Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress

ME Neganova, SG Klochkov, YR Aleksandrova… - Seminars in Cancer …, 2022 - Elsevier
Epigenetic changes associated with histone modifications play an important role in the
emergence and maintenance of the phenotype of various cancer types. In contrast to direct …

Function and mechanism of novel histone posttranslational modifications in health and disease

H Xu, M Wu, X Ma, W Huang… - BioMed Research …, 2021 - Wiley Online Library
Histone posttranslational modifications (HPTMs) are crucial epigenetic mechanisms
regulating various biological events. Different types of HPTMs characterize and shape …

Development of 2 bromodomain and extraterminal inhibitors with distinct pharmacokinetic and pharmacodynamic profiles for the treatment of advanced malignancies

G Falchook, S Rosen, P LoRusso, J Watts, S Gupta… - Clinical Cancer …, 2020 - AACR
Purpose: Bromodomain and extraterminal (BET) proteins are key epigenetic transcriptional
regulators, inhibition of which may suppress oncogene expression. We report results from 2 …

[HTML][HTML] Advancements in the treatment of triple-negative breast cancer: A narrative review of the literature

I Landry, V Sumbly, M Vest - Cureus, 2022 - ncbi.nlm.nih.gov
Triple-negative breast cancers (TNBCs) are aggressive tumors that are more common in
young women, African American populations, and those with hereditary mutations. These …

A phase I study of pelabresib (CPI-0610), a small-molecule inhibitor of BET proteins, in patients with relapsed or refractory lymphoma

KA Blum, JG Supko, MB Maris, IW Flinn, A Goy… - Cancer Research …, 2022 - AACR
Purpose: NF-κB, a transcription factor essential for inflammatory responses, is constitutively
activated in many lymphomas. In preclinical studies, pelabresib (CPI-0610), an …

Systematically mitigating the p38α activity of triazole-based BET inhibitors

AS Carlson, H Cui, A Divakaran… - ACS Medicinal …, 2019 - ACS Publications
The Bromodomain and Extra Terminal (BET) family of proteins recognize post-translational
N-ε-acetylated lysine modifications, regulating transcription as “reader” proteins …

Role of BET inhibitors in triple negative breast cancers

D Khandekar, V Tiriveedhi - Cancers, 2020 - mdpi.com
Bromodomain and extraterminal domain (BET) proteins have evolved as key multifunctional
super-regulators that control gene expression. These proteins have been shown to …

Fragment hotspot mapping to identify selectivity-determining regions between related proteins

MD Smilova, PR Curran, CJ Radoux… - Journal of Chemical …, 2022 - ACS Publications
Selectivity is a crucial property in small molecule development. Binding site comparisons
within a protein family are a key piece of information when aiming to modulate the selectivity …

Review on: BRD4 inhibitors for anticancer research

VV Singh, S Alauddin - Human Gene, 2023 - Elsevier
Abstract Treatment of cancer is now in a phase of new possibilities, and with the targeted
therapy, the advancement of the therapy is considered as the next generation of cancer …

OTX015 epi-drug exerts antitumor effects in ovarian cancer cells by blocking GNL3-mediated radioresistance mechanisms: Cellular, molecular and computational …

F Megiorni, S Camero, P Pontecorvi, L Camicia… - Cancers, 2021 - mdpi.com
Simple Summary The outcome for women diagnosed with ovarian cancer (OC), the most
aggressive gynecological tumor worldwide, remains very poor. Encouraging therapeutic …