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Screening Technique for Heat Shock Protein 90 Inhibitors from Natural Products

  • Yue Hu
  • Xiao J. Zhang
  • Xiao T. Yang
  • Ying Y. Tang
  • Lin Y. Hu
  • Dong ZhuEmail author
Chapter
Part of the Heat Shock Proteins book series (HESP, volume 19)

Abstract

Heat shock protein 90 (Hsp90) has emerged as an important target in cancer therapy, in which case screening inhibitors targeted Hsp90 attracted special attention on anti-cancer research. Recent progress in the development of screening technique for Hsp90 inhibitors has taken place. Particular emphasis is focused on ligand fishing screening assay based on protein affinity such as fluorescent ligand fishing that serve as a screening platform show case. This context will focus on strategies to screen and validate potential Hsp90 inhibitors from natural products and the development of screening techniques that are currently applied for the discovery of bioactive compounds from complex mixtures.

Keywords

High-throughput screening Hsp90 Hsp90 inhibitors Ligand fishing Virtual screening 

Abbreviations

AFI-MS

Automated flow injection ESI-MS

Aha1

Activator of Hsp90 ATPase homologue 1

Cdc37

Cell division cycle 37 homologue

CDD

C-terminal dimerisation domain

CE

Capillary electrophoresis

CEfrag

Fragment screening technology based on capillary electrophoresis

CTD

Carboxy-terminal domain

Cy3B-GM

Cy3B-labeled geldanamycin

EGCG

Epigallocatechin gallate

EI-MS

Electrospray ionization mass spectrometry

FBDD

Fragment-based drug discovery

FP

Fluorescence polarization

GA

Geldanamycin

Grp94, HSPC4

glucose-regulated protein 94

Hop

Hsc70/Hsp90-organizing protein

Hsf1

Heat shock factor 1

Hsp90

Heat shock protein 90

HSPC1

Hsp90AA1

HSPC2

Hsp90α

HSPC3

Hsp90β

HTS

High-throughput screening

MD

Middle domain

MEEVD

Met-Glu-Glu-Val-Asp

mP

Millipolarization

NMR

Nuclear magnetic resonance

NTD

Amino-terminal domain

p23

Prostaglandin E synthase 3

PTMs

Post-translational modifications

QDs

Quantum dots

QSAR

Quantitative structure-activity relationship

ROCS

Rapid overlay of chemical structures;

S. elongates

Synechococcus elongates

SCLC

Small-cell lung carcinoma

SPR

Surface plasmon resonance

TPR

Tetratricopeptide repeat

Trap-1, HSPC5

Tumor necrosis factor receptor-associated protein 1

Notes

Acknowledgements

This work was supported by the Project of National Natural Science Foundation of China (81573388). This work was also sponsored by ‘Qing Lan Project of Jiangsu province’ and ‘Six talent peaks project of Jiangsu Province (YY-032)’. We also greatly appreciate the sponsorship of ‘A Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions’ (PAPD).

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Copyright information

© Springer Nature Switzerland AG 2019

Authors and Affiliations

  • Yue Hu
    • 1
  • Xiao J. Zhang
    • 1
  • Xiao T. Yang
    • 1
  • Ying Y. Tang
    • 1
  • Lin Y. Hu
    • 1
  • Dong Zhu
    • 1
    • 2
    • 3
    Email author
  1. 1.School of PharmacyNanjing University of Chinese MedicineNanjingPeople’s Republic of China
  2. 2.Jiangsu Key Laboratory for Functional Substance of Chinese MedicineNanjingPeople’s Republic of China
  3. 3.State Key Laboratory Cultivation Base for TCM Quality and EfficacyNanjing University of Chinese MedicineNanjingPeople’s Republic of China

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