Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts

Anna Falanga; Elliott Shaw; Maria Benedetta Donati; Rossella Consonni; Tiziano Barbui; Stuart Gordon

doi:10.1016/0049-3848(89)90209-0

Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts

Anna Falanga, Elliott Shaw, Maria Benedetta Donati, Rossella Consonni, Tiziano Barbui, Stuart Gordon

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Abstract

Cancer procoagulant (CP) is a cysteine proteinase from cancer cells that initiates blood coagulation. Members of two classes of unique and highly specific cysteine proteinase inhibitors, peptidyl diazomethyl ketones (PDK) and peptidyl sulfonium salts (PSS), were studied to determine whether or not they inhibited CP. The inhibitors did not impair the activity of the coagulation system. There was a differential inhibitory effect of the 6 PDK and 2 PSS inhibitors, influenced by the amino acid composition or sequence of the peptide moiety, that suggests differences in structural features of the active site of CP and papain. CP was inhibited by both classes of inhibitors.

Original language	English
Pages (from-to)	389-398
Number of pages	10
Journal	Thrombosis Research
Volume	54
Issue number	5
DOIs	https://doi.org/10.1016/0049-3848(89)90209-0
Publication status	Published - Jun 1 1989

Keywords

cancer procoagulant
coagulation
cysteine proteinase
cysteine proteinase inhibitor
peptidyl diazomethyl ketone
peptidyl sulfonium salt

ASJC Scopus subject areas

Cardiology and Cardiovascular Medicine
Hematology

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10.1016/0049-3848(89)90209-0

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title = "Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts",

abstract = "Cancer procoagulant (CP) is a cysteine proteinase from cancer cells that initiates blood coagulation. Members of two classes of unique and highly specific cysteine proteinase inhibitors, peptidyl diazomethyl ketones (PDK) and peptidyl sulfonium salts (PSS), were studied to determine whether or not they inhibited CP. The inhibitors did not impair the activity of the coagulation system. There was a differential inhibitory effect of the 6 PDK and 2 PSS inhibitors, influenced by the amino acid composition or sequence of the peptide moiety, that suggests differences in structural features of the active site of CP and papain. CP was inhibited by both classes of inhibitors.",

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T1 - Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts

AU - Falanga, Anna

AU - Shaw, Elliott

AU - Donati, Maria Benedetta

AU - Consonni, Rossella

AU - Barbui, Tiziano

AU - Gordon, Stuart

PY - 1989/6/1

Y1 - 1989/6/1

N2 - Cancer procoagulant (CP) is a cysteine proteinase from cancer cells that initiates blood coagulation. Members of two classes of unique and highly specific cysteine proteinase inhibitors, peptidyl diazomethyl ketones (PDK) and peptidyl sulfonium salts (PSS), were studied to determine whether or not they inhibited CP. The inhibitors did not impair the activity of the coagulation system. There was a differential inhibitory effect of the 6 PDK and 2 PSS inhibitors, influenced by the amino acid composition or sequence of the peptide moiety, that suggests differences in structural features of the active site of CP and papain. CP was inhibited by both classes of inhibitors.

AB - Cancer procoagulant (CP) is a cysteine proteinase from cancer cells that initiates blood coagulation. Members of two classes of unique and highly specific cysteine proteinase inhibitors, peptidyl diazomethyl ketones (PDK) and peptidyl sulfonium salts (PSS), were studied to determine whether or not they inhibited CP. The inhibitors did not impair the activity of the coagulation system. There was a differential inhibitory effect of the 6 PDK and 2 PSS inhibitors, influenced by the amino acid composition or sequence of the peptide moiety, that suggests differences in structural features of the active site of CP and papain. CP was inhibited by both classes of inhibitors.

KW - cancer procoagulant

KW - coagulation

KW - cysteine proteinase

KW - cysteine proteinase inhibitor

KW - peptidyl diazomethyl ketone

KW - peptidyl sulfonium salt

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Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts

Abstract

Keywords

ASJC Scopus subject areas

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