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Proteomic profiling and potential cellular target identification of K11777, a clinical cysteine protease inhibitor, in Trypanosoma brucei

机译:布氏锥虫中临床半胱氨酸蛋白酶抑制剂K11777的蛋白质组分析和潜在的细胞靶标鉴定

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摘要

We report herein the design, synthesis and application of K11777-derived activity-based probes (ABPs) allowing in situ profiling and identification of potential cellular targets of K11777 in Trypanosoma brucei. More than a billion people suffer from neglected tropical diseases (NTDs), including malaria (caused by Plasmodium falciparum), sleeping sickness (aka Human African trypano-somiasis; caused by Trypanosoma brucei), Chagas' disease (aka American trypanosomiasis; caused by Trypanosoma cruzi), leishmaniasis, onchocerciasis, lymphatic filariasis and schistosomiasis.1 Most drugs available to date however are limited by parasite resistance and marked host toxicity.
机译:我们在此报告了K11777衍生的基于活性的探针(ABP)的设计,合成和应用,可在布鲁氏锥虫中原位分析和鉴定K11777的潜在细胞靶标。超过十亿人患有被忽视的热带病(NTD),包括疟疾(由恶性疟原虫引起),昏睡病(又称人类非洲锥虫病;由布鲁氏锥虫病引起),恰加斯氏病(又称美洲锥虫病;由锥虫病引起) Cruzi),利什曼病,盘尾丝虫病,淋巴丝虫病和血吸虫病。1然而,迄今为止,大多数可用药物受到寄生虫耐药性和明显的宿主毒性的限制。

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  • 来源
    《Chemical Communications》 |2012年第6期|p.835-837|共3页
  • 作者单位

    Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543;

    Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Singapore 117543;

    Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Singapore 117543;

    Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543;

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  • 入库时间 2022-08-17 13:20:12

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