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      Design and synthesis of enediyne–peptide conjugates and their inhibiting activity against chymotrypsin

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      Bioorganic & Medicinal Chemistry

      Elsevier BV

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          Abstract

          Novel enediyne-amino acid conjugates 1-4 have been synthesized. All of these effectively target the enzyme chymotrypsin inhibiting its proteolytic activity. The conjugate with a directly linked phenyl alanine is the most effective inhibitor with a K(i) of 3 microM. The mode of inhibition is mostly competitive or of a mixed type depending on the nature of the inhibitor.

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          Author and article information

          Journal
          Bioorganic & Medicinal Chemistry
          Bioorganic & Medicinal Chemistry
          Elsevier BV
          09680896
          June 2009
          June 2009
          : 17
          : 11
          : 3900-3908
          Article
          10.1016/j.bmc.2009.04.019
          19428261
          © 2009

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