TMC-2A, -2B and -2C, novel dipeptidyl peptidase IV inhibitors produced by Aspergillus oryzae A374. I. Taxonomy of producing strain, fermentation, and biochemical properties.

نویسندگان

  • N Nonaka
  • Y Asai
  • M Nishio
  • K Takahashi
  • T Okuda
  • S Tanaka
  • T Sugita
  • T Ohnuki
  • S Komatsubara
چکیده

TMC-2A(1), -2B (2) and -2C (3), novel dipeptidyl peptidase IV (DPIV) inhibitors, were isolated from the fermentation broth of Aspergillus oryzae A374. TMC-2A, -2B and -2C inhibited rat kidney DPIV with IC50 value of 8.1 microM, 17 microM, and 20 microM, respectively, as well as human DPIV prepared from mononuclear cells and adenocarcinoma cells. TMC-2 compounds inhibited only DPIV among the proteases tested, indicating their high selectivity for DPIV. The kinetic analyses revealed that TMC-2A was an uncompetitive inhibitor. Taxonomy and fermentation of the producing strain are also described.

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عنوان ژورنال:
  • The Journal of antibiotics

دوره 50 8  شماره 

صفحات  -

تاریخ انتشار 1997