1yt9

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Image:1yt9.jpg

1yt9, resolution 3.00Å

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HIV Protease with oximinoarylsulfonamide bound

Overview

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.

About this Structure

1YT9 is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Full crystallographic information is available from OCA.

Reference

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

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