Image-Guided Synthesis Reveals Potent Blood-Brain Barrier Permeable Histone Deacetylase Inhibitors

Butyrate Histone Deacetylase Inhibitors

In addition to being a part of the metabolic fatty acid fuel cycle, butyrate is also capable of inducing growth arrest in a variety of normal cell types and senescence-like phenotypes in gynecological cancer cells, inhibiting DNA synthesis and cell growth in colonic tumor cell lines, suppressing hTERT mRNA expression and telomerase activity in human prostate cancer cells, and inducing stem cell...

Intercellular transfer of P-glycoprotein in human blood-brain barrier endothelial cells is increased by histone deacetylase inhibitors

The blood-brain barrier (BBB) controls the entry of compounds into the brain, thereby regulating brain homeostasis. Efflux transporters such as P-glycoprotein (Pgp) significantly contribute to BBB function. Multiple signaling pathways modulate the expression and activity of Pgp in response to xenobiotics and disease. A non-genetic way of intercellular transfer of Pgp occurs in cancer cells, but...

FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors.

The purpose of this work--the first of its kind--was to evaluate the impact of chronic selective histone deacetylase (HDAC) inhibitor treatment on brain activity using uptake of the radioligand (18)F-fluorodeoxyglucose and positron emission tomography ((18)FDG-PET). HDAC dysfunction and other epigenetic mechanisms are implicated in diverse CNS disorders and animal research suggests HDAC inhibit...

Largazole Analogues as Histone Deacetylase Inhibitors: Synthesis and Biological Evaluation

A. Al-Hamashi, J. Almaliti, R. Farrell, V. L. Tillekeratne University of Toledo Purpose Histone deacetylase (HDAC) enzymes, which are overexpressed in many cancer tissues, present a potential target for cancer chemotherapy.HDAC inhibitors (HDACis) are currently being investigated as potential anticancer agents. Most of the current HDACis are not selective and have high potential toxicity. Selec...

Molecular Design, Synthesis and Simulation of Histone Deacetylase Inhibitors