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  • Title: Design and synthesis of redox stable analogues of sunflower trypsin inhibitors (SFTI-1) on solid support, potent inhibitors of matriptase.
    Author: Jiang S, Li P, Lee SL, Lin CY, Long YQ, Johnson MD, Dickson RB, Roller PP.
    Journal: Org Lett; 2007 Jan 04; 9(1):9-12. PubMed ID: 17192072.
    Abstract:
    [structure: see text] Matriptase is a member of the emerging class of type II transmembrane serine proteases. It was found that the sunflower trypsin inhibitor (SFTI-1), isolated from sunflower seeds, inhibits matriptase with a subnanomolar Ki of 0.92 nM. On the basis of this result, we designed and synthesized its proteolytically stable analogues, SFTI-2 and SFTI-3. SFTI-3 exhibited very good binding affinity to matriptase, and it was metabolically stable.
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