1t7k

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Image:1t7k.gif

1t7k, resolution 2.10Å

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Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea

Overview

A series of novel azacyclic urea HIV protease inhibitors bearing a benzenesulfonamide group at P1' were synthesized utilizing a parallel synthesis method. Structural studies of early analogs bound in the enzyme active site were used to design more potent inhibitors. The effects of substituting the P1' benzenesulfonyl group on antiviral activity and protein binding are described.

About this Structure

1T7K is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.

Reference

Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors., Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8. PMID:15225729

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