Thirty years of HDAC inhibitors: 2020 insight and hindsight

TCS Ho, AHY Chan, A Ganesan - Journal of medicinal chemistry, 2020 - ACS Publications
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …

The emergence of drug resistance to targeted cancer therapies: Clinical evidence

AB Sarmento-Ribeiro, A Scorilas, AC Gonçalves… - Drug Resistance …, 2019 - Elsevier
For many decades classical anti-tumor therapies included chemotherapy, radiation and
surgery; however, in the last two decades, following the identification of the genomic drivers …

Epigenetic regulation of energy metabolism in obesity

W Gao, JL Liu, X Lu, Q Yang - Journal of molecular cell biology, 2021 - academic.oup.com
Obesity has reached epidemic proportions globally. Although modern adoption of a
sedentary lifestyle coupled with energy-dense nutrition is considered to be the main cause …

Histone 4 lysine 5/12 acetylation enables developmental plasticity of Pristionchus mouth form

MS Werner, T Loschko, T King, S Reich… - nature …, 2023 - nature.com
Abstract Development can be altered to match phenotypes with the environment, and the
genetic mechanisms that direct such alternative phenotypes are beginning to be elucidated …

Spatiotemporal and global profiling of DNA–protein interactions enables discovery of low-affinity transcription factors

AD Guo, KN Yan, H Hu, L Zhai, TF Hu, H Su, Y Chi… - Nature Chemistry, 2023 - nature.com
Precise dissection of DNA–protein interactions is essential for elucidating the recognition
basis, dynamics and gene regulation mechanism. However, global profiling of weak and …

Therapies targeting epigenetic alterations in acute kidney injury-to-chronic kidney disease transition

F Tanemoto, I Mimura - Pharmaceuticals, 2022 - mdpi.com
Acute kidney injury (AKI) was previously thought to be a merely transient event; however,
recent epidemiological evidence supports the existence of a causal relationship between …

[HTML][HTML] Epigenetic regulation in macrophage migration inhibitory factor (MIF)-mediated signaling in cancer and inflammation

A Osipyan, D Chen, FJ Dekker - Drug discovery today, 2021 - Elsevier
Highlights•Macrophage migration inhibitory factor (MIF) plays a crucial role in cancer and
inflammatory diseases.•Epigenetic mechanisms are involved in MIF-mediated …

Activity-based DNA-encoded library screening

WG Cochrane, ML Malone, VQ Dang… - ACS combinatorial …, 2019 - ACS Publications
Robotic high-throughput compound screening (HTS) and, increasingly, DNA-encoded
library (DEL) screening are driving bioactive chemical matter discovery in the postgenomic …

H3K18Ac as a marker of cancer progression and potential target of anti-cancer therapy

M Hałasa, A Wawruszak, A Przybyszewska, A Jaruga… - Cells, 2019 - mdpi.com
Acetylation and deacetylation are posttranslational modifications (PTMs) which affect the
regulation of chromatin structure and its remodeling. Acetylation of histone 3 at lysine placed …

HDAC inhibitors enhance the anti-tumor effect of immunotherapies in hepatocellular carcinoma

C Shen, M Li, Y Duan, X Jiang, X Hou, F Xue… - Frontiers in …, 2023 - frontiersin.org
Hepatocellular carcinoma (HCC), the most common liver malignancy with a poor prognosis
and increasing incidence, remains a serious health problem worldwide. Immunotherapy has …