Modification of the Thioglycosyl-Naphthalimides as Potent and Selective Human O-GlcNAcase Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00406
Abstract: β-N-Acetylhexosaminidases are widely distributed exoglycosidases and have attracted significant attention due to their important roles in the field of pesticide and drug discovery. Remarkably, human O-GlcNAcase (hOGA) and human β-N-acetylhexosaminidase (HsHex) possess the same catalytic… read more here.
Keywords: hoga; thioglycosyl naphthalimides; human glcnacase; naphthalimides potent ... See more keywords
Insights into activity and inhibition from the crystal structure of human O-GlcNAcase.
Sign Up to like & getrecommendations! Published in 2017 at "Nature chemical biology"
DOI: 10.1038/nchembio.2357
Abstract: O-GlcNAc hydrolase (OGA) catalyzes removal of βα-linked N-acetyl-D-glucosamine from serine and threonine residues. We report crystal structures of Homo sapiens OGA catalytic domain in apo and inhibited states, revealing a flexible dimer that displays three… read more here.
Keywords: crystal structure; activity inhibition; inhibition crystal; structure human ... See more keywords