HIGHLY SENSITIVE PEPTIDE-4-METHYLCOUMARYL-7-AMIDE SUBSTRATES FOR BLOOD-CLOTTING PROTEASES AND TRYPSIN

HIGHLY SENSITIVE PEPTIDE-4-METHYLCOUMARYL-7-AMIDE SUBSTRATES FOR BLOOD-CLOTTING PROTEASES AND TRYPSIN
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DOI:
10.1111/j.1432-1033.1988.tb13849.x
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发表时间:
1988-02-15
期刊:
EUROPEAN JOURNAL OF BIOCHEMISTRY
影响因子:
--
通讯作者:
SAKAKIBARA, S
SAKAKIBARA, S
中科院分区:
其他
文献类型:
--
作者:
KAWABATA, SI;MIURA, T;SAKAKIBARA, S

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新合成了Boc-Xaa-Yaa-Arg-NH-Mec型7-氨基-4-甲基courmarine (Mec)的74种肽酰胺,并对其进行了凝血蛋白酶和胰蛋白酶的特异性底物检测。这些底物的Xaa和Yaa残基分别被12种和15种不同的氨基酸取代。在这些肽中,发现以下是对单个酶最敏感的底物:Boc-Asp(OBzl)-Pro-Arg-NH-Mec (kcat = 160 s-1, Km = 11 .mu)。M, kcat/Km = 15,000,000 M-1 s-1)。凝血酶,Z -
Seventy-four peptide amides of 7-amino-4-methylcourmarine (Mec) of the type Boc-Xaa-Yaa-Arg-NH-Mec were newly synthesized and tested to find specific substrates for blood-clotting proteases and trypsin. The Xaa and Yaa residues of these substrates have been replaced by 12 and 15 different amino acids, respectively. Among these peptides, the following were found to be most sensitive substrates for individual enzymes: Boc-Asp(OBzl)-Pro-Arg-NH-Mec (kcat = 160 s-1, Km = 11 .mu.M, kcat/Km = 15,000,000 M-1 s-1) for human .alpha.-thrombin, Z-