Novel Hsp90 inhibitor FW-04-806 displays potent antitumor effects in HER2-positive breast cancer cells as a single agent or in combination with lapatinib

Highlights • FW-04-806 was identified to be a potent Hsp90 inhibitor. • The combination of FW-04-806 and the lapatinib displayed synergistic effects. • FW-04-806 was able to abrogate the amplification of HER3 mediated by lapatinib. • FW-04-806 could be an integral part of treatment strategies aimed...

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Bibliographic Details
Published in:Cancer letters 2015-01, Vol.356 (2), p.862-871
Main Authors: Huang, Wei, Wu, Qun-dan, Zhang, Min, Kong, Ying-li, Cao, Pin-rong, Zheng, Wei, Xu, Jian-hua, Ye, Min
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - pharmacology
Antineoplastic Combined Chemotherapy Protocols
Apoptosis
Apoptosis - drug effects
Blotting, Western
Breast cancer
Breast Neoplasms - drug therapy
Breast Neoplasms - metabolism
Breast Neoplasms - pathology
Cancer therapies
Cell cycle
Cell division
Cell growth
Cell Proliferation - drug effects
Drug Resistance, Neoplasm - drug effects
Drug Synergism
Epidermal growth factor
Female
FW-04-806
Gene Expression Regulation, Neoplastic - drug effects
Hematology, Oncology and Palliative Medicine
HER2
HER2-positive breast cancer
HER3
HSP90 Heat-Shock Proteins - antagonists & inhibitors
HSP90 Heat-Shock Proteins - genetics
HSP90 Heat-Shock Proteins - metabolism
Humans
Immunoenzyme Techniques
Kinases
Mice
Mice, Inbred BALB C
Mice, Nude
Oxazoles - pharmacology
Phosphatidylinositol 3-Kinases - genetics
Phosphatidylinositol 3-Kinases - metabolism
Phosphorylation - drug effects
Plasmids
Proteins
Proto-Oncogene Proteins c-akt - genetics
Proto-Oncogene Proteins c-akt - metabolism
Quinazolines - pharmacology
Real-Time Polymerase Chain Reaction
Receptor, ErbB-2 - genetics
Receptor, ErbB-2 - metabolism
Reverse Transcriptase Polymerase Chain Reaction
RNA, Messenger - genetics
Tumor Cells, Cultured
Xenograft Model Antitumor Assays
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Summary:Highlights • FW-04-806 was identified to be a potent Hsp90 inhibitor. • The combination of FW-04-806 and the lapatinib displayed synergistic effects. • FW-04-806 was able to abrogate the amplification of HER3 mediated by lapatinib. • FW-04-806 could be an integral part of treatment strategies aimed at HER2/3 blockade.
ISSN:0304-3835
1872-7980
DOI:10.1016/j.canlet.2014.10.040