Selected article for: "catalytic domain and crystal structure"

Author: Lee, Youngjin; Ryu, Young Bae; Youn, Hyung-Seop; Cho, Jung Keun; Kim, Young Min; Park, Ji-Young; Lee, Woo Song; Park, Ki Hun; Eom, Soo Hyun
Title: Structural basis of sialidase in complex with geranylated flavonoids as potent natural inhibitors
  • Cord-id: i08zc62d
  • Document date: 2014_4_30
  • ID: i08zc62d
    Snippet: Sialidase catalyzes the removal of a terminal sialic acid from glycoconjugates and plays a pivotal role in nutrition, cellular interactions and pathogenesis mediating various infectious diseases including cholera, influenza and sepsis. An array of antiviral sialidase agents have been developed and are commercially available, such as zanamivir and oseltamivir for treating influenza. However, the development of bacterial sialidase inhibitors has been much less successful. Here, natural polyphenoli
    Document: Sialidase catalyzes the removal of a terminal sialic acid from glycoconjugates and plays a pivotal role in nutrition, cellular interactions and pathogenesis mediating various infectious diseases including cholera, influenza and sepsis. An array of antiviral sialidase agents have been developed and are commercially available, such as zanamivir and oseltamivir for treating influenza. However, the development of bacterial sialidase inhibitors has been much less successful. Here, natural polyphenolic geranylated flavonoids which show significant inhibitory effects against Cp-NanI, a sialidase from Clostridium perfringens, are reported. This bacterium causes various gastrointestinal diseases. The crystal structure of the Cp-NanI catalytic domain in complex with the best inhibitor, diplacone, is also presented. This structure explains how diplacone generates a stable enzyme–inhibitor complex. These results provide a structural framework for understanding the interaction between sialidase and natural flavonoids, which are promising scaffolds on which to discover new anti-sialidase agents.

    Search related documents:
    Co phrase search for related documents
    • acid sodium and acute respiratory syndrome: 1, 2, 3, 4, 5
    • active site and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25
    • active site and low sequence: 1, 2, 3, 4, 5
    • active site and low sequence identity: 1
    • active site enzyme and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17
    • activity screen and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7
    • activity screening and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11
    • acute respiratory syndrome and additional hydrogen bond: 1
    • acute respiratory syndrome and logistic curve: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10
    • acute respiratory syndrome and low homology: 1, 2, 3, 4, 5
    • acute respiratory syndrome and low sequence: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10
    • acute respiratory syndrome and low sequence identity: 1, 2, 3
    • acute respiratory syndrome and luria lb bertani: 1