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Search query: peptide inhibitors
742 articles match your search "peptide inhibitors"Results 1 to 10, sorted by relevance:
research papers
Crystal structures of peptide deformylase from S. aureus in complex with novel inhibitors are presented together with their functional analysis. A detailed comparative analysis of these structures as well as the activities of the inhibitors allowed the elucidation of distinctive structural changes which depend upon the class of inhibitor.
research papers
The structure of PSK, a novel antimicrobial peptide identified in Chrysomya megacephala larvae, was determined by X-ray crystallography and small-angle X-ray scattering, which revealed a distinct fold compared with published homologous peptides.
BIOLOGY | MEDICINE
Open access
Utilizing a peptide-anchoring strategy, transient signal-peptide complexes of a Gram-positive bacterial signal peptidase were trapped, revealing the atomic details of their interaction.
research communications
Two high-resolution co-crystal structures of the mitotic protein kinase haspin with previously reported conjugates consisting of an ATP analogue and a histone H3(1–7) peptide analogue confirm the bisubstrate character of the compounds and provide directions for the future development of more specific haspin inhibitors.
research papers
A series of structures show the development of novel inhibitors of carboxypeptidase B. These inhibitors were designed to mimic peptide-based inhibitors of the protein.
research papers
Botulinum neurotoxins have been declared as a Category A agent by the Centers of Disease Control and Prevention owing to their extremely poisonous nature and are potential bioweapon and bioterrorism agents. Towards the discovery of antidotes, structures of inhibitory peptide-enzyme complexes were determined, the structure-activity relationship was determined and a pharmacophore was developed.
crystallization communications
Human α-thrombin was crystallized in complex with specific peptide inhibitors of general sequence D-Phe-Pro-D-Arg-P1′-CONH2. The crystals belonged to the orthorhombic space group P212121 and diffracted to beyond 1.3 Å resolution.
BIOLOGY | MEDICINE
Open access
Crystal structures of N-myristoyltransferase with four distinct Leishmania-selective small-molecule inhibitors identify key binding-site residues and suggest strategies to design compounds with increased affinity.
crystallization papers
Diffraction-quality Se-met crystals of S. aureus PDF were prepared that belong to space group C2221 with unit-ell parameters of a = 94.1 b = 121.9 c = 47.6 Å. Crystals were also prepared with three PDF inhibitors: thiorphan, actinonin and PNU-172550.
research communications
The benzamidine-derived ligand GSK144 inhibits the target enzyme kallikrein 5 (KLK5) with a pIC50 of 7.1. X-ray crystallography of KLK5 proved challenging, with the only structure solved being that with GSK144. To enable structure-guided design in support of medicinal chemistry, a KLK6-derived crystal system was developed. Here, a biochemical pharmacological assessment of the KLK6 surrogate enzymes compared with KLK5 is described and details of the X-ray structures obtained with GSK144 are discussed.