4FZG: 20S Yeast Proteasome in Complex With Glidobactin

Citation:
Abstract
Natural products represent valuable lead structures for drug discovery. However, for most bioactive compounds no cellular target is yet identified and many substances predicted from genome analysis are inaccessible due to their life stage-dependent biosynthesis, which is not reflected in common isolation procedures. In response to these issues, an NMR-based and target-directed protease assay for inhibitor detection of the proteasome was developed. The methodology is suitable for one-shot identification of inhibitors in conglomerates and crude culture broths. The technique was applied for analysis of the different life stages of the bacterium Photorhabdus luminescens, which resulted in the isolation and characterization of cepafungin I (CepI), the strongest proteasome inhibitor described to date. Its biosynthesis is strictly regulated and solely induced by the specific environmental conditions determined by our methodology. The transferability of the developed technique to other drug targets may disclose an abundance of novel compounds applicable for drug development.
PDB ID: 4FZGDownload
MMDB ID: 104256
PDB Deposition Date: 2012/7/6
Updated in MMDB: 2012/12 
Experimental Method:
x-ray diffraction
Resolution: 3  Å
Source Organism:
Similar Structures:
Biological Unit for 4FZG: 32-meric; determined by author
Molecular Components in 4FZG
Label Count Molecule
Proteins (28 molecules)
2
Proteasome Component Y7
Molecule annotation
2
Proteasome Component Y13
Molecule annotation
2
Proteasome Component Pre6
Molecule annotation
2
Proteasome Component Pup2
Molecule annotation
2
Proteasome Component Pre5
Molecule annotation
2
Proteasome Component C1
Molecule annotation
2
Proteasome Component C7-alpha
Molecule annotation
2
Proteasome Component Pup1
Molecule annotation
2
Proteasome Component Pup3
Molecule annotation
2
Proteasome Component C11
Molecule annotation
2
Proteasome Component Pre2
Molecule annotation
2
Proteasome Component C5
Molecule annotation
2
Proteasome Component Pre4
Molecule annotation
2
Proteasome Component Pre3
Molecule annotation
Nucleotide(1 molecule)
4
Glidobactin
Molecule annotation
* Click molecule labels to explore molecular sequence information.

Citing MMDB
.