HIV Protease with oximinoarylsulfonamide boundHIV Protease with oximinoarylsulfonamide bound

Structural highlights

1yt9 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:
Gene:POL (Human immunodeficiency virus 1)
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 need for a potent HIV protease inhibitor (PI) to combat emerging PI-resistant viruses is anticipated. Analogs formulated from the combination of structural fragments of Ritonavir, Lopinavir, and Amprenavir were synthesized. Analogs containing the oxime pharmacophore were found to have improved activities against both wild type and resistant (A17) viruses. The synthesis and structure-activity relationships (SAR) based upon the in vitro IC50 of this series of compounds are reported.

Oximinoarylsulfonamides as potent HIV protease inhibitors.,Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8. PMID:15837308[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

See Also

References

  1. Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ. Oximinoarylsulfonamides as potent HIV protease inhibitors. Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8. PMID:15837308 doi:10.1016/j.bmcl.2005.03.008

1yt9, resolution 3.00Å

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