17α-Ethynylestradiol Peptide Labeling by 'Click' Chemistry

被引：5

作者：

Bol'shakov, Oleg I. ^{[1
]}

Lebedyeva, Iryna O. ^{[1
]}

Katritzky, Alan R. ^{[1
,2
]}

机构：

[1] Univ Florida, Dept Chem, Ctr Heterocycl Cpds, Gainesville, FL 32611 USA

[2] King Abdulaziz Univ, Dept Chem, Jeddah 21589, Saudi Arabia

来源：

SYNTHESIS-STUTTGART | 2012年 / 44卷 / 18期

关键词：

cyclization; azides; alkynes; peptides; drugs; click chemistry; MECHANISM-BASED INACTIVATION; P450S; 2B1; AZIDE; DIAZOTRANSFER; ESTRADIOL; LIGATION; IDENTIFICATION; HYALURONAN;

D O I：

10.1055/s-0032-1316702

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A synthesis of 17 alpha-ethynylestradiol-labeled native peptides is reported. The peptide moiety is tethered to the steroid hormone by a 1,2,3-triazole bridge formed by a CuAAC reaction in which the azido group of the peptide combines with the terminal acetylenic moiety of ethynylestradiol to link the two bioactive molecules. Thus bioconjugates containing the hormone moiety at three positions within the peptide molecule could be useful targets for hormono-enzyme interaction studies.

引用

页码：2926 / 2932

页数：7

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