MICROTUBE BATCH PROTEIN CRYSTALLIZATION - APPLICATIONS TO HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-2 (HIV-2) PROTEASE AND HUMAN RENIN

For therapeutically relevant targets, the evaluation of enzymes in com plex with their inhibitors by cocrystallization and high resolution st ructural analysis has become a vital component of structure-driven dru g design and development. Two approaches, hanging drop vapor diffusion and a novel microtube batch method, were utilized in parallel to grow crystals of recombinant HIV-2 protease and recombinant human renin in complex with inhibitors. In the case of HIV-2 protease in complex wit h a reduced amide inhibitor, crystallization was achieved only by the microbatch method. In the case of human renin, the addition of precipi tant was required for crystal growth. The microbatch method described here is a useful supplementary or alternative approach for screening p arameters and generating crystals suitable for high resolution structu ral analysis. (C) 1994 Wiley-Liss, Inc.