2bb9: Difference between revisions
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New page: left|200px<br /> <applet load="2bb9" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bb9, resolution 1.35Å" /> '''Structure of HIV1 p... |
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[[Image:2bb9.gif|left|200px]]<br /> | [[Image:2bb9.gif|left|200px]]<br /><applet load="2bb9" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2bb9" size=" | |||
caption="2bb9, resolution 1.35Å" /> | caption="2bb9, resolution 1.35Å" /> | ||
'''Structure of HIV1 protease and AKC4p_133a complex.'''<br /> | '''Structure of HIV1 protease and AKC4p_133a complex.'''<br /> | ||
==Overview== | ==Overview== | ||
A series of monopyrrolinone-based HIV-1 protease inhibitors possessing | A series of monopyrrolinone-based HIV-1 protease inhibitors possessing rationally designed P2' side chains have been synthesized and evaluated for activity against wild-type HIV-1 protease. The most potent inhibitor displays subnanomolar potency in vitro for the wild-type HIV-1 protease. Additionally, the monopyrrolinone inhibitors retain potency in cellular assays against clinically significant mutant forms of the virus. X-ray structures of these inhibitors bound in the wild-type enzyme reveal important insights into the observed biological activity. | ||
==About this Structure== | ==About this Structure== | ||
2BB9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with AKC as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http:// | 2BB9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=AKC:'>AKC</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BB9 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Human immunodeficiency virus 1]] | [[Category: Human immunodeficiency virus 1]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Charnley, A | [[Category: Charnley, A K.]] | ||
[[Category: III, A | [[Category: III, A B.Smith.]] | ||
[[Category: Kuo, L | [[Category: Kuo, L C.]] | ||
[[Category: Munshi, S.]] | [[Category: Munshi, S.]] | ||
[[Category: AKC]] | [[Category: AKC]] | ||
[[Category: protease]] | [[Category: protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:35:56 2008'' | ||
