Structure of an inhibitor complex of the proteinase from feline immunodeficiency virus
- 1 June 1995
- journal article
- research article
- Published by Springer Nature in Nature Structural & Molecular Biology
- Vol. 2 (6) , 480-488
- https://doi.org/10.1038/nsb0695-480
Abstract
The crystal structure of a recombinant form of the proteinase encoded by the feline immunodeficiency virus (FIV PR) has been solved at 2 Å 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.Keywords
This publication has 29 references indexed in Scilit:
- Alternative Native Flap Conformation Revealed by 2·3 Å Resolution Structure of SIV ProteinaseJournal of Molecular Biology, 1994
- Three-dimensional structure of a simian immunodeficiency virus protease/inhibitor complex. Implications for the design of human immunodeficiency virus type 1 and 2 protease inhibitorsBiochemistry, 1993
- Crystal structure of human immunodeficiency virus (HIV) type 2 protease in complex with a reduced amide inhibitor and comparison with HIV-1 protease structures.Proceedings of the National Academy of Sciences, 1993
- Crystal structures of HIV-1 protease-inhibitor complexesPerspectives in Drug Discovery and Design, 1993
- Structure-Based Inhibitors of HIV-1 ProteaseAnnual Review of Biochemistry, 1993
- Origin and General Nature of RetrovirusesPublished by Springer Nature ,1992
- Structure of the aspartic protease from Rous sarcoma retrovirus refined at 2-.ANG. resolutionBiochemistry, 1990
- Structure of Complex of Synthetic HIV-1 Protease with a Substrate-Based Inhibitor at 2.3 Å ResolutionScience, 1989
- Conserved Folding in Retroviral Proteases: Crystal Structure of Synthetic HIV-1 ProteaseScience, 1989
- The Human Immunodeficiency Virus: Infectivity and Mechanisms of PathogenesisScience, 1988