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

      Bioorganic & Medicinal Chemistry

      Chymotrypsin, antagonists & inhibitors, Cyclization, Drug Design, Enediynes, chemical synthesis, chemistry, pharmacology, Enzyme Activation, drug effects, Enzyme Inhibitors, Molecular Structure, Peptides, Substrate Specificity

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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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          Journal
          19428261
          10.1016/j.bmc.2009.04.019

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