Synthesis of a bis-azido analogue of acromelic acid for radioisotope-free photoaffinity labeling and biochemical studies

Synthesis of a bis-azido analogue of acromelic acid for radioisotope-free photoaffinity labeling and biochemical studies
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DOI:
10.1016/j.bmcl.2006.01.083
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发表时间:
2006-05-01
影响因子:
2.7
通讯作者:
Suzuki, M
Suzuki, M
中科院分区:
医学4区
文献类型:
--
作者:
Sun, P;Wang, GX;Suzuki, M

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一种新型的烯丙酸类似物,其苯基具有两种不同类型的叠氮官能团,其中一种是芳香的N-3作为光亲和基团,通过光照射与靶蛋白结合,另一种是烷基N-3作为光解作用的检测基团,通过Staudinger-Bertozzi反应识别连接产物。设计并合成了一种无放射性同位素的生化探针,有望用于类碱受体的研究。(C) 2006 Elsevier Ltd版权所有。
A novel acromelic acid analogue containing a phenyl group possessing two different types of azido functional groups, of which one is the aromatic N-3 acting as a photoaffinity group to bind to a target protein by photoirradiation and the other is alkyl N-3 group which survives photolysis acting as a detecting group through the Staudinger-Bertozzi reaction to identify the ligated product, was designed and synthesized as a radioisotope-free biochemical probe potentially for studies on kainoid receptors. (C) 2006 Elsevier Ltd. All rights reserved.