Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90)
Copyright policy )Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90)
The molecular chaperone heat shock protein 90 (Hsp90) is a current inhibition target for the treatment of diseases, including cancer. In humans, there are two major cytosolic isoforms of Hsp90 (Hsp90α and Hsp90β). Hsp90α is inducible and Hsp90β is constitutively expressed. Most Hsp90 inhibitors are pan-inhibitors that target both cytosolic isoforms of Hsp90. The development of isoform-selective inhibitors of Hsp90 may enable better clinical outcomes. Herein, by using virtual screening and binding studies, we report our work in the identification and characterisation of novel isoform-selective ligands for the middle domain of Hsp90β. Our results pave the way for further development of isoform-selective Hsp90 inhibitors.
- University of Melbourne Australia
- University of Auckland New Zealand
- Keele University United Kingdom
- School of Chemical Sciences United States
570, Binding Sites, ligand binding, Xanthones, Hsp90, 540, virtual screening, Ligands, intrinsic tryptophan fluorescence, Article, Molecular Docking Simulation, Spectrometry, Fluorescence, Protein Domains, Humans, Protein Isoforms, QD, HSP90 Heat-Shock Proteins, isoform-selective, QD415, Protein Binding
570, Binding Sites, ligand binding, Xanthones, Hsp90, 540, virtual screening, Ligands, intrinsic tryptophan fluorescence, Article, Molecular Docking Simulation, Spectrometry, Fluorescence, Protein Domains, Humans, Protein Isoforms, QD, HSP90 Heat-Shock Proteins, isoform-selective, QD415, Protein Binding
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