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Synthesis of [3(R)-amino-2(S)-sulfhydryl-5-sulfonate]-pentanoyl-(S)-3-[125I]-iodotyrosyl-(S)-aspartic acid: a radiolabelled inhibitor of aminopeptidase A

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‐[125I]‐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.
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https://hal-normandie-univ.archives-ouvertes.fr/hal-02385512
Contributor : Laurent Bischoff <>
Submitted on : Thursday, November 28, 2019 - 6:51:08 PM
Last modification on : Tuesday, September 22, 2020 - 3:38:32 AM

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Christelle David-Basei, Laurent Bischoff, Marie-Claude Fournie-Zaluski, Bernard Roques. Synthesis of [3(R)-amino-2(S)-sulfhydryl-5-sulfonate]-pentanoyl-(S)-3-[125I]-iodotyrosyl-(S)-aspartic acid: a radiolabelled inhibitor of aminopeptidase A. Journal of Labelled Compounds and Radiopharmaceuticals, Wiley-Blackwell, 2001, 44 (1), pp.89-98. ⟨10.1002/jlcr.445⟩. ⟨hal-02385512⟩

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