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research article
Functionalized pyrrolidine inhibitors of human alpha- mannosidases II in cancer: optimizing the fit to the active site
Refining the chemical structure of functionalized pyrrolidine-based inhibitors of Golgi α- mannosidase II (GMII) to optimize binding affinity provided a lead molecule that demonstrated nanomolar competitive inhibition of α-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.
Type
research article
Web of Science ID
WOS:000258749500028
Authors
•
Kuntz, Douglas A.
•
Janzer, Robert C.
•
•
Rose, David R.
•
Juillerat-Jeanneret, Lucienne
Publication date
2008
Published in
Volume
16
Start page
7337
End page
7346
Peer reviewed
REVIEWED
EPFL units
Available on Infoscience
June 5, 2008
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