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- Papers of special note have been highlighted as either of interest (•) or of considerable interest (••) to readers.
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•This review is an excellent summary of the activity assays applied to TG2 and the therapeutic potential of its inhibition.
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•This recent review presents many of the same inhibitors from the academic literature.
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•This review presents irreversible TG2 inhibitors, classed according to their warhead, including their chemical mechanisms of action.
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••The warheads and scaffolds divulged in this patent continue to inspire inhibitor design to this day.
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• This English version of WO0236798 is itself an excellent review of preceding patents.
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• This is the first patent application for reversible inhibitors of TG2.
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• This is the first patent application for antibody inhibitors of TG2.
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•• This patent discloses the first TGase inhibitor to be entered into clinical trials.
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