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

Kyoko Teramura Drug Serendipity Research Laboratories, Institute for Drug Discovery Research, Yamanauchi Pharmaceutical Co., Ltd., Tokyo, 174

Masaya Orita Molecular Chemistry Research Laboratories, Institute for Drug Discovery Research, Yamanacichi Pharmaceutical Co., Ltd., Ibaraki, 305

Hisao Matsumoto Molecular Chemistry Research Laboratories, Institute for Drug Discovery Research, Yamanacichi Pharmaceutical Co., Ltd., Ibaraki, 305

Kenichi Yasumuro Drug Serendipity Research Laboratories, Institute for Drug Discovery Research, Yamanauchi Pharmaceutical Co., Ltd., Tokyo, 174

Kenji Abe Drug Serendipity Research Laboratories, Institute for Drug Discovery Research, Yamanauchi Pharmaceutical Co., Ltd., Tokyo, 174

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.

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

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

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