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学科主题: 基础医学
题名:
Design, Synthesis, and Structure-Affinity Relationships of Novel Series of Sialosides as CD22-Specific Inhibitors
作者: Abdui-Allah, Hajaj H. M.1; Tainanaka, Taichi2; Yu, Jie2,3; Zhuoyuan, Lu2,3; Sadagopan, Magesh4; Adachi, Takahiro2; Tslibata, Takeshi2,5; Kelm, Soerge6; Ishida, Hideharu1; Kiso, Makoto1,4,5
刊名: JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2008-11-13
DOI: 10.1021/jm8000696
卷: 51, 期:21, 页:6665-6681
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: MYELIN-ASSOCIATED GLYCOPROTEIN ; N-ACETYLNEURAMINIC ACID ; CELL ANTIGEN RECEPTOR ; NEURAL SIGLECS ; B-CELLS ; IMMUNOGLOBULIN SUPERFAMILY ; STEREOSELECTIVE-SYNTHESIS ; SYSTEMATIC SYNTHESIS ; FUNCTIONAL-GROUPS ; INNATE IMMUNITY
英文摘要:

Sialosides incorporating substituted amides or amines at 9-position of sialic acid moiety have been synthesized and evaluated as CD22 inhibitors. Several derivatives exhibited inhibitory potency in sub- to low micromolar range (e. g., 8o, 9d, 9g, and 9k showed IC50 values 0.40, 0.47, 0.24, and 0.23 mu M, respectively, for hCD22, while 8p. 8q, and 9f, showed IC50 values 1.70, 2.90, and 4.10 mu M, respectively, for mCD22). The most significant result was the strongly enhanced affinity of 9g and 9k containing 9-(2′ or 4′-hydroxy-4-biphenyl) methylamino substituents (600-fold more potent for hCD22 than the corresponding 9-hydroxy derivative; 7a). Molecular modeling study was carried out to get some insights into the molecular basis of CD22 inhibition. To the best of our knowledge, this is the first systematic structure-affinity relationship study on inhibition of CD22.

语种: 英语
所属项目编号: 17101007
项目资助者: ministry of Education, Culture, Sports, Science, and Technology (MEXT) of Japan ; CREST of JST (Japan Science and Technology Corporation)
WOS记录号: WOS:000260730900010
Citation statistics:
内容类型: 期刊论文
版本: 出版稿
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65664
Appears in Collections:基础医学院_免疫学系_期刊论文

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作者单位: 1.Gifu Univ, United Grad Sch Agr Sci, Dept Appl Bioorgan Chem, Gifu 5011193, Japan
2.Tokyo Med & Dent Univ, Sch Med Sci, Immunol Lab, Tokyo, Japan
3.Peking Univ, Hlth Sci Ctr, Sch Basic Med Sci, Dept Immunol, Beijing, Peoples R China
4.Kyoto Univ, Inst Integrated Cell Mat Sci, Kyoto, Japan
5.JST, CREST, Saitama, Japan
6.Univ Bremen, Ctr Biomol Interact, Dept Biol & Chem, Bremen, Germany

Recommended Citation:
Abdui-Allah, Hajaj H. M.,Tainanaka, Taichi,Yu, Jie,et al. Design, Synthesis, and Structure-Affinity Relationships of Novel Series of Sialosides as CD22-Specific Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2008,51(21):6665-6681.
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