Highly sensitive peptide‐4‐methylcoumaryl‐7‐amide substrates for blood‐clotting proteases and trypsin
作者： Shun-Ichiro KAWABATA , Takako MIURA , Takashi MORITA , Hisao KATO , Kazuo FUJIKAWA
DOI: 10.1111/J.1432-1033.1988.TB13849.X
关键词:
摘要: Seventy-four peptide amides of 7-amino-4-methylcoumarine (Mec) the type Boc-Xaa-Yaa-Arg-NH-Mec were newly synthesized and tested to find specific substrates for blood-clotting proteases trypsin. The Xaa Yaa residues these have been replaced by 12 15 different amino acids, respectively. Among peptides, followings found be most sensitive individual enzymes: Boc-Asp(OBzl)-Pro-Arg-NH-Mec (kcat= 160 s−1, Km= 11 μM, kcat/Km=15000000 M−1 s−1) human α-thrombin, Z-< Glu-Gly-Arg-NH-Mec(kcat= 19 59 kcat/Km= 320000 bovine factor Xa, Boc-Gln-Gly-Arg-NH-Mec 5.8 140 42000) XIIa, Boc-Asp(OBzl)-Ala-Arg-NH-Mec 9.2 120 77000 activated protein C, Boc-Gly-Phe-Arg-NH-Mec 29 230 130000 plasma kallikrein. Moreover, Boc-Glu(OBzl)-Ala-Arg-NH-Mec 46 370 120000 was as a good substrate XIa. Bovine trypsin effectively hydrolyzed peptide-NH-Mec containing Ala Pro at P2 site. reactive Boc-Gln-Ala-Arg-NH-Mec 6.0 20000000 s−1).
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