search results

results of search on CRYSTALLOGRAPHY JOURNALS ONLINE Subscribe to an rss feed of this search

Search query: peptide inhibitors

742 articles match your search "peptide inhibitors"

Results 1 to 10, sorted by relevance:

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.

Download citation
Download citation

link to html
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.
Follow IUCr Journals
Sign up for e-alerts
Follow IUCr on Twitter
Follow us on facebook
Sign up for RSS feeds