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1jld

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[[Image:1jld.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1jld| PDB=1jld | SCENE= }}
{{STRUCTURE_1jld| PDB=1jld | SCENE= }}
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'''POTENT HIV PROTEASE INHIBITORS CONTAINING A NOVEL (HYDROXYETHYL)AMIDE ISOSTERE'''
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===POTENT HIV PROTEASE INHIBITORS CONTAINING A NOVEL (HYDROXYETHYL)AMIDE ISOSTERE===
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==Overview==
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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 &lt; 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 (&lt; 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.
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The line below this paragraph, {{ABSTRACT_PUBMED_9216835}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 9216835 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9216835}}
==About this Structure==
==About this Structure==
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[[Category: Hiv-2 protease]]
[[Category: Hiv-2 protease]]
[[Category: Polyprotein]]
[[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 Tue Jul 1 20:25:28 2008''

Revision as of 17:25, 1 July 2008

Image:1jld.png

Template:STRUCTURE 1jld

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

Template:ABSTRACT PUBMED 9216835

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 Tue Jul 1 20:25:28 2008

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