Peptide affinity labels for thrombin and other trypsin-like proteases

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;PPA is an aromatic amino acid residue;PPB is H, or a C.sub.1 -C.sub.4 alkyl group, or aryl;PPY is selected from the group consisting of hydrogen, aroyl, C.sub.1 -C.sub.6 acyl, and Q--(A)--.sub.n, wherein PPQ=hydrogen, aroyl, or C.sub.1 -C.sub.6 acyl,P Pn=1-10,PPA 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═ 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.