2fde

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Image:2fde.gif

2fde, resolution 2.7Å

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Wild type HIV protease bound with GW0385

Overview

A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.

About this Structure

2FDE is a Single protein structure of sequence from Human immunodeficiency virus 1 with and as ligands. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.

Reference

Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385., Miller JF, Andrews CW, Brieger M, Furfine ES, Hale MR, Hanlon MH, Hazen RJ, Kaldor I, McLean EW, Reynolds D, Sammond DM, Spaltenstein A, Tung R, Turner EM, Xu RX, Sherrill RG, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1788-94. Epub 2006 Feb 3. PMID:16458505

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