| Structural highlights
2won is a 2 chain structure with sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Related: | 1odw, 1hvr, 1rth, 1bwa, 1rev, 1bvg, 1c0t, 1s1x, 1vru, 1rt5, 1dmp, 1bwb, 1g6l, 1tl1, 1rt3, 1bv9, 1lwc, 1rtj, 1s1t, 1jlc, 1t05, 1hxb, 1hvh, 1jlq, 1jla, 1ncp, 1jlg, 1rt4, 1fk9, 1jlb, 1rt6, 1hwr, 1rtd, 1lw0, 1qbs, 1a30, 1s1v, 1ex4, 1qbr, 1ep4, 1qbt, 1c0u, 1tkt, 1o1w, 1dtq, 1dtt, 1jlf, 1e6j, 1s1u, 1s1w, 1rti, 1tkx, 1fb7, 1jkh, 1qbu, 1tl3, 1lw2, 3phv, 1jle, 1c1b, 1rt7, 1rt1, 1lwe, 1hiv, 1klm, 1fko, 1rt2, 1tkz, 1exq, 1lv1, 1ody, 1c1c, 1esk, 1tam, 1bv7, 1fkp, 1vrt, 1lwf, 1bve |
| Activity: | RNA-directed DNA polymerase, with EC number 2.7.7.49 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
The non-nucleoside reverse transcriptase inhibitors (NNRTIs) are key components of highly active antiretroviral therapy (HAART) for the treatment of HIV-1. A major problem with the first approved NNRTIs was the emergence of mutations in the HIV-1 reverse transcriptase (RT), in particular K103N and Y181C, which led to resistance to the entire class. We adopted an iterative strategy to synthesize and test small molecule inhibitors from a chemical series of pyrazoles against wild-type (wt) RT and the most prevalent NNRTI resistant mutants. The emerging candidate, lersivirine (UK-453,061), binds the RT enzyme in a novel way (resulting in a unique resistance profile), inhibits over 60% of viruses bearing key RT mutations with EC50 values within 10-fold of wt viruses, and has excellent selectivity against a range of human targets. Altogether lersivirine is a highly potent and selective NNRTI, with excellent efficacy against NNRTI-resistant viruses.
Lersivirine: a Non-Nucleoside Reverse Transcriptase Inhibitor with Activity against Drug-Resistant Human Immunodeficiency Virus-1.,Corbau R, Mori J, Phillips C, Fishburn L, Martin A, Mowbray C, Panton W, Smith-Burchnell C, Thornberry A, Ringrose H, Knochel T, Irving S, Westby M, Wood A, Perros M Antimicrob Agents Chemother. 2010 Jul 26. PMID:20660667[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Corbau R, Mori J, Phillips C, Fishburn L, Martin A, Mowbray C, Panton W, Smith-Burchnell C, Thornberry A, Ringrose H, Knochel T, Irving S, Westby M, Wood A, Perros M. Lersivirine: a Non-Nucleoside Reverse Transcriptase Inhibitor with Activity against Drug-Resistant Human Immunodeficiency Virus-1. Antimicrob Agents Chemother. 2010 Jul 26. PMID:20660667 doi:10.1128/AAC.01455-09
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