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Expert Opinion on Therapeutic Patents Volume 26, 2016 - Issue 1
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Reviews

Transglutaminase inhibitors: a patent review

Jeffrey W. KeillorDepartment of Chemistry and Biomolecular Sciences, University of Ottawa, 10 Marie-Curie, Ottawa, OntarioK1N 6N5, CanadaCorrespondence[email protected]
&
Kim Y.P. ApperleyDepartment of Chemistry and Biomolecular Sciences, University of Ottawa, 10 Marie-Curie, Ottawa, OntarioK1N 6N5, Canada
Pages 49-63 | Published online: 24 Nov 2015

Bibliography

  • 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.

••The warheads and scaffolds divulged in this patent continue to inspire inhibitor design to this day.

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••Many of the warheads shown in this patent are still employed in current inhibitor design.

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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 patent discloses the first TGase inhibitor to be entered into clinical trials.

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