|
Givinostat
Givinostat (International Nonproprietary Name, INN) or gavinostat (originally ITF2357) is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Givinostat is in numerous phase II clinical trials (including for relapsed leukemias and myelomas), and has been granted orphan drug designation in the European Union for the treatment of juvenile idiopathic arthritis, systemic juvenile idiopathic arthritis, polycythaemia vera. and Duchenne muscular dystrophy. A preclinical study produced early results suggesting the molecule might help with diastolic dysfunction. ITF2357 was discovered at :it:Italfarmaco, Italfarmaco of Milan, Italy. It was patented in 1997 and first described in the scientific literature in 2005. Adverse effects In clinical trials of givinostat as a salvage therapy for advanced Hodgkin's lymphoma, the most common adverse drug reaction, adverse reactions ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Histone Deacetylase Inhibitor
Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. HDIs have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics. More recently they are being investigated as possible treatments for cancers, parasitic and inflammatory diseases. Cellular biochemistry/pharmacology To carry out gene expression, a cell must control the coiling and uncoiling of DNA around histones. This is accomplished with the assistance of histone acetyl transferases (HAT), which acetylate the lysine residues in core histones leading to a less compact and more transcriptionally active euchromatin, and, on the converse, the actions of histone deacetylases (HDAC), which remove the acetyl groups from the lysine residues leading to the formation of a condensed and transcriptionally silenced chromatin. Reversible modification of the terminal tails of core histones constitutes the major epigenetic mechanism for re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |