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Introduction

HDAC6 selective inhibitors

Histone N-terminal tails are crucial in helping to maintain chromatin stability and are subject to numerous modifications such as acetylation; histone acetylation tends to open up chromatin structures therefore histone acetyl transferases (HATs) generally are transcriptional activators whereas histone deacetylases (HDACs) tend to be repressors. HDACs are an important target in cancer epigenetics. Quimatryx is making excellent progress in the design and development of potent isoform selective HDAC inhibitors, specially HDAC6 inhibitors.

HDAC6 has Important roles in cancer development, as it is essential for the oncogenic transformation of primary cells and the malignant growth of cancer cells. It also regulates tumour cell proliferation and survival, promotes cancer migration and has been related to metastasis.

The increase in the suppressive activity of Tregs, via HDAC6 inhibition, is an important target to treat autoinmune diseases, such as multiple sclerosis. Moreover, HDAC6 has been linked with neurodegenerative disorders, as Alzheimer, Parkinson and dementia.

Moreover, low toxicity is expected when inhibiting HDAC6. An study with HDAC6-null mice has shown that is not an essential gene, as those mice are normal. Besides, synergistic activity with important marketed chemotherapeutics decreases the dose regime and, therefore, the toxicity of the treatment

 

   QUIMATRYX

   Paseo Mikeletegi 69, 3┬¬ planta

   20009 San Sebasti├ín

   Tel: 946 08 70 37

   www.quimatryx.com