Targeting histone deacetylases for cancer therapy: Trends and challenges

T Liang, F Wang, RM Elhassan, Y Cheng… - … Pharmaceutica Sinica B, 2023 - Elsevier
Dysregulation of histone deacetylases (HDACs) is closely related to tumor development and
progression. As promising anticancer targets, HDACs have gained a great deal of research …

Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design

D Mi, Y Li, H Gu, Y Li, Y Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

Epigenetic control of pancreatic cancer metastasis

L Krauß, C Schneider, E Hessmann, D Saur… - Cancer and Metastasis …, 2023 - Springer
Surgical resection, when combined with chemotherapy, has been shown to significantly
improve the survival rate of patients with pancreatic ductal adenocarcinoma (PDAC) …

The application of PROTAC in HDAC

S Chen, Y Zheng, B Liang, Y Yin, J Yao, Q Wang… - European journal of …, 2023 - Elsevier
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great
opportunities for scientific research and industrial applications. Histone deacetylase (HDAC) …

Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects

J Ru, Y Wang, Z Li, J Wang, C Ren, J Zhang - European Journal of …, 2023 - Elsevier
Histone deacetylases (HDACs) catalyze the hydrolysis of acetyl-l-lysine side chains in
histones and non-histones, which are key to epigenetic regulation in humans. Targeting …

[HTML][HTML] Discovery of highly potent HDAC8 PROTACs with anti-tumor activity

C Zhao, D Chen, F Suo, R Setroikromo, WJ Quax… - Bioorganic …, 2023 - Elsevier
Various diseases are deeply associated with aberrations in HDAC8 functions. These
aberrations can be assigned to either structural functions or catalytic functions of HDAC8 …

Chemically induced degradation of epigenetic targets

M Kabir, X Yu, HÜ Kaniskan, J Jin - Chemical Society Reviews, 2023 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional small molecules that
induce the ternary complex formation between a protein-of-interest (POI) and an E3 ligase …

PROTACs: A novel strategy for cancer drug discovery and development

X Han, Y Sun - MedComm, 2023 - Wiley Online Library
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …

Proteomics‐Based Discovery of First‐in‐Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)

W Ji, WS Byun, W Lu, X Zhu… - Angewandte Chemie …, 2023 - Wiley Online Library
Chemical probes are essential tools for understanding biological systems and for
credentialing potential biomedical targets. Programmed cell death 2 (PDCD2) is a member …