Targets
TheraCryf is focused on developing products to address areas of high unmet need in oncology and behavioural brain disorders.SFX-01
- STAT3 and pSTAT3 – STAT3 (signal transducer and activator of transcription 3) and phospho STAT3 (pSTAT3) has importance in controlling cancer metastases. Malfunction in these pathways has been implicated in a number of cancers including breast cancer. Research is ongoing into the role of SFX-01 and its inhibition of STAT3/ pSTAT3 in relation to the development of resistance to other therapeutic options.
- Nrf2 (nuclear factor erythroid 2-related factor 2) is a transcription factor that is associated with a broad range of diseases characterised by excessive oxidative stress. Nrf2 regulates many target genes including those used in encoding proteins involved in the cellular antioxidant response, damage repair, protein homeostasis and maintenance of metabolic balance. SFX-01 inactivates a protein associated with regulating Nrf2, known as KEAP1 (Kelch-like ECH-associated protein 1), allowing accumulation of Nrf2 and an increase in expression of target genes, potentially improving the cellular response to inflammatory and fibrotic challenges.
- SHP2 (Src homology-2 domain-containing protein tyrosine phosphatase-2) is involved in several cancer-related processes, including cancer cell invasion and metastasis, apoptosis, DNA damage, cell proliferation, cell cycle and drug resistance. SHP2 may therefore be a therapeutic target of great potential. In-vitro and in-vivo data demonstrates that SFX-01 modifies SHP2, inhibiting its phosphatase activity which is implicated in many aspects of solid tumour and haematological cancers.
Highly Selective Orexin 1 Receptor Antagonist (Ox-1)
Orexin has a role in reward, feeding behaviour & anxiety and, via the Ox2 receptor, also has a role in sleep. Receptors are found in the hypothalamus, enteric nervous system and gut. Orexigenic signalling via the Ox1 receptor has been implicated in several addictive disorders including binge eating disorder (BED) and alcohol use disorder (AUD).
Proof of concept data has been generated in a rodent model of BED with TheraCryf’s candidate Ox1 antagonist.
Clinical trials using orexin 1 antagonists have demonstrated alleviation of panic and anxiety in human models of these conditions.
Atypical Inhibitor of the Brain Dopamine Active Transporter (DAT)
Dopamine has a role in alertness amongst its other functions in the central nervous system. A gradual increase in brain dopamine without fast release of dopamine (as caused by amphetamines) is expected to cause alleviation of symptoms of fatigue and narcolepsy.
Proof concept data has been generated in rodent models of fatigue and of narcolepsy using TheraCryf’s candidate atypical DAT inhibitor.