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 …
Bromodomain drug discovery–the past, the present, and the future
With the bromodomain (BRD) inhibitor JQ1, a remarkable success story of BRD4 as a novel
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …
Photoinduced hydroarylation and cyclization of alkenes with luminescent platinum (II) complexes
H Cheng, TL Lam, Y Liu, Z Tang… - Angewandte Chemie, 2021 - Wiley Online Library
Photoinduced hydroarylation of alkenes is an appealing synthetic strategy for arene
functionalization. Herein, we demonstrated that aryl radicals generated from electron …
functionalization. Herein, we demonstrated that aryl radicals generated from electron …
Reset of inflammatory priming of joint tissue and reduction of the severity of arthritis flares by bromodomain inhibition
J Friščić, C Reinwald, M Böttcher… - Arthritis & …, 2023 - Wiley Online Library
Objective We have recently shown that priming of synovial fibroblasts (SFs) drives arthritis
flares. Pathogenic priming of SFs is essentially mediated by epigenetic reprogramming …
flares. Pathogenic priming of SFs is essentially mediated by epigenetic reprogramming …
Fatty Acids Support the Fitness and Functionality of Tumor-Resident CD8+ T Cells by Maintaining SCML4 Expression
M Feng, X Liu, X Hao, Y Ren, G Dong, J Tian, Y Wang… - Cancer Research, 2023 - AACR
CD8+ tissue-resident memory T (Trm) cells and tumor-infiltrating lymphocytes (TIL) regulate
tumor immunity and immune surveillance. Characterization of Trm cells and TILs could help …
tumor immunity and immune surveillance. Characterization of Trm cells and TILs could help …
Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
K Klein - RMD open, 2018 - rmdopen.bmj.com
The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra …
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra …
BRPF1-KAT6A/KAT6B complex: molecular structure, biological function and human disease
G Zu, Y Liu, J Cao, B Zhao, H Zhang, L You - Cancers, 2022 - mdpi.com
Simple Summary BRPF1 (also named as BR140) was identified 28 years ago, and it was not
until the past 5 years that its mutations in humans caught increasing attention. Those …
until the past 5 years that its mutations in humans caught increasing attention. Those …
Targeting epigenetic regulation for cancer therapy using small molecule inhibitors
A Kumar, L Emdad, PB Fisher, SK Das - Advances in Cancer Research, 2023 - Elsevier
Cancer cells display pervasive changes in DNA methylation, disrupted patterns of histone
posttranslational modification, chromatin composition or organization and regulatory …
posttranslational modification, chromatin composition or organization and regulatory …
Advancements in the Development of Non‐BET Bromodomain Chemical Probes
MA Clegg, NCO Tomkinson, RK Prinjha… - …, 2019 - Wiley Online Library
The bromodomain and extra terminal (BET) family of bromodomain‐containing proteins
(BCPs) have been the subject of extensive research over the past decade, resulting in a …
(BCPs) have been the subject of extensive research over the past decade, resulting in a …
Discovery of dual TAF1-ATR inhibitors and ligand-induced structural changes of the taf1 tandem bromodomain
RM Karim, L Yang, L Chen, MJ Bikowitz… - Journal of Medicinal …, 2022 - ACS Publications
Bromodomains regulate chromatin remodeling and gene transcription through recognition of
acetylated lysines on histones and other proteins. Bromodomain-containing protein TAF1, a …
acetylated lysines on histones and other proteins. Bromodomain-containing protein TAF1, a …