High-throughput screening for Hsp90 ATPase inhibitors

Christopher Avila, M. Kyle Hadden, Zeqiang Ma, Boris A. Kornilayev, Qizhuang Ye, Brian S J Blagg

Research output: Contribution to journalArticle

32 Citations (Scopus)

Abstract

Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of ∼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 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

Original languageEnglish (US)
Pages (from-to)3005-3008
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number11
DOIs
StatePublished - Jun 1 2006
Externally publishedYes

Fingerprint

High-Throughput Screening Assays
Adenosine Triphosphatases
Assays
Screening
Throughput
Inhibitory Concentration 50
Yeasts
Scaffolds
Yeast

Keywords

  • High-throughput screening
  • Hsp90
  • Inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Avila, C., Hadden, M. K., Ma, Z., Kornilayev, B. A., Ye, Q., & Blagg, B. S. J. (2006). High-throughput screening for Hsp90 ATPase inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(11), 3005-3008. https://doi.org/10.1016/j.bmcl.2006.02.063

High-throughput screening for Hsp90 ATPase inhibitors. / Avila, Christopher; Hadden, M. Kyle; Ma, Zeqiang; Kornilayev, Boris A.; Ye, Qizhuang; Blagg, Brian S J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 11, 01.06.2006, p. 3005-3008.

Research output: Contribution to journalArticle

Avila, C, Hadden, MK, Ma, Z, Kornilayev, BA, Ye, Q & Blagg, BSJ 2006, 'High-throughput screening for Hsp90 ATPase inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 11, pp. 3005-3008. https://doi.org/10.1016/j.bmcl.2006.02.063
Avila, Christopher ; Hadden, M. Kyle ; Ma, Zeqiang ; Kornilayev, Boris A. ; Ye, Qizhuang ; Blagg, Brian S J. / High-throughput screening for Hsp90 ATPase inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 11. pp. 3005-3008.
@article{87ed92bb1ceb462ba0966c5dd1ba3621,
title = "High-throughput screening for Hsp90 ATPase inhibitors",
abstract = "Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of ∼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 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.",
keywords = "High-throughput screening, Hsp90, Inhibitors",
author = "Christopher Avila and Hadden, {M. Kyle} and Zeqiang Ma and Kornilayev, {Boris A.} and Qizhuang Ye and Blagg, {Brian S J}",
year = "2006",
month = "6",
day = "1",
doi = "10.1016/j.bmcl.2006.02.063",
language = "English (US)",
volume = "16",
pages = "3005--3008",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "11",

}

TY - JOUR

T1 - High-throughput screening for Hsp90 ATPase inhibitors

AU - Avila, Christopher

AU - Hadden, M. Kyle

AU - Ma, Zeqiang

AU - Kornilayev, Boris A.

AU - Ye, Qizhuang

AU - Blagg, Brian S J

PY - 2006/6/1

Y1 - 2006/6/1

N2 - Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of ∼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 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

AB - Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of ∼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 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

KW - High-throughput screening

KW - Hsp90

KW - Inhibitors

UR - http://www.scopus.com/inward/record.url?scp=33646036989&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33646036989&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.02.063

DO - 10.1016/j.bmcl.2006.02.063

M3 - Article

C2 - 16530412

AN - SCOPUS:33646036989

VL - 16

SP - 3005

EP - 3008

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 11

ER -