[New dipeptide fluorogenic substrates of human tissue kallikrein].
Based on 4-methylcoumarinyl-7-amide (Amc) arginine and a series N-alkyloxycarbonyl derivatives of phenylalanine, eleven Amc-derivatives of the type ROCO-Phe-Arg-Amc (R = alkyl) were synthesized; also were n-C3H7OCO-Leu-Arg-Amc and n-C3H7OCO-D-Phe-Arg-Amc synthesized. The enzymatic hydrolysis of these compounds under the action of tissue and plasma human kallikreins were studied. Tissue kallikrein from human urine hydrolyzed the compounds with R = n-propyl and n-butyl and n-C3H7OCO-Leu-Arg-Amc more readily than the known substrates Z-Phe-Arg-Amc and H-Pro-Phe-Arg-Amc. n-C3H7OCO-D-Phe-Arg-Amc is a weak inhibitor of this enzyme (Ki = 1.5.10(-4) M). Human plasma kallikrein hydrolyzed these novel substrates at a lower rate than Z-Phe-Arg-Amc.
Pozdnev
V F
VF
Rabinovich
S E
SE
Paskhina
T S
TS
D001120:Arginine; D004151:Dipeptides / Q000138:chemical synthesis / Q000378:metabolism*; D005453:Fluorescence; D006801:Humans; D006868:Hydrolysis; D007610:Kallikreins / Q000097:blood / Q000378:metabolism* / Q000652:urine; D010649:Phenylalanine; D013379:Substrate Specificity
D004151:Dipeptides; D010649:Phenylalanine; D001120:Arginine; D007610:Kallikreins
Novye dipeptidnye fluorogennye substraty tkanevogo kallikreina cheloveka.