Unknown

Dataset Information

0

FM807, a curcumin analogue, shows potent antitumor effects in nasopharyngeal carcinoma cells by heat shock protein 90 inhibition.


ABSTRACT: Nasopharyngeal carcinoma (NPC) is an epithelial malignancy usually associated with overexpression of both epidermal growth factor receptor (EGFR) and ?-catenin. FM807 is a novel curcumin analogue with antitumor activity against both poorly and well-differentiated NPC cell lines as well as good selectivity for tumor cells. FM807 actions were shown to include inhibition of cell growth, induction of necrotic/late apoptotic cell death, and G1 arrest in NPC cells. Crucially, it exhibited potent antitumor effects both in vitro and in vivo. Binding of FM807 to the N-terminus of Hsp90 disrupted Hsp90/client complexes, resulting in degradation of the Hsp90 client protein EGFR and inhibition of the downstream Raf/MEK/ERK and PI3K/AKT pathway. FM807 also depleted levels of the intranuclear transcription factors ?-catenin, Cyclin D1 and c-Myc levels by inhibiting Hsp90 chaperoned nuclear transport. In conjunction with its low toxicity in NPC xenograft mice, these results provide a sound preclinical basis for further development of FM807 as a novel therapeutic agent in the treatment of NPC.

SUBMITTER: Ye M 

PROVIDER: S-EPMC5362491 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

altmetric image

Publications

FM807, a curcumin analogue, shows potent antitumor effects in nasopharyngeal carcinoma cells by heat shock protein 90 inhibition.

Ye Min M   Huang Wei W   Wu Wen-Wei WW   Liu Yang Y   Ye Sheng-Nan SN   Xu Jian-Hua JH  

Oncotarget 20170201 9


Nasopharyngeal carcinoma (NPC) is an epithelial malignancy usually associated with overexpression of both epidermal growth factor receptor (EGFR) and β-catenin. FM807 is a novel curcumin analogue with antitumor activity against both poorly and well-differentiated NPC cell lines as well as good selectivity for tumor cells. FM807 actions were shown to include inhibition of cell growth, induction of necrotic/late apoptotic cell death, and G1 arrest in NPC cells. Crucially, it exhibited potent antit  ...[more]

Similar Datasets

| S-EPMC4641597 | biostudies-literature
| S-EPMC3706359 | biostudies-literature
| S-EPMC1895907 | biostudies-literature
| S-EPMC7058811 | biostudies-literature
| S-EPMC3384095 | biostudies-literature
| S-EPMC5045423 | biostudies-literature
| S-EPMC8588116 | biostudies-literature
| S-EPMC5863695 | biostudies-literature
| S-EPMC3699005 | biostudies-literature
| S-EPMC4813586 | biostudies-literature