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Development of Sulfo-Sialic Acids into Next-Generation Antimicrobial Agents

Research Project

Project/Area Number 18K06577
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
Research InstitutionKobe University

Principal Investigator

Vavricka Christopher  神戸大学, 科学技術イノベーション研究科, 准教授 (20809199)

Co-Investigator(Kenkyū-buntansha) 清田 洋正  岡山大学, 環境生命科学研究科, 教授 (30234397)
Project Period (FY) 2018-04-01 – 2021-03-31
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2020: ¥260,000 (Direct Cost: ¥200,000、Indirect Cost: ¥60,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
KeywordsSynthetic biology / Sulfo-sialic acid / Fluorine / Covalent inhibitor / Neuraminidase (NA) / Antivirals / Anomeric sulfo / Anomeric phosphono / NA inhibitor / Anomeric sulfonate / Bioproduction / Anti-virals / Sialic acid / Sulfonic acids / Neuraminidase / Covalent inhibitors / Microwave reaction / Decarboxylation / Fluoro sugars / Influenza neuraminidase / Drug development / Novel carbohydrates
Outline of Final Research Achievements

Fluorinated sulfonates and phosphonates were designed as inhibitors of sialic acid binding viruses. Three milestones were reached to produce target sialic acid analogues: 1) C-2 fluorine introduction into pyranose analogues, 2) introduction of fluorine and hydroxy groups into C-1 and C-2 positions of open-chain analogues, and 3) substitution of the sialic acid anomeric carboxy with a sulfonamide group.

Academic Significance and Societal Importance of the Research Achievements

このプロジェクトで開発した化合物群は、将来の感染爆発(パンデミック)に備えた抗ウィルス薬リードとして役立つものです。そして、薬剤耐性を獲得した微生物・ウィルスにも幅広く効果を示す可能性を持っています。さらには、本化合物群の微生物生産システムも構築しました。本手法は、従来、高価値な医薬品製造のために行っていた工業化学的プロセスを代替する持続可能な手段となり得ます。

Report

(4 results)
  • 2020 Annual Research Report   Final Research Report ( PDF )
  • 2019 Research-status Report
  • 2018 Research-status Report

Research Products

(8 results)

All 2020 2019 2018

All Journal Article (4 results) (of which Int'l Joint Research: 2 results,  Peer Reviewed: 3 results,  Open Access: 2 results) Presentation (4 results)

  • [Journal Article] Towards Improvement of Covalent Neuraminidase Inhibitors with Anomeric Substitution2020

    • Author(s)
      Christopher J. Vavricka, Tatsuma Matsumoto, Hiromasa Kiyota
    • Journal Title

      TIGG

      Volume: 32 Issue: 185 Pages: E1-E5

    • DOI

      10.4052/tigg.1801.1e

      10.4052/tigg.1801.1E

    • NAID

      130007790321

    • ISSN
      0915-7352, 1883-2113
    • Related Report
      2020 Annual Research Report 2019 Research-status Report 2018 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Dynamic Metabolomics for Engineering Biology: Accelerating Learning Cycles for Bioproduction2020

    • Author(s)
      Vavricka Christopher J.、Hasunuma Tomohisa、Kondo Akihiko
    • Journal Title

      Trends in Biotechnology

      Volume: 38 Pages: 68-82

    • DOI

      10.1016/j.tibtech.2019.07.009

    • Related Report
      2020 Annual Research Report 2019 Research-status Report
  • [Journal Article] Single-Stage Astaxanthin Production Enhances the Nonmevalonate Pathway and Photosynthetic Central Metabolism in Synechococcus sp. PCC 70022019

    • Author(s)
      Tomohisa Hasunuma, Ayako Takaki, Mami Matsuda, Yuichi Kato, Christopher J. Vavricka, Akihiko Kondo
    • Journal Title

      ACS Synthetic Biology

      Volume: 8 Pages: 2701-2709

    • DOI

      10.1021/acssynbio.9b00280

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] Mechanism-based tuning of insect 3,4-dihydroxyphenylacetaldehyde synthase for synthetic bioproduction of benzylisoquinoline alkaloids2019

    • Author(s)
      Christopher J. Vavricka, Takanobu Yoshida, Yuki Kuriya, Shunsuke Takahashi, Teppei Ogawa, Fumie Ono, Kazuko Agari, Hiromasa Kiyota, Jianyong Li, Jun Ishii, Kenji Tsuge, Hiromichi Minami, Michihiro Araki, Tomohisa Hasunuma, Akihiko Kondo
    • Journal Title

      Nature Communications

      Volume: 10 Pages: 2015-2015

    • DOI

      10.1038/s41467-019-09610-2

    • NAID

      120006778260

    • Related Report
      2019 Research-status Report 2018 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Presentation] Genome-scale prediction of gene ontology from yeast knockout MASS fingerprints2019

    • Author(s)
      VAVRICKA, CHRISTOPHER JOHN
    • Organizer
      Frontiers in Genome Engineering 2019
    • Related Report
      2019 Research-status Report
  • [Presentation] Application of the design, build, test and learn paradigm to the discovery and engineering of specialized aromatic aldehyde synthases2019

    • Author(s)
      VAVRICKA, CHRISTOPHER JOHN, 清田洋正, 荒木通啓, 近藤昭彦, 蓮沼誠久
    • Organizer
      The 37th Symposium on Environmental Science of Pesticide
    • Related Report
      2019 Research-status Report
  • [Presentation] Re-design, synthesis, and bio-analysis of sulfosialic acids as covalent inhibitors of neuraminidase2019

    • Author(s)
      VAVRICKA, CHRISTOPHER JOHN, 松本 達磨, 荒木 通啓, 蓮沼 誠久, 泉 実, 清田 洋正
    • Organizer
      第61回天然有機化合物討論会 2019年9月
    • Related Report
      2019 Research-status Report
  • [Presentation] シアル酸1位置換誘導体の合成研究2018

    • Author(s)
      松本達磨、武藤千明、森さおり、Christopher J. Vavricka、蓮沼誠久、泉実、清田洋正
    • Organizer
      農芸化学会中四国支部大会
    • Related Report
      2018 Research-status Report

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Published: 2018-04-23   Modified: 2022-01-27  

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