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 …
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 …
been extensively concerned in recent years. Over 20 years development, accumulated …
Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
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) …
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) …
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 …
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
Various diseases are deeply associated with aberrations in HDAC8 functions. These
aberrations can be assigned to either structural functions or catalytic functions of HDAC8 …
aberrations can be assigned to either structural functions or catalytic functions of HDAC8 …
Chemically induced degradation of epigenetic targets
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional small molecules that
induce the ternary complex formation between a protein-of-interest (POI) and an E3 ligase …
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
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …
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)
Chemical probes are essential tools for understanding biological systems and for
credentialing potential biomedical targets. Programmed cell death 2 (PDCD2) is a member …
credentialing potential biomedical targets. Programmed cell death 2 (PDCD2) is a member …