Synthesis and characterization of αvβ₃-targeting peptidomimetic chelate conjugates for PET and SPECT imaging.
Synthesis and characterization of αvβ₃-targeting peptidomimetic chelate conjugates for PET and SPECT imaging.
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DOI：
10.1016/j.bmcl.2012.07.024
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发表时间：
2012-09-01
影响因子：
2.7
通讯作者：
Baidoo, Kwamena E.
中科院分区：
文献类型：
--
作者：
Kim, Young-Seung;Nwe, Kido;Milenic, Diane E.;Brechbiel, Martin W.;Satz, Stanley;Baidoo, Kwamena E.
关键词：
There is growing interest in small peptidomimetic αvβ3 integrin antagonists that are readily synthesized and characterized and can be easily handled using physiological conditions. Peptidomimetic 4-[2-(3,4,5,6-tetrahydropyrimidine-2-ylamino)ethyloxy]benzoyl-2-[N-(3-amino-neopenta-1-carbamyl)]-aminoethylsulfonyl-amino-β-alanine (IAC) was successfully conjugated to 1-(1-carboxy-3-carbo-t-butoxypropyl)-4,7-(carbo-tert-butoxymethyl)-1,4,7-triazacyclononane (NODAGA(tBu)3) and 1-(1-carboxy-3-carbotertbutoxymethyl)-1,4,7,10-tetraazacyclododecane (DOTAGA(tBu)4) and radiolabeled with 111In, 67Ga and 203Pb. Results of a radioimmunoassay demonstrated binding to purified αvβ3 integrin when one to four equivalents of integrin were added to the reaction. Based on this promising result, investigations are moving forward to evaluate the NODA-GA-IAC and DOTA-GA-IAC conjugates for the targeting tumor associated angiogenesis and αvβ3 integrin positive tumors to define their PET and SPECT imaging qualities as well as their potential for delivery of therapeutic radionuclides.
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DOI：
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发表时间：
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影响因子：
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作者：
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