Synthesis of [3(R)‐amino‐2(S)‐sulfhydryl‐5‐sulfonate]‐pentanoyl‐(S)‐3‐[ 125 I]‐iodotyrosyl‐(S)‐aspartic acid: a radiolabelled inhibitor of aminopeptidase A
Author(s) -
DavidBasei Christelle,
Bischoff Laurent,
FournieZaluski MarieClaude,
Roques Bernard P.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.445
Subject(s) - chemistry , aspartic acid , aminopeptidase , sulfonate , enzyme , amino acid , stereochemistry , enzyme inhibitor , biochemistry , leucine , organic chemistry , sodium
Abstract In order to investigate the localization of aminopeptidase A in the central nervous system and peripheral organs, we have synthesized the first radiolabelled inhibitor of this enzyme. This molecule, [3(R)‐amino‐2(S)‐sulfhydryl‐5‐sulfonate]‐pentanoyl‐(S)‐3‐[ 125 I]‐iodotyrosyl‐(S)‐aspartic acid, exhibited a Ki value of 4.8 nM for aminopeptidase A. A high purity was obtained with a specific activity of about 2,000 Ci/mmol at the end of the synthesis. Copyright © 2001 John Wiley & Sons, Ltd.
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