EpiAxis science in detail
Lysine-specific demethylase 1 (LSD1, also known as KDM1A) is an epigenetic eraser enzyme that can remove methyl groups from lysine residues on histones H3K4me1/2 and H3K9me1/2. LSD1 is known to be aberrantly expressed in many cancers and is associated with inferior prognosis as this aberrant LSD1 expression contributes to impaired cellular differentiation and increased cancer cell proliferation, metastasis and invasiveness.
Importantly, LSD1 is enriched in both chemotherapy and immuno-therapy (IO) resistant cancers, facilitating tumour progression and recurrence.
Our research focus
Development of less toxic and more effective cancer therapies using epigenetics, with an initial focus of LSD1 and its role in cancer. EpiAxis is also developing a series of products targeting PKC theta and PD1/PDL1.
Novel mechanism of action: Nuclear translocation inhibition
Our nuclear translocation peptides are designed to:
1) Prevent the entry of LSD1 into the nucleus by binding to LSD1 nuclear shuttle proteins Importins 1 and 3; and
2) Then enter the nucleus to disrupt the LSD1/CoREST axis, leading to degradation of existing nuclear LSD1 pool. The net effect is a substantial reduction in the effective LSD1 nuclear pool leading to epigenetic change.
This is summarised below: