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ACS Med Chem Lett. 2012 Oct 4;3(12):1024-8. doi: 10.1021/ml300241m. eCollection 2012 Dec 13.

SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.

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CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
Evotec AG , Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.


We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.


acrylamides; celiac disease; in vitro ADME; plasma stability; polar surface area

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