It's been a busy week for publications. This has just been published by a team at Oxford University in the UK (with collaboration and partial funding from Hong Kong). https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.1c01204
A very large research team from a high profile institution is looking to develop their own FTO inhibitors. I don't have time right now to pick the paper apart in detail but after a skim read one thing jumped right out at me:
The paper claims that this molecule (FG-2216) is the most potent FTO inhibitor identified with an IC50 of 3μM. The reference links to this paper which I don't have access to, but importantly was published in 2010. A little outdated in the field of FTO inhibitors I think. Comparatively, Zantrene is 0.146μM making it over 20 times as potent as FG-2216. I'm scratching my head to understand why these research teams continue to overlook Zantrene when listing current known inhibitors. Could it really be as Dr T has suggested, that teams wanting to find inhibitors would remove the need for their own funding by acknowledging a potent, selective inhibitor is already in the clinic? I can understand little groups doing it, but it feels off to see Oxford completely overlook Zantrene here. Maybe I'm just trying too hard to poke a hole in my investment thesis.
@RaceOncology could you shed any further light on why we have only seen one study (Chicago Paper) of many published that have acknowledged Zantrene as a relevant inhibitor of FTO?
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