IR@PKUHSC  > 北京大学基础医学院  > 免疫学系
学科主题基础医学
Design, Synthesis, and Structure-Affinity Relationships of Novel Series of Sialosides as CD22-Specific Inhibitors
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
2008-11-13
DOI10.1021/jm8000696
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
WOS记录号WOS:000260730900010
项目编号17101007
资助机构ministry of Education, Culture, Sports, Science, and Technology (MEXT) of Japan ; CREST of JST (Japan Science and Technology Corporation)
引用统计
被引频次:23[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
版本出版稿
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65664
专题北京大学基础医学院_免疫学系
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
推荐引用方式
GB/T 7714
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.
APA Abdui-Allah, Hajaj H. M..,Tainanaka, Taichi.,Yu, Jie.,Zhuoyuan, Lu.,Sadagopan, Magesh.,...&Kiso, Makoto.(2008).Design, Synthesis, and Structure-Affinity Relationships of Novel Series of Sialosides as CD22-Specific Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,51(21),6665-6681.
MLA Abdui-Allah, Hajaj H. M.,et al."Design, Synthesis, and Structure-Affinity Relationships of Novel Series of Sialosides as CD22-Specific Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 51.21(2008):6665-6681.
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