1qbr

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[[Image:1qbr.gif|left|200px]]
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{{Seed}}
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[[Image:1qbr.png|left|200px]]
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{{STRUCTURE_1qbr| PDB=1qbr | SCENE= }}
{{STRUCTURE_1qbr| PDB=1qbr | SCENE= }}
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'''HIV-1 PROTEASE INHIBITORS WIIH LOW NANOMOLAR POTENCY'''
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===HIV-1 PROTEASE INHIBITORS WIIH LOW NANOMOLAR POTENCY===
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==Overview==
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Cyclic urea amides, a novel series of HIV-1 protease (HIV PR) inhibitors, have increased activity against drug-resistant mutants of the HIV PR. The design strategy for these inhibitors is based on the hypotheses that (i) the hydrogen-bonding interactions between the inhibitor and the protease backbone will remain constant for wild-type and mutant enzymes and (ii) inhibitors which are capable of forming many nonbonded interactions, distributed throughout the active site, will experience a lower percent change in binding energy as a result of mutation in the target enzyme than those that form fewer interactions by partial occupation of the active site. The cyclic urea amide, SD146, forms 14 hydrogen bonds and 191 van der Waals contacts to HIV PR. SD146 is a very potent antiviral agent (IC90 = 5.1 nM) against wild-type HIV and maintains the same or improved level of high potency against a range of mutant strains of HIV with resistance to a wide variety of HIV protease inhibitors.
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The line below this paragraph, {{ABSTRACT_PUBMED_9003516}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 9003516 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9003516}}
==About this Structure==
==About this Structure==
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[[Category: Chang, C H.]]
[[Category: Chang, C H.]]
[[Category: Aspartyl protease]]
[[Category: Aspartyl protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:06:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:38:23 2008''

Revision as of 23:38, 27 July 2008

Image:1qbr.png

Template:STRUCTURE 1qbr

HIV-1 PROTEASE INHIBITORS WIIH LOW NANOMOLAR POTENCY

Template:ABSTRACT PUBMED 9003516

About this Structure

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

Reference

Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV., Jadhav PK, Ala P, Woerner FJ, Chang CH, Garber SS, Anton ED, Bacheler LT, J Med Chem. 1997 Jan 17;40(2):181-91. PMID:9003516

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