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- W1990259368 abstract "NAG‐thiazoline (NGT) and its derivatives are well‐known inhibitors against most β‐acetylglucosaminidases (β‐GlcNAcases) except for insect and bacterial chitinolytic β‐GlcNAcases, including the molting‐indispensable OfHex1 from the insect Ostrinia furnacalis . Here, we report the co‐crystal structure of OfHex1 in complex with NGT. This structure reveals a large active pocket in OfHex1 that may account for the poor inhibitory activity of NGT. To test this hypothesis, a bulky substituent was designed and synthesized on the thiazoline ring of NGT. The resulting compound (NMAGT) was determined to be a submicromolar inhibitor of OfHex1 with a K i value of 0.13 μM, which is 600‐fold lower than K i value of NGT. Molecular dynamics simulation analysis supported the good fit of NMAGT to the active pocket." @default.
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- W1990259368 date "2014-11-29" @default.
- W1990259368 modified "2023-10-13" @default.
- W1990259368 title "Exploring NAG‐thiazoline and its derivatives as inhibitors of chitinolytic β‐acetylglucosaminidases" @default.
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- W1990259368 doi "https://doi.org/10.1016/j.febslet.2014.11.032" @default.
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