7upj

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[[Image:7upj.gif|left|200px]]
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{{STRUCTURE_7upj| PDB=7upj | SCENE= }}
{{STRUCTURE_7upj| PDB=7upj | SCENE= }}
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'''HIV-1 PROTEASE/U101935 COMPLEX'''
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===HIV-1 PROTEASE/U101935 COMPLEX===
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==Overview==
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Recently, cyclooctylpyranone derivatives with m-carboxamide substituents (e.g. 2c) were identified as potent, nonpeptidic HIV protease inhibitors, but these compounds lacked significant antiviral activity in cell culture. Substitution of a sulfonamide group at the meta position, however, produces compounds with excellent HIV protease binding affinity and antiviral activity. Guided by an iterative structure-based drug design process, we have prepared and evaluated a number of these derivatives, which are readily available via a seven-step synthesis. A few of the most potent compounds were further evaluated for such characteristics as pharmacokinetics and toxicity in rats and dogs. From this work, the p-cyanophenyl sulfonamide derivative 35k emerged as a promising inhibitor, was selected for further development, and entered phase I clinical trials.
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(as it appears on PubMed at http://www.pubmed.gov), where 9089336 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9089336}}
==About this Structure==
==About this Structure==
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[[Category: Aspartyl protease]]
[[Category: Aspartyl protease]]
[[Category: Hydrolase]]
[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 22:47:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jul 3 15:18:19 2008''

Revision as of 12:19, 3 July 2008

Image:7upj.png

Template:STRUCTURE 7upj

HIV-1 PROTEASE/U101935 COMPLEX

Template:ABSTRACT PUBMED 9089336

About this Structure

7UPJ is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones., Skulnick HI, Johnson PD, Aristoff PA, Morris JK, Lovasz KD, Howe WJ, Watenpaugh KD, Janakiraman MN, Anderson DJ, Reischer RJ, Schwartz TM, Banitt LS, Tomich PK, Lynn JC, Horng MM, Chong KT, Hinshaw RR, Dolak LA, Seest EP, Schwende FJ, Rush BD, Howard GM, Toth LN, Wilkinson KR, Romines KR, et al., J Med Chem. 1997 Mar 28;40(7):1149-64. PMID:9089336

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