New and emerging HDAC inhibitors for cancer treatment.
TLDR
The influence of aberrantly regulated histone deacetylases (HDACs) in tumorigenesis is discussed and HDAC inhibitors targeting class I, II, and IV HDACs that are currently under development for use as anticancer agents are examined.Abstract:
Epigenetic enzymes are often dysregulated in human tumors through mutation, altered expression, or inappropriate recruitment to certain loci. The identification of these enzymes and their partner proteins has driven the rapid development of small-molecule inhibitors that target the cancer epigenome. Herein, we discuss the influence of aberrantly regulated histone deacetylases (HDACs) in tumorigenesis. We examine HDAC inhibitors (HDACis) targeting class I, II, and IV HDACs that are currently under development for use as anticancer agents following the FDA approval of two HDACis, vorinostat and romidepsin.read more
Citations
More filters
Journal ArticleDOI
Combination therapy in combating cancer.
Reza Bayat Mokhtari,Reza Bayat Mokhtari,Tina S. Homayouni,Narges Baluch,Evgeniya Morgatskaya,Sushil Kumar,Bikul Das,Herman Yeger +7 more
TL;DR: An approach that combines repurposed pharmaceutical agents with other therapeutics has shown promising results in mitigating tumour burden, and this systematic review discusses important pathways commonly targeted in cancer therapy.
Journal ArticleDOI
Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders
TL;DR: The development of small-molecule HDAC inhibitors and their use in the laboratory, in preclinical models and in the clinic are highlighted.
Journal ArticleDOI
Histone Deacetylase Inhibitors as Anticancer Drugs.
TL;DR: Different classes of HDAC inhibitors, mechanisms of their actions and novel results of preclinical and clinical studies are summarized, including the combination with other therapeutic modalities are discussed.
Journal ArticleDOI
Epigenetic Determinants of Cancer
Stephen B. Baylin,Peter A. Jones +1 more
TL;DR: Epigenetic therapies are one standard of care for a preleukemic disorder and form of lymphoma and the application of epigenetic therapies in the treatment of solid tumors is also emerging as a viable therapeutic route.
Journal ArticleDOI
HDACs and HDAC Inhibitors in Cancer Development and Therapy
Yixuan Li,Edward Seto +1 more
TL;DR: The role of HDACs in cancer and the therapeutic potential ofHDAC inhibitors (HDACi) as emerging drugs in cancer treatment are discussed.
References
More filters
Journal ArticleDOI
ONCOMINE: A Cancer Microarray Database and Integrated Data-Mining Platform
Daniel R. Rhodes,Jianjun Yu,K. Shanker,Nandan P. Deshpande,Radhika Varambally,Debashis Ghosh,Terrence R. Barrette,Akhilesh Pandey,Arul M. Chinnaiyan +8 more
TL;DR: ONCOMINE is presented, a cancer microarray database and web-based data-mining platform aimed at facilitating discovery from genome-wide expression analyses and novel biomarkers and therapeutic targets are discovered.
Journal ArticleDOI
Anticancer activities of histone deacetylase inhibitors.
TL;DR: Recent advances in the understanding of the molecular events that underlie the anticancer effects of HDAC inhibitors are summarized and how such information could be used in optimizing the development and application of these agents in the clinic, either as monotherapies or in combination with other anticancer drugs are discussed.
Journal ArticleDOI
HDAC6 is a microtubule-associated deacetylase
Charlotte Hubbert,Amaris Guardiola,Rong Shao,Yoshiharu Kawaguchi,Akihiro Ito,Andrew B. Nixon,Minoru Yoshida,Xiao-Fan Wang,Tso-Pang Yao +8 more
TL;DR: The results show that HDAC6 is the tubulin deacetylase, and provide evidence that reversible acetylation regulates important biological processes beyond histone metabolism and gene transcription, including microtubule-dependent cell motility.
Journal ArticleDOI
Loss of acetylation at Lys16 and trimethylation at Lys20 of histone H4 is a common hallmark of human cancer
Mario F. Fraga,Esteban Ballestar,Ana Villar-Garea,Manuel Boix-Chornet,Jesús Espada,Gunnar Schotta,Tiziana Bonaldi,Claire E. Haydon,Santiago Ropero,Kevin Petrie,N. Gopalakrishna Iyer,Alberto Pérez-Rosado,Enrique Calvo,Juan Antonio López,Amparo Cano,María José Calasanz,Dolors Colomer,Miguel A. Piris,Natalie G. Ahn,Natalie G. Ahn,Axel Imhof,Carlos Caldas,Thomas Jenuwein,Manel Esteller +23 more
TL;DR: It is found that cancer cells had a loss of monoacetylated and trimethylated forms of histone H4 early and accumulated during the tumorigenic process, which is a common hallmark of human tumor cells.
Journal ArticleDOI
Acetylation and deacetylation of non-histone proteins
TL;DR: This review will focus on these non-histone targets of HATs and HDACs and the consequences of their modification.