Synthesis and biological evaluation of d-gluconhydroximo-1,5-lactam and its oxime-substituted derivatives as pharmacological chaperones for the treatment of Gaucher disease
MedChemComm, ISSN: 2040-2511, Vol: 7, Issue: 2, Page: 365-370
2016
- 5Citations
- 13Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Article Description
d-Gluconhydroximo-1,5-lactam and its oxime-substituted derivatives were prepared and assessed for inhibition and pharmacological chaperone (PC) activities in Gaucher disease cell lines derived from N370S. The most active compound, O-(d-glucopyranosylidene) amino-Z-N-dodecylcarbamate (38), gave a nearly 2.0-fold increase in N370S β-GCase activity at 12.5 μM with no inhibition to other commercially available glucosidases. Docking studies of ligand-enzyme interactions have also been conducted to account for the results of enzyme activity increase. All these results demonstrate that compound 38 is a promising PC for the treatment of GD.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84958967996&origin=inward; http://dx.doi.org/10.1039/c5md00501a; https://xlink.rsc.org/?DOI=C5MD00501A; http://xlink.rsc.org/?DOI=C5MD00501A; http://pubs.rsc.org/en/content/articlepdf/2016/MD/C5MD00501A; https://dx.doi.org/10.1039/c5md00501a; https://pubs.rsc.org/en/content/articlelanding/2016/md/c5md00501a
Royal Society of Chemistry (RSC)
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