| Structural highlights
2uy0 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: | 1a9m, 1ajv, 1ajx, 1axa, 1bqm, 1bqn, 1d4h, 1d4i, 1d4j, 1dlo, 1dw6, 1ebk, 1ebw, 1eby, 1ebz, 1ec0, 1ec1, 1ec2, 1ec3, 1eet, 1g35, 1gnm, 1gnn, 1gno, 1hbv, 1hef, 1heg, 1hih, 1hmv, 1hni, 1hnv, 1hos, 1hps, 1hpz, 1hqe, 1hqu, 1hrh, 1hte, 1htf, 1htg, 1hvi, 1hvk, 1hvp, 1hvu, 1hys, 1ikv, 1ikw, 1ikx, 1iky, 1j5o, 1kjh, 1mer, 1mes, 1met, 1meu, 1n5y, 1n6q, 1npa, 1npv, 1npw, 1qe1, 1qmc, 1r0a, 1rdh, 1rtd, 1rvl, 1rvm, 1rvn, 1rvo, 1rvp, 1rvq, 1rvr, 1s6p, 1s6q, 1s9e, 1s9g, 1sbg, 1suq, 1sv5, 1t03, 1t05, 1t7k, 1tv6, 1tvr, 1uwb, 1w5v, 1w5w, 1w5x, 1w5y, 1yt9, 1zp8, 1zpa, 2b5j, 2b6a, 2ban, 2bb9, 2bbb, 2be2, 2hmi, 3hvt, 3tlh, 2uxz |
| Activity: | HIV-1 retropepsin, with EC number 3.4.23.16 |
| 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
A new generation of HIV-1 protease inhibitors encompassing a tertiary-alcohol-based transition-state mimic has been developed. By elongation of the core structure of recently reported inhibitors with two carbon atoms and by varying the P1' group of the compounds, efficient inhibitors were obtained with Ki down to 2.3 nM and EC50 down to 0.17 microM. Two inhibitor-enzyme X-ray structures are reported.
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.,Wu X, Ohrngren P, Ekegren JK, Unge J, Unge T, Wallberg H, Samuelsson B, Hallberg A, Larhed M J Med Chem. 2008 Feb 28;51(4):1053-7. Epub 2008 Jan 24. PMID:18215014[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Wu X, Ohrngren P, Ekegren JK, Unge J, Unge T, Wallberg H, Samuelsson B, Hallberg A, Larhed M. Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic. J Med Chem. 2008 Feb 28;51(4):1053-7. Epub 2008 Jan 24. PMID:18215014 doi:10.1021/jm070680h
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