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| {{STRUCTURE_1em6| PDB=1em6 | SCENE= }} | | {{STRUCTURE_1em6| PDB=1em6 | SCENE= }} |
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| '''HUMAN LIVER GLYCOGEN PHOSPHORYLASE A COMPLEXED WITH GLCNAC AND CP-526,423'''
| | ===HUMAN LIVER GLYCOGEN PHOSPHORYLASE A COMPLEXED WITH GLCNAC AND CP-526,423=== |
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| ==Overview==
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| Background: Glycogen phosphorylases catalyze the breakdown of glycogen to glucose-1-phosphate for glycolysis. Maintaining control of blood glucose levels is critical in minimizing the debilitating effects of diabetes, making liver glycogen phosphorylase a potential therapeutic target.Results: The binding site in human liver glycogen phosphorylase (HLGP) for a class of promising antidiabetic agents was identified crystallographically. The site is novel and functions allosterically by stabilizing the inactive conformation of HLGP. The initial view of the complex revealed key structural information and inspired the design of a new class of inhibitors which bind with nanomolar affinity and whose crystal structure is also described. Conclusions: We have identified the binding site of a new class of allosteric HLGP inhibitors. The crystal structure revealed the details of inhibitor binding, led to the design of a new class of compounds, and should accelerate efforts to develop therapeutically relevant molecules for the treatment of diabetes.
| | The line below this paragraph, {{ABSTRACT_PUBMED_10980448}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 10980448 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_10980448}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Allosteric binding]] | | [[Category: Allosteric binding]] |
| [[Category: Allosteric site]] | | [[Category: Allosteric site]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 15:16:01 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 00:58:11 2008'' |
