Similarity of the effects of tosyl-L-arginine methyl ester, atropine, caffeine and antitumour alkylating agent on some biological functions of thrombin and platelet 12-lipoxygenase.
The effect of the synthetic thrombin substrate (TAME) and three compounds exerting an opposite effect on Ca-PPI and AdC (caffeine, atropine and meta-tolyl derivative of mechlorethamine (TDM)) on hormone-like and catalytic functions of thrombin was studied. It is shown that both TAME and other drugs under test block effectively the thrombin-induced platelet aggregation, as well as protect the active site of the enzyme from denaturation by dithiothreitol. The same compounds inhibit thrombin in thrombin-fibrinogen reaction and platelet 12-lipoxygenase. These data suggest identity of thrombin moieties which determine its enzymatic and hormone-like activities.
Radchenko
I V
IV
Institute of Bioorganic and Petroleum, Chemistry Academy of Sciences of Ukraine, Kyiv.
Kostyuchenko
N V
NV
Naidenova IYu
Batrak
G N
GN
Poda
G I
GI
Mogilevich
S E
SE
Kibirev
V K
VK
Luik
A I
AI
D000477:Alkylating Agents / Q000494:pharmacology*; D000818:Animals; D001092:Arachidonate 12-Lipoxygenase / Q000145:classification / Q000187:drug effects*; D001285:Atropine / Q000494:pharmacology*; D001792:Blood Platelets / Q000201:enzymology; D002110:Caffeine / Q000494:pharmacology*; D002384:Catalysis; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013917:Thrombin / Q000187:drug effects*; D014106:Tosylarginine Methyl Ester / Q000494:pharmacology*
D000477:Alkylating Agents; D002110:Caffeine; D001285:Atropine; D014106:Tosylarginine Methyl Ester; D001092:Arachidonate 12-Lipoxygenase; D013917:Thrombin