Nafamostat mesilate is an extremely potent inhibitor of human tryptase

Shuji Mori; Yoshinori Itoh; Ryoko Shinohata; Toshiaki Sendo; Ryozo Oishi; Masahiro Nishibiro

doi:10.1254/jphs.92.420

Nafamostat mesilate is an extremely potent inhibitor of human tryptase

Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi, Masahiro Nishibiro

Research output: Contribution to journal › Article › peer-review

92 Citations (Scopus)

Abstract

Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its K_i value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent K_i value was estimated to be 95.3 pM, which was 1,000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.

Original language	English
Pages (from-to)	420-423
Number of pages	4
Journal	Journal of Pharmacological Sciences
Volume	92
Issue number	4
DOIs	https://doi.org/10.1254/jphs.92.420
Publication status	Published - Aug 1 2003

Keywords

Inhibition
Nafamostat mesilate
Tryptase

ASJC Scopus subject areas

Molecular Medicine
Pharmacology

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10.1254/jphs.92.420

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abstract = "Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its Ki value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent Ki value was estimated to be 95.3 pM, which was 1,000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.",

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T1 - Nafamostat mesilate is an extremely potent inhibitor of human tryptase

AU - Mori, Shuji

AU - Itoh, Yoshinori

AU - Shinohata, Ryoko

AU - Sendo, Toshiaki

AU - Oishi, Ryozo

AU - Nishibiro, Masahiro

PY - 2003/8/1

Y1 - 2003/8/1

N2 - Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its Ki value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent Ki value was estimated to be 95.3 pM, which was 1,000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.

AB - Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its Ki value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent Ki value was estimated to be 95.3 pM, which was 1,000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.

KW - Inhibition

KW - Nafamostat mesilate

KW - Tryptase

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Nafamostat mesilate is an extremely potent inhibitor of human tryptase

Abstract

Keywords

ASJC Scopus subject areas

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