Abstract
A novel inhibitor of prolyl endopeptidase, the propeptin analog propeptin-2 (C105H130N24O(24)), missing two amino acid residues from the propeptin C-terminus was isolated from the fermentation broth of propeptin-producing Microbispora sp. SNA-115 grown using a large inoculum. It shows the same enzyme inhibition activity as propeptin against prolyl endopeptidase (Ki=1.5 microM), but its antimicrobial activity against Mycobacterium phlei is more than 100-fold lower.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Actinomycetales / growth & development
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Actinomycetales / metabolism*
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Amino Acids / metabolism
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Culture Media / metabolism
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / metabolism*
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Enzyme Inhibitors / pharmacology
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Microbial Sensitivity Tests
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Mycobacterium phlei / drug effects
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Peptides, Cyclic / chemistry*
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Peptides, Cyclic / metabolism*
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Peptides, Cyclic / pharmacology
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Prolyl Oligopeptidases
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Serine Endopeptidases / metabolism
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Structure-Activity Relationship
Substances
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Amino Acids
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Culture Media
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Enzyme Inhibitors
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Peptides, Cyclic
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propeptin
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Serine Endopeptidases
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Prolyl Oligopeptidases