Mak, OW, Chand, R, Reynisson, J and Leung, IKH (2019) Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90). International Journal of Molecular Sciences, 20 (21). ISSN 1422-0067

[thumbnail of ijms-20-05333.pdf]
ijms-20-05333.pdf - Published Version
Available under License Creative Commons Attribution.

Download (1MB) | Preview


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.

Item Type: Article
Additional Information: This is the final published version of the article (version of record). It first appeared online via MDPI at - please refer to any applicable terms of use of the publisher.
Uncontrolled Keywords: Hsp90, intrinsic tryptophan fluorescence, isoform-selective, ligand binding, virtual screening
Subjects: Q Science > QD Chemistry
Q Science > QD Chemistry > QD415 Biochemistry
Divisions: Faculty of Medicine and Health Sciences > School of Pharmacy and Bioengineering
Related URLs:
Depositing User: Symplectic
Date Deposited: 18 Dec 2019 11:44
Last Modified: 18 Dec 2019 11:48

Actions (login required)

View Item
View Item