2rf2

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==Overview==
==Overview==
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This Letter describes the design, synthesis, and biological evaluation of, novel 3-indole sulfonamides as potent non-nucleoside reverse transcriptase, inhibitors (NNRTIs) with balanced profiles against common HIV RT mutants, K103N and Y181C.
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This Letter describes the design, synthesis, and biological evaluation of novel 3-indole sulfonamides as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with balanced profiles against common HIV RT mutants K103N and Y181C.
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)., Zhao Z, Wolkenberg SE, Lu M, Munshi V, Moyer G, Feng M, Carella AV, Ecto LT, Gabryelski LJ, Lai MT, Prasad SG, Yan Y, McGaughey GB, Miller MD, Lindsley CW, Hartman GD, Vacca JP, Williams TM, Bioorg Med Chem Lett. 2007 Nov 28;. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18083561 18083561]
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Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)., Zhao Z, Wolkenberg SE, Lu M, Munshi V, Moyer G, Feng M, Carella AV, Ecto LT, Gabryelski LJ, Lai MT, Prasad SG, Yan Y, McGaughey GB, Miller MD, Lindsley CW, Hartman GD, Vacca JP, Williams TM, Bioorg Med Chem Lett. 2008 Jan 15;18(2):554-9. Epub 2007 Nov 28. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18083561 18083561]
[[Category: Human immunodeficiency virus 1]]
[[Category: Human immunodeficiency virus 1]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: zinc-finger]]
[[Category: zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 13 08:18:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:46:45 2008''

Revision as of 16:46, 21 February 2008


2rf2, resolution 2.4Å

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HIV reverse transcriptase in complex with inhibitor 7e (NNRTI)

Overview

This Letter describes the design, synthesis, and biological evaluation of novel 3-indole sulfonamides as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with balanced profiles against common HIV RT mutants K103N and Y181C.

About this Structure

2RF2 is a Protein complex structure of sequences from Human immunodeficiency virus 1 with as ligand. Active as RNA-directed DNA polymerase, with EC number 2.7.7.49 Known structural/functional Site: . Full crystallographic information is available from OCA.

Reference

Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)., Zhao Z, Wolkenberg SE, Lu M, Munshi V, Moyer G, Feng M, Carella AV, Ecto LT, Gabryelski LJ, Lai MT, Prasad SG, Yan Y, McGaughey GB, Miller MD, Lindsley CW, Hartman GD, Vacca JP, Williams TM, Bioorg Med Chem Lett. 2008 Jan 15;18(2):554-9. Epub 2007 Nov 28. PMID:18083561

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