1tw7
From Proteopedia
(New page: 200px<br /> <applet load="1tw7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tw7, resolution 1.3Å" /> '''Wide Open 1.3A Struc...) |
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| - | [[Image:1tw7.gif|left|200px]]<br /> | + | [[Image:1tw7.gif|left|200px]]<br /><applet load="1tw7" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1tw7" size=" | + | |
caption="1tw7, resolution 1.3Å" /> | caption="1tw7, resolution 1.3Å" /> | ||
'''Wide Open 1.3A Structure of a Multi-drug Resistant HIV-1 Protease Represents a Novel Drug Target'''<br /> | '''Wide Open 1.3A Structure of a Multi-drug Resistant HIV-1 Protease Represents a Novel Drug Target'''<br /> | ||
==Overview== | ==Overview== | ||
| - | This report examines structural changes in a highly mutated, clinical | + | This report examines structural changes in a highly mutated, clinical multidrug-resistant HIV-1 protease, and the crystal structure has been solved to 1.3 A resolution in the absence of any inhibitor. This protease variant contains codon mutations at positions 10, 36, 46, 54, 62, 63, 71, 82, 84, and 90 that confer resistance to protease inhibitors. Major differences between the wild-type and the variant include a structural change initiated by the M36V mutation and amplified by additional mutations in the flaps of the protease, resulting in a "wide-open" structure that represents an opening that is 8 A wider than the "open" structure of the wild-type protease. A second structural change is triggered by the L90M mutation that results in reshaping the 23-32 segment. A third key structural change of the protease is due to the mutations from longer to shorter amino acid side chains at positions 82 and 84. |
==About this Structure== | ==About this Structure== | ||
| - | 1TW7 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 NA 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:// | + | 1TW7 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=NA:'>NA</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=1TW7 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Human immunodeficiency virus 1]] | [[Category: Human immunodeficiency virus 1]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Jimenez, Y | + | [[Category: Jimenez, Y L.]] |
| - | [[Category: Kovari, L | + | [[Category: Kovari, L C.]] |
[[Category: Martin, P.]] | [[Category: Martin, P.]] | ||
| - | [[Category: Merigan, T | + | [[Category: Merigan, T C.]] |
[[Category: Proteasa, G.]] | [[Category: Proteasa, G.]] | ||
| - | [[Category: Vickrey, J | + | [[Category: Vickrey, J F.]] |
[[Category: Wawrzak, Z.]] | [[Category: Wawrzak, Z.]] | ||
| - | [[Category: Winters, M | + | [[Category: Winters, M A.]] |
[[Category: NA]] | [[Category: NA]] | ||
[[Category: aids]] | [[Category: aids]] | ||
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[[Category: polyprotein]] | [[Category: polyprotein]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:18:02 2008'' |
Revision as of 13:18, 21 February 2008
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Wide Open 1.3A Structure of a Multi-drug Resistant HIV-1 Protease Represents a Novel Drug Target
Overview
This report examines structural changes in a highly mutated, clinical multidrug-resistant HIV-1 protease, and the crystal structure has been solved to 1.3 A resolution in the absence of any inhibitor. This protease variant contains codon mutations at positions 10, 36, 46, 54, 62, 63, 71, 82, 84, and 90 that confer resistance to protease inhibitors. Major differences between the wild-type and the variant include a structural change initiated by the M36V mutation and amplified by additional mutations in the flaps of the protease, resulting in a "wide-open" structure that represents an opening that is 8 A wider than the "open" structure of the wild-type protease. A second structural change is triggered by the L90M mutation that results in reshaping the 23-32 segment. A third key structural change of the protease is due to the mutations from longer to shorter amino acid side chains at positions 82 and 84.
About this Structure
1TW7 is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.
Reference
"Wide-open" 1.3 A structure of a multidrug-resistant HIV-1 protease as a drug target., Martin P, Vickrey JF, Proteasa G, Jimenez YL, Wawrzak Z, Winters MA, Merigan TC, Kovari LC, Structure. 2005 Dec;13(12):1887-95. PMID:16338417
Page seeded by OCA on Thu Feb 21 15:18:02 2008
