2fdd

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[[Image:2fdd.gif|left|200px]]
[[Image:2fdd.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2fdd |SIZE=350|CAPTION= <scene name='initialview01'>2fdd</scene>, resolution 1.58&Aring;
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The line below this paragraph, containing "STRUCTURE_2fdd", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=385:(3R,3AS,6AR)-HEXAHYDROFURO[2,3-B]FURAN-3-YL+[(1S,2R)-3-[(1,3-BENZODIOXOL-5-YLSULFONYL)(ISOBUTYL)AMINO]-2-HYDROXY-1-{4-[(2-METHYL-1,3-THIAZOL-4-YL)METHOXY]BENZYL}PROPYL]CARBAMATE'>385</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2fdd| PDB=2fdd | SCENE= }}
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|RELATEDENTRY=[[2fde|2FDE]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fdd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fdd OCA], [http://www.ebi.ac.uk/pdbsum/2fdd PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fdd RCSB]</span>
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}}
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'''Crystal structure of HIV protease D545701 bound with GW0385'''
'''Crystal structure of HIV protease D545701 bound with GW0385'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Xu, R X.]]
[[Category: Xu, R X.]]
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[[Category: hiv protease]]
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[[Category: Hiv protease]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:45:31 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:01:15 2008''
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Revision as of 00:45, 4 May 2008

Image:2fdd.gif

Template:STRUCTURE 2fdd

Crystal structure of HIV protease D545701 bound with GW0385


Overview

A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.

About this Structure

2FDD is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385., Miller JF, Andrews CW, Brieger M, Furfine ES, Hale MR, Hanlon MH, Hazen RJ, Kaldor I, McLean EW, Reynolds D, Sammond DM, Spaltenstein A, Tung R, Turner EM, Xu RX, Sherrill RG, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1788-94. Epub 2006 Feb 3. PMID:16458505 Page seeded by OCA on Sun May 4 03:45:31 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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