4NH9: Correlation Between Chemotype-dependent Binding Conformations Of Hsp90 Alpha/beta And Isoform Selectivity

Citation:
Abstract
HSP90 continues to be a target of interest for neurodegeneration indications. Selective knockdown of the HSP90 cytosolic isoforms alpha and beta is sufficient to reduce mutant huntingtin protein levels in vitro. Chemotype-dependent binding conformations of HSP90alpha/beta appear to strongly influence isoform selectivity. The rational design of HSP90alpha/beta inhibitors selective versus the mitochondrial (TRAP1) and endoplasmic reticulum (GRP94) isoforms offers a potential mitigating strategy for mechanism-based toxicities. Better tolerated HSP90 inhibitors would be attractive for targeting chronic neurodegenerative diseases such as Huntington's disease.
PDB ID: 4NH9Download
MMDB ID: 116880
PDB Deposition Date: 2013/11/4
Updated in MMDB: 2014/01
Experimental Method:
x-ray diffraction
Resolution: 2.77  Å
Source Organism:
Similar Structures:
Biological Unit for 4NH9: monomeric; determined by author and by software (PISA)
Molecular Components in 4NH9
Label Count Molecule
Protein (1 molecule)
1
Endoplasmin(Gene symbol: HSP90B1)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

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