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

Abstract	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.
Authors	N Nonaka, Y Asai, M Nishio, K Takahashi, T Okuda, S Tanaka, T Sugita, T Ohnuki, S Komatsubara
Journal	The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 50 Issue 8 Pg. 646-52 (Aug 1997) ISSN: 0021-8820 [Print] England
PMID	9315076 (Publication Type: Journal Article)
Chemical References	Enzyme Inhibitors Indoles Isoquinolines TMC 2A TMC 2B TMC 2C Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
Topics	Animals Aspergillus oryzae Cells, Cultured Dipeptidyl-Peptidases and Tripeptidyl-Peptidases (antagonists & inhibitors) Enzyme Inhibitors (isolation & purification, pharmacology) Fermentation Humans Indoles (isolation & purification, pharmacology) Isoquinolines (isolation & purification, pharmacology) Kidney (drug effects, enzymology) Male Rats Rats, Sprague-Dawley

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