Effects of Ym-51084 and Ym-51085, New Inhibitors Produced by Streptomyces Sp. Q21705, on Cathepsin L

Abstract The structures of YM-51084 and YM-51085, new protease inhibitors produced by Streptomyces sp. Q21705, were determined by H- and 13C-NMR and mass spectrometry. Both were characterized by the basic structures of an acytripeptide. YM-51084 was elucidated to be isovaleryl-tyrosyl-valyl-phenylal...

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Veröffentlicht in:	Journal of enzyme inhibition 1996-01, Vol.11 (2), p.115-121
Hauptverfasser:	Teramura, Kyoko, Orita, Masaya, Matsumoto, Hisao, Yasumuro, Kenichi, Abe, Kenji
Format:	Artikel
Sprache:	eng
Schlagworte:	Carbon Isotopes Cathepsin B - antagonists & inhibitors Cathepsin B - chemistry Cathepsin L Cathepsins - antagonists & inhibitors Cathepsins - chemistry Cysteine Endopeptidases Cysteine Proteinase Inhibitors - chemistry Cysteine Proteinase Inhibitors - pharmacology cystene protease Endopeptidases Enzyme Activation - drug effects Humans Hydrogen Kidney - enzymology Magnetic Resonance Spectroscopy Molecular Structure Oligopeptides - pharmacology osteoporosis Papain - antagonists & inhibitors Papain - chemistry protease inhibitor Spectrometry, Mass, Fast Atom Bombardment - methods Streptomyces - chemistry
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Zusammenfassung:	Abstract The structures of YM-51084 and YM-51085, new protease inhibitors produced by Streptomyces sp. Q21705, were determined by H- and 13C-NMR and mass spectrometry. Both were characterized by the basic structures of an acytripeptide. YM-51084 was elucidated to be isovaleryl-tyrosyl-valyl-phenylalaninal and YM-51085 was the reduced phenylalaninol form of YM-51084. These compounds proved to strongly inhibit human kidney cathepsin L; the IC50 values being 9.6 × 10-−9M and 3.5 × 10−7M, respectively.
ISSN:	1475-6366 8755-5093 1475-6374
DOI:	10.3109/14756369609036538