HDAC6

HDAC6

A gene on chromosome Xp11.23 that encodes histone deacetylase 6; it belongs to class II of the histone deacetylase/acuc/apha family, which has histone deacetylase activity and represses transcription. HDAC6 plays a key role in degrading misfolded proteins too abundant for chaperone refolding and the ubiquitin-proteasome system by transporting the miscreants to aggresomes, which clear the misfoldizens by autophagy.
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These include programs in multiple indications for the orally bioavailable, HDAC6 selective inhibitor, ricolinostat (ACY-1215) and the company's HDAC1 inhibitor programme in orphan blood disorders such as sickle cell disease and beta-thalassemia.
The acquisition will provide Celgene with, among other things, worldwide rights to Acetylon's selective HDAC6 inhibitor programs and intellectual property in oncology, neurodegeneration, and autoimmune disease, including its lead drug candidates citarinostat (ACY-241) and ricolinostat (ACY-1215).
The TEPs address protein targets in cancer - HDAC6, SETDB1, PHIP, KDM3B, KDM4D, RECQL5, and malaria - PfBDP4B.
HDAC6 deacetylase activity is required for hypoxia-induced invadopodia formation and cell invasion.
Carbamazepine promotes Her-2 protein degradation in breast cancer cells by modulating HDAC6 activity and acetylation of Hsp90.
The new patent application is based on the ability of HDAC6 inhibitors to influence mechanisms both inside and outside of the cell nucleus.
Because recombinant HDAC6 binds directly to the protein phosphatase 1 (PP1) catalytic subunit, TSA disrupts endogenous HDAC6-PP1 complexes and activates PP1 (Brush et al.
Karus Therapeutics Ltd, a leader in the development of innovative medicines with breakthrough potential and originally a University of Southampton spin-out, has secured major investment to advance the company s proprietary PI3-Kinase p110 delta/beta and HDAC6 inhibitor programmes through early clinical trials in inflammation and cancer.
Por otra parte, el modulador HDAC6 de TGF-[beta]1 induce la transicion epitelio-mesenquimal, y juega un papel critico en la progresion tumoral (107).
Acetylon's intellectual property, which is being licensed from Harvard University and the Dana-Farber Cancer Institute, includes structural families of HDAC6 isoform-selective inhibitors, as well as a powerful and unique discovery and development platform for creating new selective HDAC inhibitors.
The Company's scientific excellence is reflected in its proprietary PI3K and HDAC6 inhibitor programmes, from which innovative small molecule drugs with significant clinical and commercial potential have been developed.