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Affinity Group
1.A. Wlodawer, A. Gustchina, L. Reshetnikova, J. Lubkowski, A. Zdanov, K.Y. Hui, E.L. Angleton, W.G. Farmerie, M.M.
Goodenow, D. Bhatt, L. Zhang and B.M. Dunn (1995) "Structure of an Inhibitor Complex of the Protease from Feline
Immunodeficiency Virus", Nature Structural Biology 2, 480-488
The crystal structure of a recombinant form of the proteinase encoded by the feline immunodeficiency virus (FIV PR) has been
solved at 2 A resolution and refined to an R-factor of 0.148. The refined structure includes a peptidomimetic, statine-based
inhibitor, LP-149, which is an even more potent inhibitor of HIV PR. Kinetic parameters were obtained for the cleavage of five
substrates by FIV PR, and inhibition constants were measured for four inhibitors. The structure of FIV PR resembles other
related retroviral enzymes although few inhibitors of HIV PR are capable of inhibiting FIV PR. The structure of FIV PR will
enhance our knowledge of this class of enzymes, and will direct testing of new proteinase inhibitors in a feline animal model.
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