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Inhibitors of HIV-1 protease: a major success of structure-assisted drug design.
Retroviral protease from the human immunodeficiency virus type 1 (HIV-1) was identified over a decade ago as a potential target for structure-based drug design and four drugs are already approved, and others are undergoing clinical trials.
Catalytic triads and their relatives.
Review of these enzymes shows that the acid-base-ser/thr pattern of catalytic residues is generally conserved, although the individual acids and bases can vary.
Structural Basis for the Substrate Specificity of Tobacco Etch Virus Protease*
Analysis of the protein-ligand interactions helps to delineate the structural determinants of substrate specificity and provides guidance for reengineering the enzyme to further improve its utility for biotechnological applications.
Structure of bovine pancreatic trypsin inhibitor
The structure of form II crystals of bovine pancreatic trypsin inhibitor has been investigated by joint refinement of X-ray and neutron data and eleven amide hydrogens were found to be protected from exchange after three months of soaking the crystals in deuterated mother liquor at pH 8·2.
Protein crystallography for non‐crystallographers, or how to get the best (but not more) from published macromolecular structures
This review attempts to provide a brief outline of technical aspects of crystallography and to explain the meaning of some parameters that should be evaluated by users of macromolecular structures in order to interpret, but not over‐interpret, the information present in the coordinate files and in their description.
Filamentous phage infection: crystal structure of g3p in complex with its coreceptor, the C-terminal domain of TolA.
The structure of the fusion protein presented here clearly shows that, during the infection process, the g3p N2 domain is displaced by the TolA D3 domain, which is not similar to any previously known protein motifs.
Conserved folding in retroviral proteases: crystal structure of a synthetic HIV-1 protease.
The crystal structure of chemically synthesized HIV-1 protease has been determined with the use of a model based on the Rous sarcoma virus protease structure, and the observed arrangement of the dimer interface suggests possible designs for dimerization inhibitors.
High-resolution structure of the catalytic domain of avian sarcoma virus integrase.
The crystal structure of the isolated catalytic domain of avian sarcoma virus (ASV) IN is reported, solved using multiwavelength anomalous diffraction data for a selenomethionine derivative and refined at 1.7 A resolution.
Crystal structure of rabbit muscle creatine kinase 1
The crystal structure of rabbit muscle creatine kinase, solved at 2.35 Å resolution by X‐ray diffraction methods, clearly identified the active site with bound sulfates surrounded by a constellation
Crystal structure of plant aspartic proteinase prophytepsin: inactivation and vacuolar targeting
Structural analysis of prophytepsin led to the identification of a putative membrane receptor‐binding site involved in Golgi‐mediated transport to vacuoles, suggesting that all saposins and saposin‐like domains share a common topology.