A TRANSFERASE IN DISORAZOLE SYNTHASE

二甲拉唑合成酶中的转移酶

• 批准号: 8169903
• 负责人: IRIMPAN I MATHEWS
• 金额: $ 0.3万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-05-01 至 2011-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8169903
• 关键词: Antineoplastic Agents; Apoptosis; Binding; Catalysis; Cell Death; Cell Line; Cell division; Clinical Trials; Computer Retrieval of Information on Scientific Projects Database; Epothilones; Funding; Grant; Institution; Lung; Microtubules; Multi-Drug Resistance; Ovarian; Paclitaxel; Pharmaceutical Preparations; Research; Research Personnel; Resources; Source; Transferase; Tubulin; United States National Institutes of Health; Vincristine; malignant breast neoplasm; polymerization

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Microtubules have been an attractive target for anticancer drugs since the identification and use of taxols for the treatment of lung, ovarian, and breast cancers. Taxol binds to and stabilizes microtubules, resulting in an arrest in cell division and eventual cell death. Compounds identified more recently with a similar action to taxol are the epothilones and discodermolides, both of which are in clinical trials. The disorazole A1, one of 29 related macrocyclic polyketides from a strain of Sorangium cellulosum, has been shown to inhibit the polymerization of tubulin, inducing apoptosis at picomolar concentrations. In contrast to the vincristine group of drugs, disorazoles are effective against multidrug-resistant cell lines. The structural study is aimed at understanding the mechanism of the catalysis of a transferase in disorazole synthase.

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