Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases that is therapeutically used in the treatment of pancreatitis and disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Considering the structural similarity between gabexate mesylate and arginine-based inhibitors of trypsin-like serine proteinases. the effect of gabexate mesylate on human and bovine mast cell tryptase action was investigated. Values of the inhibition constant (K-i) for gabexate mesylate binding to human and bovine tryptase were 3.4 x 10(-9) M and 1.8 x 10(-7) M (at pH 7.4 and 37.0 degrees), respectively. Furthermore, gabexate mesylate inhibited the fibrinogenolytic activity of human tryptase. On the basis of the available x-ray crystal structure of human tryptase, the possible binding mode of gabexate mesylate to human and bovine tryptase was analyzed. Human tryptase inhibition by gabexate mesylate may account for the reported prevention of inflammation, erosion, and ulceration of skin and mucosae. (C) 2001 Elsevier Science Inc. All rights reserved.

Erba, F., Fiorucci, L., Pascarella, S., Menegatti, E., Ascenzi, P., Ascoli, F. (2001). Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. BIOCHEMICAL PHARMACOLOGY, 61(3), 271-276 [10.1016/S0006-2952(00)00550-5].

Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug

ERBA, FULVIO;FIORUCCI, LAURA;
2001-01-01

Abstract

Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases that is therapeutically used in the treatment of pancreatitis and disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Considering the structural similarity between gabexate mesylate and arginine-based inhibitors of trypsin-like serine proteinases. the effect of gabexate mesylate on human and bovine mast cell tryptase action was investigated. Values of the inhibition constant (K-i) for gabexate mesylate binding to human and bovine tryptase were 3.4 x 10(-9) M and 1.8 x 10(-7) M (at pH 7.4 and 37.0 degrees), respectively. Furthermore, gabexate mesylate inhibited the fibrinogenolytic activity of human tryptase. On the basis of the available x-ray crystal structure of human tryptase, the possible binding mode of gabexate mesylate to human and bovine tryptase was analyzed. Human tryptase inhibition by gabexate mesylate may account for the reported prevention of inflammation, erosion, and ulceration of skin and mucosae. (C) 2001 Elsevier Science Inc. All rights reserved.
2001
Pubblicato
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore BIO/10 - BIOCHIMICA
English
Bovine tryptase; Enzyme inhibition; Gabexate mesylate; Human tryptase; Structural aspects
Erba, F., Fiorucci, L., Pascarella, S., Menegatti, E., Ascenzi, P., Ascoli, F. (2001). Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. BIOCHEMICAL PHARMACOLOGY, 61(3), 271-276 [10.1016/S0006-2952(00)00550-5].
Erba, F; Fiorucci, L; Pascarella, S; Menegatti, E; Ascenzi, P; Ascoli, F
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/52612
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