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PDBsum entry 3ddf
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References listed in PDB file
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Key reference
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Title
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Functionalized pyrrolidine inhibitors of human type ii alpha-Mannosidases as anti-Cancer agents: optimizing the fit to the active site.
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Authors
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H.Fiaux,
D.A.Kuntz,
D.Hoffman,
R.C.Janzer,
S.Gerber-Lemaire,
D.R.Rose,
L.Juillerat-Jeanneret.
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Ref.
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Bioorg Med Chem Lett, 2008,
16,
7337-7346.
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PubMed id
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Abstract
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Refining the chemical structure of functionalized pyrrolidine-based inhibitors
of Golgi alpha-mannosidase II (GMII) to optimize binding affinity provided a
lead molecule that demonstrated nanomolar competitive inhibition of
alpha-mannosidases II and an optimal fit in the active site of Drosophila GMII
by X-ray crystallography. Esters of this lead compound also inhibited the growth
of human glioblastoma and brain-derived endothelial cells more than the growth
of non-tumoral human fibroblasts, suggesting their potential for anti-cancer
therapy.
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