Results 161 to 170 of about 4,448 (184)
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Synthesis of NAM-thiazoline derivatives as novel O-GlcNAcase inhibitors
Carbohydrate Research, 2016Human O-GlcNAcase (GH 84) and human β-N-acetyl-D-hexosaminidase (GH 20) from Homo sapiens are two therapeutic enzyme targets that share the same catalytic mechanism but play different physiological roles in vivo. Selective inhibition toward one of these enzymes is therefore of importance to regulate the corresponding bioprocess.
Tian Liu, Huizhe Lu, Qing Yang
exaly +3 more sources
Enzymatic characterization and inhibition of the nuclear variant of human O-GlcNAcase [PDF]
Carbohydrate Research, 2009 Increasing cellular O-GlcNAc levels through pharmacological inhibition of O-GlcNAcase, the enzyme responsible for removal of the O-GlcNAc post-translational modification, is being increasingly used to aid in discerning the roles played by this form of intracellular glycosylation.
Matthew S Macauley, David J Vocadlo
exaly +4 more sources
Location and characterization of the O-GlcNAcase active site
Biochimica et Biophysica Acta (BBA) - General Subjects, 2006NCOAT is a bifunctional nucleo-cytoplasmic protein with both O-GlcNAcase and histone acetyltransferase domains. The O-GlcNAcase domain catalyzes the removal of O-linked GlcNAc modifications from proteins and we have found that it resides in the N-terminal third of NCOAT.
Clifford, Toleman +2 more
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Isoforms of human O-GlcNAcase show distinct catalytic efficiencies
Biochemistry (Moscow), 2010O-GlcNAcase (OGA) is a family 84 glycoside hydrolase catalyzing the hydrolytic cleavage of O-linked beta-N-acetylglucosamine (O-GlcNAc) from serine and threonine residues of proteins. Thus far, three forms of OGA have been identified in humans. Here we optimized the expression of these isoforms in E.
Jing, Li +6 more
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O‐GlcNAcase is essential for embryonic development and maintenance of genomic stability [PDF]
Aging Cell, 2012 SummaryDysregulation of O‐GlcNAc modification catalyzed by O‐GlcNAc transferase (OGT) and O‐GlcNAcase (OGA) contributes to the etiology of chronic diseases of aging, including cancer, cardiovascular disease, type 2 diabetes, and Alzheimer’s disease.
Minseok Song +2 more
exaly +4 more sources
Structure and mechanism of a bacterial β-glucosaminidase having O-GlcNAcase activity
Nature Structural and Molecular Biology, 2006 O-GlcNAc is an abundant post-translational modification of serine and threonine residues of nucleocytoplasmic proteins. This modification, found only within higher eukaryotes, is a dynamic modification that is often reciprocal to phosphorylation. In a manner analogous to phosphatases, a glycoside hydrolase termed O-GlcNAcase cleaves O-GlcNAc from ...
Keith A Stubbs +2 more
exaly +3 more sources
Structural insight into the mechanism of streptozotocin inhibition of O-GlcNAcase
Carbohydrate Research, 2009Despite decades of its use in diabetes research, the mechanism of cytotoxicity of streptozotocin (STZ) toward pancreatic beta-islet cells has remained a topic of discussion. Although STZ toxicity is likely a function of its capacity to promote DNA alkylation, it has been proposed that STZ induces pancreatic beta-cell death through O-GlcNAcase ...
Yuan, He +4 more
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Streptozotocin, an O-GlcNAcase inhibitor, blunts insulin and growth hormone secretion
Molecular and Cellular Endocrinology, 2002Type 2 diabetes mellitus results from a complex interaction between nutritional excess and multiple genes. Whereas pancreatic beta-cells normally respond to glucose challenge by rapid insulin release (first phase insulin secretion), there is a loss of this acute response in virtually all of the type 2 diabetes patients with significant fasting ...
Kan, Liu +7 more
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Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry
Bioorganic and Medicinal Chemistry, 2006The potent O-GlcNAcase inhibitor PUGNAc was synthesized and two isomers based on the E and Z stereochemistry of the oxime moiety were separated, defined, and tested for activity. Several lines of evidence were examined in an effort to define the correct stereochemical assignments of each form of PUGNAc.
John A Hanover, Eun Ju Kim
exaly +3 more sources
Streptozotocin inhibits O-GlcNAcase via the production of a transition state analog
Biochemical and Biophysical Research Communications, 2006Streptozotocin (STZ) is a 2-deoxy-d-glucopyranose derivative of a class of drugs known as alkylnitrosoureas, and is an established diabetogenic agent whose cytotoxic affects on pancreatic beta-cells has been partially explained by the presence of its N-methyl-N-nitrosourea side chain, which has the ability to release nitric oxide as well as donate ...
Clifford, Toleman +3 more
openaire +2 more sources