2q3k: Difference between revisions
New page: left|200px<br /> <applet load="2q3k" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q3k, resolution 2.00Å" /> '''Crystal Structure o... |
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'''Crystal Structure of Lysine Sulfonamide Inhibitor Reveals the Displacement of the Conserved Flap Water Molecule in HIV-1 Protease'''<br /> | '''Crystal Structure of Lysine Sulfonamide Inhibitor Reveals the Displacement of the Conserved Flap Water Molecule in HIV-1 Protease'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2Q3K 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 PO4, ACT and MUW as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | 2Q3K 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=PO4:'>PO4</scene>, <scene name='pdbligand=ACT:'>ACT</scene> and <scene name='pdbligand=MUW:'>MUW</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q3K OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: viral protein]] | [[Category: viral protein]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:06:15 2008'' | ||
Revision as of 10:06, 23 January 2008
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Crystal Structure of Lysine Sulfonamide Inhibitor Reveals the Displacement of the Conserved Flap Water Molecule in HIV-1 Protease
Overview
Human immunodeficiency virus type 1 (HIV-1) protease has been continuously, evolving and developing resistance to all of the protease inhibitors. This, requires the development of new inhibitors that bind to the protease in a, novel fashion. Most of the inhibitors that are on the market are, peptidomimetics, where a conserved water molecule mediates hydrogen, bonding interactions between the inhibitors and the flaps of the protease., Recently a new class of inhibitors, lysine sulfonamides, was developed to, combat the resistant variants of HIV protease. Here we report the crystal, structure of a lysine sulfonamide. This inhibitor binds to the active site, of HIV-1 protease in a novel manner, displacing the conserved water and, making extensive hydrogen bonds with every region of the active site.
About this Structure
2Q3K is a Single protein structure of sequence from Human immunodeficiency virus 1 with PO4, ACT and MUW as ligands. Full crystallographic information is available from OCA.
Reference
Crystal structure of lysine sulfonamide inhibitor reveals the displacement of the conserved flap water molecule in human immunodeficiency virus type 1 protease., Nalam MN, Peeters A, Jonckers TH, Dierynck I, Schiffer CA, J Virol. 2007 Sep;81(17):9512-8. Epub 2007 Jun 27. PMID:17596316
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