Selected article for: "active site and close proximity"

Author: Powers, Chelsea N.; Setzer, William N.
Title: An In-Silico Investigation of Phytochemicals as Antiviral Agents Against Dengue Fever
  • Document date: 2016_8_23
  • ID: q7thhtg3_27
    Snippet: In addition to docking energies, it is useful to consider proximity of electrophilic ligands (e.g., epoxides or enones) to nucleophilic residues in the active site. A search of the docked ligands with DENV protease has revealed three sesquiterpenoid -methylene lactones that dock in close proximity to the -OH group of Ser196. Ineupatorolide A, bigelovin, and 2-de-ethoxy-2-methoxyphantomolin (Fig. 2) dock with the methylene carbon within 3.6 Ã… of .....
    Document: In addition to docking energies, it is useful to consider proximity of electrophilic ligands (e.g., epoxides or enones) to nucleophilic residues in the active site. A search of the docked ligands with DENV protease has revealed three sesquiterpenoid -methylene lactones that dock in close proximity to the -OH group of Ser196. Ineupatorolide A, bigelovin, and 2-de-ethoxy-2-methoxyphantomolin (Fig. 2) dock with the methylene carbon within 3.6 Ã… of the serine -OH. These ligands can presumably undergo conjugate addition with the -OH group and form a covalent intermediate thereby inhibiting the protease.

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