Disease relevance of

• Inhibition of Escherichia coli glucosamine synthetase by novel electrophilic analogues of glutamine--comparison with 6-diazo-5-oxo-norleucine [1].

High impact information on

• Proteolytically stable peptide inhibitors of human TG2 were designed containing acivicin or alternatively 6-diazo-5-oxo-norleucine (DON) as warheads [2].
• The substitution of a glutamine residue with 6-diazo-5-oxo-norleucine (DON) transforms an immunodominant gluten peptide into a potent inhibitor of tissue transglutaminase [3].
• An inhibitor of glucosamine synthesis, 6-diazo-5-oxo-norleucine (DON) was found to inhibit glycosaminoglycan synthesis by approx. 60%, and the size of the proteoglycans was also diminished [4].
• Inhibition of morphogenetic cell interactions by 6-diazo-5-oxo-norleucine (DON) [5].
• At 8 days of development, the time of ureteral induction of the metanephric mesenchyme, 6-diazo-5-oxo-norleucine, an inhibitor of proteoglycan biosynthesis, is administered as a single microinjection into the posterolateral body wall [6].

Chemical compound and disease context of

• A series of electrophilic glutamine analogues based on 6-diazo-5-oxo-norleucine has been prepared, using novel synthetic routes, and evaluated as inhibitors of Escherichia coli glucosamine synthetase [1].

Biological context of

• Inhibition of UDP-N-acetylglucosamine biosynthesis, with 6-diazo-5-oxo-norleucine added to Lab-D, abolished most of the glucose-stimulated leptin release and downregulated leptin gene expression [7].

Anatomical context of

• On co-culture of BCG-activated macrophages and the clonal pancreatic beta-cell line BRIN-BD11, macrophage-specific beta-cell death was significantly reduced on prior exposure of macrophages to 6-diazo-5-oxo-norleucine [8].
• We also demonstrate that potent inhibition of cytokine production can be achieved by incubating macrophages or monocytes in the presence of the glutaminase inhibitor 6-diazo-5-oxo-norleucine [8].

Associations of with other chemical compounds

• Renal rudiments (7 to 9 days of incubation) were exposed to tunicamycin, 6-diazo-5-oxo-norleucine or control media in vitro and then they were permitted to develop further as grafts in ovo [9].

References