Chemical proteomics to reveal interaction between chemicals and proteins at angstrom level

化学蛋白质组学揭示化学物质和蛋白质之间埃水平的相互作用

• 批准号: 17GS0221
• 负责人: OSADA Hiroyuki
• 金额: $ 265.82万
• 依托单位: The Institute of Physical and Chemical Research
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Creative Scientific Research
• 财政年份: 2005
• 资助国家: 日本
• 起止时间: 2005 至 2009
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-17GS0221/
• 关键词: 化学生物学; 構造生物学; バイオプローブ; 蛋白質; 相互作用; 受容体; リガンド; 化合物アレイ; ライブラリー; 低分子化合物; 結晶構造解析; 標的分子

Chemical biology is the interdisciplinary research area combining organic chemistry and molecular biology. In this study, we fused the research of both chemical biology and structural biology to construct a novel academic framework. We have developed chemical array system which can efficiently detect an interaction between bioactive small molecules (ligands) and their target proteins (receptors), and rapidly analyze the structure-activity relationship. Moreover, the interaction between a ligand and its receptor was successfully confirmed by co-crystallography. Our research outline is expected to contribute to drug discovery and progress of bioscience.

化学生物学是结合有机化学和分子生物学的跨学科研究领域。在这项研究中，我们融合了化学生物学和结构生物学的研究，以构建一个新的学术框架。我们开发了化学阵列系统，可以有效地检测生物活性小分子（配体）及其靶蛋白（受体）之间的相互作用，并迅速分析结构活性关系。此外，配体与其受体之间的相互作用通过共结晶成功证实。我们的研究大纲预计将有助于药物发现和生物科学进展。

项目成果

Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta

• DOI: 10.1080/14756360802693312
• 发表时间: 2009-08-01
• 期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
• 影响因子: 5.6
• 作者: Na, Minkyun;Kim, Bo Yeon;Ahn, Jong Seog
• 通讯作者: Ahn, Jong Seog

Functional Characterization of ttmM Unveils New Tautomycin Analogs and Insight into Tautomycin Biosynthesis and Activity

• DOI: 10.1021/ol900293j
• 发表时间: 2009-04-02
• 期刊: ORGANIC LETTERS
• 影响因子: 5.2
• 作者: Ju, Jianhua;Li, Wenli;Shen, Ben
• 通讯作者: Shen, Ben

Inhibition of Hsp90 activates osteoclast c-Src signaling and promotes growth of prostate carcinoma cells in bone

• DOI: 10.1073/pnas.0805354105
• 发表时间: 2008-10-07
• 期刊: PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
• 影响因子: 11.1
• 作者: Yano, Akihiro;Tsutsumi, Shinji;Neckers, Len
• 通讯作者: Neckers, Len

Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein

• DOI: 10.1016/j.bmc.2008.02.050
• 发表时间: 2008-04-15
• 期刊: BIOORGANIC & MEDICINAL CHEMISTRY
• 影响因子: 3.5
• 作者: Jain, Hiteshkumar D.;Zhang, Chunchun;Cook, James M.
• 通讯作者: Cook, James M.

Osteoclast-targeting small molecules for the treatment of neoplastic bone metastases

• DOI: 10.1111/j.1349-7006.2009.01294.x
• 发表时间: 2009-11-01
• 期刊: CANCER SCIENCE
• 影响因子: 5.7
• 作者: Kawatani, Makoto;Osada, Hiroyuki
• 通讯作者: Osada, Hiroyuki