2q1l: Difference between revisions
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New page: left|200px<br /> <applet load="2q1l" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q1l, resolution 2.050Å" /> '''Design and Synthes... |
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[[Image:2q1l. | [[Image:2q1l.jpg|left|200px]]<br /><applet load="2q1l" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2q1l" size=" | |||
caption="2q1l, resolution 2.050Å" /> | caption="2q1l, resolution 2.050Å" /> | ||
'''Design and Synthesis of Pyrrole-based, Hepatoselective HMG-CoA Reductase Inhibitors'''<br /> | '''Design and Synthesis of Pyrrole-based, Hepatoselective HMG-CoA Reductase Inhibitors'''<br /> | ||
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==Overview== | ==Overview== | ||
This manuscript describes the design and synthesis of a series of, pyrrole-based inhibitors of HMG-CoA reductase for the treatment of, hypercholesterolemia. Analogs were optimized using structure-based design, and physical property considerations resulting in the identification of, 44, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and, chronic efficacy in a pre-clinical animal models. | This manuscript describes the design and synthesis of a series of, pyrrole-based inhibitors of HMG-CoA reductase for the treatment of, hypercholesterolemia. Analogs were optimized using structure-based design, and physical property considerations resulting in the identification of, 44, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and, chronic efficacy in a pre-clinical animal models. | ||
==About this Structure== | ==About this Structure== | ||
2Q1L 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 882 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Hydroxymethylglutaryl-CoA_reductase_(NADPH) Hydroxymethylglutaryl-CoA reductase (NADPH)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.34 1.1.1.34] Full crystallographic information is available from [http:// | 2Q1L 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=882:'>882</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Hydroxymethylglutaryl-CoA_reductase_(NADPH) Hydroxymethylglutaryl-CoA reductase (NADPH)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.34 1.1.1.34] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q1L OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: statin]] | [[Category: statin]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:32:37 2008'' | ||
