Peptide affinity labels for thrombin and other trypsin-like proteases

Abstract

Abstract 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 1 -C 4 alkyl group, or aryl; Y is selected from the group consisting of hydrogen, aroyl, C 1 -C 6 acyl, and Q--(A)-- n , wherein Q=hydrogen, aroyl, or C 1 -C 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 2 --, --CH 2 --CH 2 --,--CH 2 --CH 2 --CH 2 --, --CH═CH-- and --CH(OH)--CH 2 . The affinity label is useful for irreversibly inactivating thrombin and trypsin-like enzymes and may be used as a potential anticlotting agent.

Inventors

• 👤 Elliott N. Shaw
• 👤 Charles A. Kettner

Bibliographic Details