Modulation of human Hsp90α conformational dynamics by allosteric ligand interaction at the c-terminal domain:

Penkler, David L; Tastan Bishop, Özlem

Title: Modulation of human Hsp90α conformational dynamics by allosteric ligand interaction at the c-terminal domain:
Creator: Penkler, David L
Creator: Tastan Bishop, Özlem
Date Issued: 2018
Date: 2018
Type: text
Type: article
Identifier: http://hdl.handle.net/10962/148402
Identifier: vital:38736
Identifier: DOI: 10.1101/386755
Description: Recent years have seen heat shock protein 90 kDa (Hsp90) attract significant interest as a viable drug target, particularly for cancer. To date, designed inhibitors that target the ATPase domain demonstrate potent anti-proliferative effects, but have failed clinical trials due to high levels of associated toxicity. To circumvent this, the focus has shifted away from the ATPase domain. One option involves modulation of the protein through allosteric activation/inhibition. Here, we propose a novel approach: we use previously obtained information via residue perturbation scanning coupled with dynamic residue network analysis to identify allosteric drug targeting sites for inhibitor docking.
Format: pdf
Language: English
Relation: Scientific reports
Relation: Penkler, D.L. and Bishop, Ö.T., 2019. Modulation of human Hsp90α conformational dynamics by allosteric ligand interaction at the c-terminal domain. Scientific reports, 9(1), pp.1-17.
Relation: Scientific reports volume 9 number 1 1 17 2018 2045-2322
Rights: Publisher
Rights: Use of this resource is governed by the terms and conditions of the nature research Terms and Conditions statement (https://0-www.nature.com.wam.seals.ac.za/info/terms-and-conditions)

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RU Research Unit in Bioinformatics (RUBi)

Tastan Bishop, Ozlem (Prof)

RU Department of Biochemistry, Microbiology and Bioinformatics

SDG 03. Good Health and Well-Being

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