Design and synthesis of biotin- or alkyne-conjugated photoaffinity probes for studying the target molecules of PD 404182

被引:13
|
作者
Mizuhara, Tsukasa [1 ]
Oishi, Shinya [1 ]
Ohno, Hiroaki [1 ]
Shimura, Kazuya [2 ]
Matsuoka, Masao [2 ]
Fujii, Nobutaka [1 ]
机构
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan
[2] Kyoto Univ, Inst Virus Res, Sakyo Ku, Kyoto 6068507, Japan
关键词
Anti-HIV agents; PD; 404182; Photoaffinity labeling; Pyrimidobenzothiazine; HUMAN-IMMUNODEFICIENCY-VIRUS; HEPATITIS-C VIRUS; POTENT INHIBITORS; BINDING-SITE; CXCR4; ANTAGONISTS; HIV-1; REPLICATION; CCR5; IDENTIFICATION; ENFUVIRTIDE; DERIVATIVES;
D O I
10.1016/j.bmc.2013.01.016
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
To investigate the mechanism of action of the potent antiviral compound PD 404182, three novel photo-affinity probes equipped with a biotin or alkyne indicator were designed and synthesized based on previous structure-activity relationship studies. These probes retained the potent anti-HIV activity of the original pyrimidobenzothiazine derivatives. In photoaffinity labeling studies using HIV-1-infected H9 cells (H9IIIB), eight potential proteins were observed to bind PD 404182. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2079 / 2087
页数:9
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