Design, synthesis, and evaluation of 5'-S-aminoethyl-N(6)- azidobenzyl-5'-thioadenosine biotin conjugate: a bifunctional photoaffinity probe for the es nucleoside transporter.
Design, synthesis, and evaluation of 5'-S-aminoethyl-N(6)- azidobenzyl-5'-thioadenosine biotin conjugate: a bifunctional photoaffinity probe for the es nucleoside transporter.
复制标题
5-S-氨基乙基-N(6)-叠氮基-5-硫代腺苷生物素缀合物的设计、合成和评估：es核苷转运蛋白的双功能光亲和探针。
DOI：
10.1021/bc034165j
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
Buolamwini,JohnK
中科院分区：
文献类型：
--
作者：
Addo,JamesK;Buolamwini,JohnK
A bifunctional biotinylated photoaffinity label for the nitrobenzylmercaptopurine riboside (NBMPR)-sensitive (es) nucleoside transporter (ENT1) has been synthesized and evaluated. This new probe,5‘-S-aminoethyladenosine-N6-azidobenzyl-5‘-thioadenosine biotin conjugate (SAEATA-14-biotin), exhibited high-affinity binding to theestransporter in K562 cells as determined by flow cytometry, with aKiof 2.69 nM in competition against 5-(SAENTA)-x8-fluorescein. It also exhibited covalent linking to theestransporter in BeWo cell membranes upon UV irradiation. This new bifunctional probe is a potential tool for determining the amino acid residues involved in ligand binding at the NBMPR-binding site of the ENT1 nucleoside transporter, as well as for the purification of the transporter.
