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10.1021/ml3000534

http://scihub22266oqcxt.onion/10.1021/ml3000534
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C4025795!4025795!24900505
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suck abstract from ncbi


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pmid24900505      ACS+Med+Chem+Lett 2012 ; 3 (7): 530-4
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  • Design and Synthesis of Potent, Selective Inhibitors of Matriptase #MMPMID24900505
  • Colombo É; Désilets A; Duchêne D; Chagnon F; Najmanovich R; Leduc R; Marsault E
  • ACS Med Chem Lett 2012[Jul]; 3 (7): 530-4 PMID24900505show ga
  • Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1?P4 substrate recognition sequence of the enzyme. Preliminary structure?activity relationships indicate that this benzothiazole-containing RQAR-peptidomimetic is a very potent inhibitor and possesses a good selectivity for matriptase versus other serine proteases. A molecular model was generated to elucidate the key contacts between inhibitor 1 and matriptase.
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