HDAC inhibitors still need a home run, despite recent approval

  title={HDAC inhibitors still need a home run, despite recent approval},
  author={Malini Guha},
  journal={Nature Reviews Drug Discovery},
  • Malini Guha
  • Published 1 April 2015
  • Psychology, Medicine
  • Nature Reviews Drug Discovery
A beleaguered class of epigenetic modulators continues to struggle for oncology success, but new insights into their mechanisms in cancer may yet offer hope. 
HDAC inhibitors still need a home run, despite recent approval
It is shown that mocetinostat is an inhibitor of class I histone deacetylases (HDACs) and also an inhibitors of HDAC11, which is in class IV.
Recent advances in small molecular modulators targeting histone deacetylase 6
Histone deacetylase 6 (HDAC6) is a unique isozyme in the HDAC family with various distinguished characters. HDAC6 is predominantly localized in the cytoplasm and has several specific nonhistone sub...
Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors.
A mini library of HDAC inhibitors with peptoid-based cap groups was synthesized using an efficient multicomponent approach and the most potent HDAC6 inhibitor revealed remarkable chemosensitizing properties and completely reverted the cisplatin resistance in Cal27 CisR cells.
Histone Deacetylase Inhibitors: A Prospect in Drug Discovery
Due to gene expression, an impending requirement to prudently transfer cytotoxicity to cancerous cells, HDAC inhibitors may be developed as anticancer agents.
Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs.
XZ9002 is more effective to inhibit cancer cell proliferation than its proteolysis-inactive counterpart, suggesting HDAC3 degradation is a novel and promising anticancer approach.
PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes.
The authors' PROTAC increased histone acetylation levels and compromised colon cancer HCT116 cell viability, establishing a degradation strategy as an alternative to class I HDAC inhibition.
The Histone Deacetylase Inhibitor Entinostat/Syndax 275 in Osteosarcoma.
Clinical trials are in development to evaluate this combination of gemcitabine and HDAC inhibitor, entinostat/Syndax 275, as a potential treatment option for patients with refractory osteosarcoma.
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
Prodrug 13 has therapeutic potential as a new class of anticancer agent for further clinical translation after demonstrating excellent in vivo anticancer activities in a human prostate carcinoma xenograft model with no observed toxicity.
The Roadmap Epigenomics Project opens new drug development avenues
The US National Institutes of Health's US$240-million epigenomics investment could improve the study of disease biology, the identification of new targets, the validation of animal models and more.
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.