3OWD: Crystal Structure Of Hsp90 With N-Aryl-Benzimidazolone Ii

Citation:
Abstract
We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors (9) targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation.
PDB ID: 3OWDDownload
MMDB ID: 93670
PDB Deposition Date: 2010/9/17
Updated in MMDB: 2011/09
Experimental Method:
x-ray diffraction
Resolution: 1.63  Å
Source Organism:
Similar Structures:
Biological Unit for 3OWD: monomeric; determined by author
Molecular Components in 3OWD
Label Count Molecule
Protein (1 molecule)
1
Heat Shock Protein HSP 90-alpha(Gene symbol: HSP90AA1)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

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