Literature DB >> 16530412

High-throughput screening for Hsp90 ATPase inhibitors.

Christopher Avila1, M Kyle Hadden, Zeqiang Ma, Boris A Kornilayev, Qi-Zhuang Ye, Brian S J Blagg.   

Abstract

Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of approximately 10,000 compounds was performed to determine the feasibility of this assay on large scale. Results from high-throughput screening indicated that the assay was reproducible (av Z-factor = 0.80) and identified 0.57% of the compounds as Hsp90 inhibitors that exhibited IC50s less than 20 microM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

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Year:  2006        PMID： 16530412     DOI： 10.1016/j.bmcl.2006.02.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  15 in total

1.  High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding of firefly luciferase.

Authors:  Lakshmi Galam; M Kyle Hadden; Zeqiang Ma; Qi-Zhuang Ye; Bo-Geon Yun; Brian S J Blagg; Robert L Matts
Journal:  Bioorg Med Chem       Date:  2007-01-04       Impact factor: 3.641

2.  KU675, a Concomitant Heat-Shock Protein Inhibitor of Hsp90 and Hsc70 that Manifests Isoform Selectivity for Hsp90α in Prostate Cancer Cells.

Authors:  Weiya Liu; George A Vielhauer; Jeffrey M Holzbeierlein; Huiping Zhao; Suman Ghosh; Douglas Brown; Eugene Lee; Brian S J Blagg
Journal:  Mol Pharmacol       Date:  2015-05-04       Impact factor: 4.436

3.  Application of docking-based comparative intermolecular contacts analysis to validate Hsp90α docking studies and subsequent in silico screening for inhibitors.

Authors:  Mahmoud A Al-Sha'er; Mutasem O Taha
Journal:  J Mol Model       Date:  2012-06-16       Impact factor: 1.810

Review 4.  Modulation of Hsp90 function in neurodegenerative disorders: a molecular-targeted therapy against disease-causing protein.

Authors:  Masahiro Waza; Hiroaki Adachi; Masahisa Katsuno; Makoto Minamiyama; Fumiaki Tanaka; Manabu Doyu; Gen Sobue
Journal:  J Mol Med (Berl)       Date:  2006-06-02       Impact factor: 4.599

5.  The rapid and direct determination of ATPase activity by ion exchange chromatography and the application to the activity of heat shock protein-90.

Authors:  Manuela Bartolini; Irving W Wainer; Carlo Bertucci; Vincenza Andrisano
Journal:  J Pharm Biomed Anal       Date:  2012-03-21       Impact factor: 3.935

6.  Diverging Novobiocin Anti-Cancer Activity from Neuroprotective Activity through Modification of the Amide Tail.

Authors:  Suman Ghosh; Yang Liu; Gaurav Garg; Mercy Anyika; Nolan T McPherson; Jiacheng Ma; Rick T Dobrowsky; Brian S J Blagg
Journal:  ACS Med Chem Lett       Date:  2016-07-05       Impact factor: 4.345

7.  Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.

Authors:  Thota Ganesh; Pahk Thepchatri; Lian Li; Yuhong Du; Haian Fu; James P Snyder; Aiming Sun
Journal:  Bioorg Med Chem Lett       Date:  2008-08-14       Impact factor: 2.823

8.  Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.

Authors:  Thota Ganesh; Jaeki Min; Pahk Thepchatri; Yuhong Du; Lian Li; Iestyn Lewis; Larry Wilson; Haian Fu; Gabriela Chiosis; Raymond Dingledine; Dennis Liotta; James P Snyder; Aiming Sun
Journal:  Bioorg Med Chem       Date:  2008-05-27       Impact factor: 3.641

9.  Synthesis and evaluation of Hsp90 inhibitors that contain the 1,4-naphthoquinone scaffold.

Authors:  M Kyle Hadden; Stephanie A Hill; Jason Davenport; Robert L Matts; Brian S J Blagg
Journal:  Bioorg Med Chem       Date:  2008-12-03       Impact factor: 3.641

10.  KU135, a novel novobiocin-derived C-terminal inhibitor of the 90-kDa heat shock protein, exerts potent antiproliferative effects in human leukemic cells.

Authors:  Shary N Shelton; Mary E Shawgo; Shawna B Matthews; Yuanming Lu; Alison C Donnelly; Kristen Szabla; Mehmet Tanol; George A Vielhauer; Roger A Rajewski; Robert L Matts; Brian S J Blagg; John D Robertson
Journal:  Mol Pharmacol       Date:  2009-09-09       Impact factor: 4.436
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