X-ray structures of five renin inhibitors bound to saccharopepsin: Exploration of active-site specificity

Journal of Molecular Biology

Volumn 303, Issue 5, 2000, Pages 745-760

  Cronin, Nora B ^a   Badasso, Mohammed O ^b   Tickle, Ian J ^a   Dreyer, Thomas ^c   Hoover, Dennis J ^d   Rosati, Robert L ^d   Humblet, Christine C ^e   Lunney, Elizabeth A ^e   Cooper, Jonathan B ^f  

^a UNIVERSITY OF LONDON   (United Kingdom)

^b UNIVERSITY OF MINNESOTA   (United States)

^c CARLSBERG LABORATORY   (Denmark)

^d PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^e PFIZER INC   (United States)

^f UNIVERSITY OF SOUTHAMPTON   (United Kingdom)

Author keywords

Aspartic proteinases; Renin inhibitors; Saccharopepsin

Indexed keywords

ASPARTIC PROTEINASE; BENZIMIDAZOLE DERIVATIVE; CYCLOPEPTIDE; RENIN INHIBITOR; SACCHAROPEPSIN; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING SITE; ENZYME ACTIVATION; ENZYME ACTIVE SITE; ENZYME KINETICS; HUMAN; HYDROGEN BOND; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN INTERACTION; PROTEIN STRUCTURE; SEQUENCE HOMOLOGY; STRUCTURE ANALYSIS; X RAY CRYSTALLOGRAPHY;

EID: 0034634367     PISSN: 00222836     EISSN: None     Source Type: Journal    
DOI: 10.1006/jmbi.2000.4181     Document Type: Article

References (44)

1. A new least-squares refinement technique based on the fast Fourier transform algorithm
2. Three-dimensional structure at 2.4 Å resolution of glycosylated saccharopepsin from the lysosome-like vacuole of Saccharomyces cerevisiae
3. PEP4 gene of Saccharomyces cerevisiae encodes proteinase A, vacuolar enzyme required for processing of vacuolar precursors
4. Crystallization and preliminary crystallographic characterization of aspartic proteinase-A from baker's yeast and its complexes with inhibitors
5. A structural comparison of 21 inhibitor complexes of the aspartic proteinase from Endothia parasitica
6. Crystal structures of native and inhibited forms of human cathepsin D: Implications for lysosomal targeting and drug design
7. US patent 4729985
8. The structure and function of the aspartic proteinases
9. Design and synthesis of potent, selective and orally active fluorine-containing renin inhibitors
10. Substrate specificity of proteinase yscA from Saccharomyces cerevisiae
11. Yeast proteinase in beer
12. Primary structure of the aspartic saccharopepsin from Saccharomyces cerevisiae
13. A systematic series of synthetic chromophoric substrates for aspartic proteinases
14. Accurate bond and angle parameters for X-ray protein structure refinement
15. An extensively modified version of MOLSCRIPT that includes greatly enhanced coloring capabilities
16. Restrained structure-factor least-squares refinement of protein structures using a vector processing computer
17. Mutants defective in processing of an enzyme located in the lysosome-like vacuole of Saccharomyces cerevisiae
18. Discovery of inhibitors of human renin with high oral bioavailability
19. PEP4 gene function is required for expression of several vacuolar hydrolases in Saccharomyces cerevisiae
20. A graphics model building and refinement system for macromolecules
21. Improved methods for building protein models in electron density maps and the location of errors in these models
22. Program DYNAFIT for the analysis of enzyme kinetic data: Application to HIV proteinase
23. Auto-indexing of rotation diffraction images and parameter refinement
24. The aspartic proteinase from S. cerevisiae folds its own inhibitor into a helix
25. Analyses of ligand binding in 5 endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors
26. Two crystal structures for cathepsin D: The lysosomal targeting signal and active site
27. Purification and properties of proteinase A from yeast
28. GRASP: A graphical representation and analysis of surface properties
29. A novel human renin inhibitor with a clinically applicable bioavailability, FK906
30. 2' variation
31. Improved Fourier coefficients for maps using phases from maps using phases from partial structures with errors
32. Design, synthesis and solution structure of a renin inhibitor
33. Studies directed toward the design of orally active renin inhibitors
34. Calculation of molecular volumes and areas for structures of known geometry
35. The definition of topological equivalence in homologous and analogous structures: A procedure involving comparison of local properties and structural relationships through dynamic programming and simulated annealing
36. Domain flexibility in aspartic proteinases
37. Exploration of sub-site binding specificity of human cathepsin D through kinetics and rule-based molecular modelling
38. On the size of the active site in proteases
39. Binding of a reduced peptide-inhibitor to the aspartic proteinase from Rhizopus chinensis: Implications for a mechanism of action
40. Vacuoles: The sole compartment of digestive enzymes in yeast (Saccharomyces cerevisiae)?
41. The PEP4 gene encodes an aspartyl protease implicated in the post-translational regulation of Saccharomyces cerevisiae vacuolar hydrolases
42. Phenotypic analysis of proteinase A mutants
43. Genetic properties of mutation at the PEP4 locus in Saccharomyces cerevisiae