that results …
options. The majority of cases of DIPG exhibit a mutation in histone-3 (H3K27M) that results …
Inhibitors of protein–protein interactions (PPIs): an analysis of scaffold choices and buried surface area
X Ran, JE Gestwicki - Current opinion in chemical biology, 2018 - Elsevier
Protein–protein interactions (PPI) were once considered 'undruggable', but clinical
successes, driven by advanced methods in drug discovery, have challenged that notion …
successes, driven by advanced methods in drug discovery, have challenged that notion …
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300
The enhancer factors CREB-binding protein (CBP) and p300 (also known as KAT3A and
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …