A selective inhibitor Gal-PUGNAc of human lysosomal beta-hexosaminidases modulates levels of the ganglioside GM2 in neuroblastoma cells.
Gal-PUGNAc (see picture), a highly selective inhibitor for beta-hexosaminidases HEXA and HEXB is cell-permeable and modulates the activity of HEXA and HEXB in tissue culture, increasing ganglioside GM2 levels. Gal-PUGNAc should allow the role of these enzymes to be studied at the cellular level without generating a complex chemical phenotype from concomitant inhibition of O-GlcNAcase.
Stubbs
Keith A
KA
Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada. kstubbs@cyllene.uwa.edu.au
Macauley
Matthew S
MS
Vocadlo
David J
DJ
D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism; D005678:G(M2) Ganglioside / Q000737:chemistry / Q000378:metabolism*; D054818:Hexosaminidase A / Q000037:antagonists & inhibitors / Q000378:metabolism; D054819:Hexosaminidase B / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D008247:Lysosomes / Q000201:enzymology; D009447:Neuroblastoma / Q000201:enzymology*; D013379:Substrate Specificity; D001619:beta-N-Acetylhexosaminidases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D004791:Enzyme Inhibitors; D005678:G(M2) Ganglioside; C110628:hexosaminidase C; D054818:Hexosaminidase A; D054819:Hexosaminidase B; D001619:beta-N-Acetylhexosaminidases