Peptide affinity labels for thrombin and other trypsin-like proteases
    9.
    发明授权
    Peptide affinity labels for thrombin and other trypsin-like proteases 失效
    凝血酶和其他胰蛋白酶样蛋白酶的肽亲和标记

    公开(公告)号:US4318904A

    公开(公告)日:1982-03-09

    申请号:US143897

    申请日:1980-04-25

    摘要: A peptide affinity label of the formula (I): ##STR1## wherein X is a radical capable of acting as a leaving group in a nucleophilic substitution reaction;A is an aromatic amino acid residue;B is H, or a C.sub.1 -C.sub.4 alkyl group, or aryl;Y is selected from the group consisting of hydrogen, aroyl, C.sub.1 -C.sub.6 acyl, and Q--(A)--.sub.n, whereinQ=hydrogen, aroyl, or C.sub.1 -C.sub.6 acyl,n=1-10,A is an amino acid residue selected from the aliphatic, hydroxy-containing, carboxylic acid group, and amide-thereof-containing, aromatic, sulfur-containing and imino-containing amino acids; and wherein J is selected from the group consisting of --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --,--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- and --CH(OH)--CH.sub.2. The affinity label is useful for irreversibly inactivating thrombin and trypsin-like enzymes and may be used as a potential anticlotting agent.

    摘要翻译: 式(I)的肽亲和标记:其中X是能够在亲核取代反应中作为离去基团的基团; A是芳香族氨基酸残基; B是H或C 1 -C 4烷基或芳基; Y选自氢,芳酰基,C 1 -C 6酰基和Q-(A)-n,其中Q =氢,芳酰基或C 1 -C 6酰基,n = 1-10,A是氨基酸 选自含脂肪族,含羟基的羧酸基和含酰胺的芳族,含硫和亚氨基的氨基酸的残基; 并且其中J选自-CH 2 - , - CH 2 -CH 2 - , - CH 2 -CH 2 -CH 2 - , - CH = CH-和-CH(OH)-CH 2。 亲和标记可用于不可逆地灭活凝血酶和胰蛋白酶样酶,并且可用作潜在的抗起球剂。