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10.1021/ml300241m

http://scihub22266oqcxt.onion/10.1021/ml300241m
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C4025666!4025666!24900424
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suck abstract from ncbi


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pmid24900424      ACS+Med+Chem+Lett 2012 ; 3 (12): 1024-8
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  • SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington s Disease #MMPMID24900424
  • Wityak J; Prime ME; Brookfield F; Courtney SM; Erfan S; Johnsen S; Johnson PD; Li M; Marston RW; Reed L; Vaidya D; Schaertl S; Pedret-Dunn A; Beconi M; Macdonald D; Muņoz-Sanjuan I; Dominguez C
  • ACS Med Chem Lett 2012[Dec]; 3 (12): 1024-8 PMID24900424show ga
  • 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.
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