FTR1335 Is a Novel Synthetic Inhibitor of Candida albicans N-Myristoyltransferase with Fungicidal Activity(Biochemistry/Molecular Biology)

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概要

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• Inhibitors of the fungal enzyme N-myristoyltransferase (Nmt) reduce fungal growth, as this enzyme is essential for viability. We found that a newly synthesized benzothiazole derivative, (1R, 3S)-N-{2-[(cyclopeanthylcarbonyl) amino]-benzothiazol-6-yl}-3-[(2-naphthylmethyl) amino] cyclohexanecarboxamide (FTR1335), preferentially inhibited Candida albicans Nmt (CaNmt) in a dose-dependent manner. The 50% inhibitory concentration (IC_<50>) for CaNmt was 0.49 nM, which was much lower than the 5400 nM IC_<50> for human Nmt (HsNmtl). The mode of CaNmt inhibition was competitive with the substrate peptide and non-competitive with myristoyl-CoA. Moreover, FTR1335 showed strong antifungal activity in vitro, and the minimum fungicidal concentration for C. albicans was 0.78 μM. These results indicate that FTR1335 might represent a novel family of Nmt inhibitors with fungicidal activity.

• 公益社団法人日本薬学会の論文
• 2005-04-01

著者

• NAKAMURA Masataka

  Human Gene Sciences Center, Tokyo Medical and Dental University

• ISHII Fumio

  Drug Evaluation Department, Life Science Institute, SSP CO., LTD.

• Ishii Fumio

  Drug Evaluation Department Life Science Institute Ssp Co. Ltd.

• Ishii Fumio

  エスエス製薬

• Nakamura Masataka

  Human Gene Sciences Center Tokyo Medical And Dental University

• Nakazawa Kyoko

  Central Research Laboratories Ssp Co. Ltd.

• Ebara Shinji

  Human Gene Sciences Center Tokyo Medical And Dental University:central Research Laboratories Ssp Co.

• NAITO Hiroyuki

  Central Research Laboratories, SSP Co., Ltd.

• ISHII Fumio

  Central Research Laboratories, SSP Co., Ltd.

• Naito Hiroyuki

  Central Research Laboratories Ssp Co. Ltd.

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