2fix: Difference between revisions
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New page: left|200px<br /> <applet load="2fix" size="450" color="white" frame="true" align="right" spinBox="true" caption="2fix, resolution 3.50Å" /> '''Structure of human ... |
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[[Image:2fix.gif|left|200px]]<br /> | [[Image:2fix.gif|left|200px]]<br /><applet load="2fix" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2fix" size=" | |||
caption="2fix, resolution 3.50Å" /> | caption="2fix, resolution 3.50Å" /> | ||
'''Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors'''<br /> | '''Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors'''<br /> | ||
==Overview== | ==Overview== | ||
A series of novel benzoxazole benzenesulfonamides was synthesized as | A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53, with an IC(50) of 0.57microM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats. | ||
==Disease== | ==Disease== | ||
Known disease associated with this structure: Fructose- | Known disease associated with this structure: Fructose-1,6-bidphosphatase deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=611570 611570]] | ||
==About this Structure== | ==About this Structure== | ||
2FIX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 870 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Fructose-bisphosphatase Fructose-bisphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.11 3.1.3.11] Full crystallographic information is available from [http:// | 2FIX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=870:'>870</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Fructose-bisphosphatase Fructose-bisphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.11 3.1.3.11] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FIX OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: intersubunit allosteric inhibitors of human liver fbpase]] | [[Category: intersubunit allosteric inhibitors of human liver fbpase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:21:51 2008'' | ||
