Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase

Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase

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 appare...

Full description

Bibliographic Details
Main Authors: Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi, Masahiro Nishibori
Format: Article
Language:English
Published: Elsevier 2003-01-01
Series:Journal of Pharmacological Sciences
Online Access:http://www.sciencedirect.com/science/article/pii/S1347861319326416
id doaj-ef62842aa6d54c39857b24df62177dc2
record_format Article
spelling doaj-ef62842aa6d54c39857b24df62177dc22020-11-24T22:01:17ZengElsevierJournal of Pharmacological Sciences1347-86132003-01-01924420423Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human TryptaseShuji Mori0Yoshinori Itoh1Ryoko Shinohata2Toshiaki Sendo3Ryozo Oishi4Masahiro Nishibori5Department of Pharmacology, Okayama University Graduate School of Medicine and Dentistry, 2-5-1 Shikata-cho, Okayama 700-8558, JapanDepartment of Hospital Pharmacy, Faculty of Medicine, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, JapanDepartment of Pharmacology, Okayama University Graduate School of Medicine and Dentistry, 2-5-1 Shikata-cho, Okayama 700-8558, JapanDepartment of Hospital Pharmacy, Faculty of Medicine, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, JapanDepartment of Hospital Pharmacy, Faculty of Medicine, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, JapanDepartment of Pharmacology, Okayama University Graduate School of Medicine and Dentistry, 2-5-1 Shikata-cho, Okayama 700-8558, JapanPreviously, 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.http://www.sciencedirect.com/science/article/pii/S1347861319326416
collection DOAJ
language English
format Article
sources DOAJ
author Shuji Mori
Yoshinori Itoh
Ryoko Shinohata
Toshiaki Sendo
Ryozo Oishi
Masahiro Nishibori
spellingShingle Shuji Mori
Yoshinori Itoh
Ryoko Shinohata
Toshiaki Sendo
Ryozo Oishi
Masahiro Nishibori
Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
Journal of Pharmacological Sciences
author_facet Shuji Mori
Yoshinori Itoh
Ryoko Shinohata
Toshiaki Sendo
Ryozo Oishi
Masahiro Nishibori
author_sort Shuji Mori
title Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
title_short Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
title_full Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
title_fullStr Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
title_full_unstemmed Nafamostat Mesilate Is an Extremely Potent Inhibitor of Human Tryptase
title_sort nafamostat mesilate is an extremely potent inhibitor of human tryptase
publisher Elsevier
series Journal of Pharmacological Sciences
issn 1347-8613
publishDate 2003-01-01
description 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.
url http://www.sciencedirect.com/science/article/pii/S1347861319326416
work_keys_str_mv AT shujimori nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
AT yoshinoriitoh nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
AT ryokoshinohata nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
AT toshiakisendo nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
AT ryozooishi nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
AT masahironishibori nafamostatmesilateisanextremelypotentinhibitorofhumantryptase
_version_ 1725840507154726912

Similar Items