[HTML][HTML] Protein acetylation at the interface of genetics, epigenetics and environment in cancer
Metabolic reprogramming is an emerging hallmark of cancer and is driven by abnormalities
of oncogenes and tumor suppressors. Accelerated metabolism causes cancer cell …
of oncogenes and tumor suppressors. Accelerated metabolism causes cancer cell …
[HTML][HTML] Chemogenomics for drug discovery: Clinical molecules from open access chemical probes
RBA Quinlan, PE Brennan - RSC Chemical Biology, 2021 - pubs.rsc.org
In recent years chemical probes have proved valuable tools for the validation of disease-
modifying targets, facilitating investigation of target function, safety, and translation. Whilst …
modifying targets, facilitating investigation of target function, safety, and translation. Whilst …
Discovery of a highly selective BET BD2 inhibitor from a DNA-encoded library technology screening hit
F Rianjongdee, SJ Atkinson, CW Chung… - Journal of Medicinal …, 2021 - ACS Publications
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively
target one of the two bromodomains in the BET proteins, have begun to emerge in the …
target one of the two bromodomains in the BET proteins, have begun to emerge in the …
Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal …
LA Harrison, SJ Atkinson, A Bassil… - Journal of Medicinal …, 2021 - ACS Publications
Domain-specific BET bromodomain ligands represent an attractive target for drug discovery
with the potential to unlock the therapeutic benefits of antagonizing these proteins without …
with the potential to unlock the therapeutic benefits of antagonizing these proteins without …
Template-hopping approach leads to potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain (BD2) inhibitors
HE Aylott, SJ Atkinson, P Bamborough… - Journal of Medicinal …, 2021 - ACS Publications
A number of reports have recently been published describing the discovery and optimization
of bromo and extraterminal inhibitors which are selective for the second bromodomain …
of bromo and extraterminal inhibitors which are selective for the second bromodomain …
Bromodomain and extra-terminal motif (BET) inhibition is synthetic lethal with loss of SMAD4 in colorectal cancer cells via restoring the loss of MYC repression
C Shi, EJ Yang, Y Liu, PK Mou, G Ren, JS Shim - Oncogene, 2021 - nature.com
The tumor suppressor SMAD4 is frequently mutated in colorectal cancer (CRC). However,
no effective targeted therapies exist for CRC with SMAD4 loss. Here, we employed a …
no effective targeted therapies exist for CRC with SMAD4 loss. Here, we employed a …
The bromodomain inhibitor PFI-3 sensitizes cancer cells to DNA damage by targeting SWI/SNF
D Lee, DY Lee, YS Hwang, HR Seo, SA Lee… - Molecular Cancer …, 2021 - AACR
Many chemotherapeutic drugs produce double-strand breaks (DSB) on cancer cell DNA,
thereby inducing cell death. However, the DNA damage response (DDR) enables cancer …
thereby inducing cell death. However, the DNA damage response (DDR) enables cancer …
Brd4-bound enhancers drive cell-intrinsic sex differences in glioblastoma
Sex can be an important determinant of cancer phenotype, and exploring sex-biased tumor
biology holds promise for identifying novel therapeutic targets and new approaches to …
biology holds promise for identifying novel therapeutic targets and new approaches to …
Design, synthesis, and biological activity evaluation of a series of novel sulfonamide derivatives as BRD4 inhibitors against acute myeloid leukemia
Z Feng, A Chen, J Shi, D Zhou, W Shi, Q Qiu, X Liu… - Bioorganic …, 2021 - Elsevier
Accumulating researches have contributed much effect to discover novel chemotherapeutic
drug for leukemia with expeditious curative effect, of which bromodomain-containing protein …
drug for leukemia with expeditious curative effect, of which bromodomain-containing protein …
Inhibition of the bromodomain and extra-terminal family of epigenetic regulators as a promising therapeutic approach for gastric cancer
SK Kang, HJ Bae, WS Kwon, TS Kim, KH Kim, S Park… - Cellular Oncology, 2021 - Springer
Purpose Epigenetic dysregulation is a common characteristic of cancers, including gastric
cancer (GC), and contributes to cancer development and progression. Although the efficacy …
cancer (GC), and contributes to cancer development and progression. Although the efficacy …