1jld

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[[Image:1jld.gif|left|200px]]
[[Image:1jld.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1jld |SIZE=350|CAPTION= <scene name='initialview01'>1jld</scene>, resolution 2.5&Aring;
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The line below this paragraph, containing "STRUCTURE_1jld", 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=PR0:3(S)-AMINO-4-PHENYL-BUTAN-2(R)-OL'>PR0</scene>, <scene name='pdbligand=QNC:2-CARBONYLQUINOLINE'>QNC</scene>, <scene name='pdbligand=RHS:3-(CARBOXYAMIDE(2-CARBOXYAMIDE-2-TERTBUTYLETHYL))PENTAN'>RHS</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_1jld| PDB=1jld | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1jld FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1jld OCA], [http://www.ebi.ac.uk/pdbsum/1jld PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1jld RCSB]</span>
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}}
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'''POTENT HIV PROTEASE INHIBITORS CONTAINING A NOVEL (HYDROXYETHYL)AMIDE ISOSTERE'''
'''POTENT HIV PROTEASE INHIBITORS CONTAINING A NOVEL (HYDROXYETHYL)AMIDE ISOSTERE'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Tong, L.]]
[[Category: Tong, L.]]
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[[Category: complex (protease/inhibitor) aid]]
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[[Category: Hiv-2 protease]]
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[[Category: hiv-2 protease]]
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[[Category: Polyprotein]]
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[[Category: polyprotein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 21:21:52 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:35:20 2008''
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Revision as of 18:21, 2 May 2008

Image:1jld.gif

Template:STRUCTURE 1jld

POTENT HIV PROTEASE INHIBITORS CONTAINING A NOVEL (HYDROXYETHYL)AMIDE ISOSTERE


Overview

A series of HIV protease inhibitors containing a novel (hydroxyethyl)amidosuccinoyl core has been synthesized. These peptidomimetic structures inhibit viral protease activity at low nanomolar concentrations (IC50 < 10 nM for HIV-1 protease). The inhibition constant (Ki) for inhibitor 19 was determined to be 7.5 pM against HIV-1 and 1.2 nM against HIV-2 proteases, respectively. Several compounds (19-24) inhibited HIV-1 replication in cell culture assays with 50% effective concentrations (EC50) = 3.7-35 nM. This series of inhibitors was found to exhibit poor bioavailability (< 10%) in the rat, following oral administration. The synthesis and biological properties of these compounds are discussed. In addition, an X-ray structure of one of these inhibitors (23) in complex with HIV-2 protease provides insight into the binding mode of this novel class of HIV protease inhibitors.

About this Structure

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

Reference

Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere., Beaulieu PL, Wernic D, Abraham A, Anderson PC, Bogri T, Bousquet Y, Croteau G, Guse I, Lamarre D, Liard F, Paris W, Thibeault D, Pav S, Tong L, J Med Chem. 1997 Jul 4;40(14):2164-76. PMID:9216835 Page seeded by OCA on Fri May 2 21:21:52 2008

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OCA

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