Peptide affinity labels for thrombin and other trypsin-like proteases

Patent · Tue Mar 09 00:00:00 EST 1982

OSTI ID:864150

Shaw, Elliott N ^[1]; Kettner, Charles A ^[2]

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1. Shoreham, NY
2. Yaphank, NY

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, 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-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.

• Research Organization: Associated Universities, Inc., Upton, NY (United States)
• DOE Contract Number: AC02-76CH00016
• Assignee: Research Corporation (New York, NY)
• Patent Number(s): US 4318904
• Application Number: 06/143,897
• OSTI ID: 864150
• Country of Publication: United States
• Language: English

Related Subjects

peptide
affinity
labels
thrombin
trypsin-like
proteases
label
formula
str1
radical
capable
acting
leaving
nucleophilic
substitution
reaction
aromatic
amino
acid
residue
-c
alkyl
aryl
selected
consisting
hydrogen
aroyl
acyl
q-
1-10
aliphatic
hydroxy-containing
carboxylic
amide-thereof-containing
sulfur-containing
imino-containing
acids
-ch
dbd
ch-
oh
useful
irreversibly
inactivating
enzymes
potential
anticlotting
agent
amino acid
carboxylic acid
amino acids
nucleophilic substitution
acid residue
peptide affinity
containing amino
substitution reaction
affinity label
/514/530/999/930/