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Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90)

Reynisson

Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90) Thumbnail


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Abstract

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 (Hsp90a and Hsp90ß). Hsp90a is inducible and Hsp90ß 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 Hsp90ß. Our results pave the way for further development of isoform-selective Hsp90 inhibitors.

Acceptance Date Oct 23, 2019
Publication Date Oct 26, 2019
Publicly Available Date Mar 29, 2024
Journal International Journal of Molecular Sciences
Print ISSN 1661-6596
Publisher MDPI
DOI https://doi.org/10.3390/ijms20215333
Keywords Hsp90, intrinsic tryptophan fluorescence, isoform-selective, ligand binding, virtual screening
Publisher URL http://doi.org/10.3390/ijms20215333

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