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Screening Technique for Heat Shock Protein 90 Inhibitors from Natural Products

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Book cover Heat Shock Protein 90 in Human Diseases and Disorders

Part of the book series: Heat Shock Proteins ((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.

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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

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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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Authors and Affiliations

  1. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China

    Yue Hu, Xiao J. Zhang, Xiao T. Yang, Ying Y. Tang, Lin Y. Hu & Dong Zhu

  2. Jiangsu Key Laboratory for Functional Substance of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China

    Dong Zhu

  3. State Key Laboratory Cultivation Base for TCM Quality and Efficacy, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China

    Dong Zhu

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  1. Yue Hu
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Correspondence to Dong Zhu .

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  1. Department of Medicine and Director, Precision Therapeutics Proteogenomics Diagnostic Center, Eleanor N. Dana Cancer Center, University of Toledo, College of Medicine and Life Sciences, Toledo, OH, USA

    Alexzander A. A. Asea

  2. Department of Experimental Radiation Oncology, MD Anderson Cancer Center, Houston, TX, USA

    Punit Kaur

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Hu, Y., Zhang, X.J., Yang, X.T., Tang, Y.Y., Hu, L.Y., Zhu, D. (2019). Screening Technique for Heat Shock Protein 90 Inhibitors from Natural Products. In: Asea, A., Kaur, P. (eds) Heat Shock Protein 90 in Human Diseases and Disorders. Heat Shock Proteins, vol 19. Springer, Cham. https://doi.org/10.1007/978-3-030-23158-3_19

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