Peptide affinity labels for thrombin and other trypsin-like proteases

Patent · Tue Mar 09 00:00:00 EST 1982

OSTI ID:7000912

Shaw, E N; Kettner, C A

A peptide affinity label is disclosed of the formula (I): as given in the patent 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], wherein Q = 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-thereofcontaining, 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[double bond]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. 2 figs.

• DOE Contract Number: AC02-76CH00016
• Assignee: Research Corp., New York, NY (United States)
• Patent Number(s): US 4318904; A
• Application Number: PPN: US 6-143897
• OSTI ID: 7000912
• Resource Relation: Patent File Date: 25 Apr 1980
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PEPTIDE HYDROLASES
LABELLING
PEPTIDES
BIOCHEMICAL REACTION KINETICS
THROMBIN
CHEMICAL COMPOSITION
BLOOD COAGULATION FACTORS
COAGULANTS
DRUGS
ENZYMES
HEMATOLOGIC AGENTS
HEMOSTATICS
HYDROLASES
KINETICS
ORGANIC COMPOUNDS
PROTEINS
REACTION KINETICS
SERINE PROTEINASES
550200* - Biochemistry