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Inhibition of Protein Methylesterase 1 Decreased Cancerous Phenotypes in Endometrial Adenocarcinoma Cell Lines and Xenograft Tumor Models

Inhibition of Protein Methylesterase 1 Decreased Cancerous Phenotypes in Endometrial Adenocarcinoma Cell Lines and Xenograft Tumor Models

Michelle Pusey, Sophie Bail, Yan Xu, Olesia Buiakova, Mariya Nestor, Jing-Jing Yang, Lyndi M Rice

Tumour Biol. 2016 Sep;37(9):11835-11842.

PMID: 27048286

Abstract:

Protein methylesterase 1 (PME-1) promotes cancerous phenotypes through the demethylation and inactivation of protein phosphatase 2A. We previously demonstrated that PME-1 overexpression promotes Akt, ERK, and may promote Wnt signaling and increases tumor burden in a xenograft model of endometrial cancer. Here, we show that covalent PME-1 inhibitors decrease cell proliferation and invasive growth in vitro but have no effect in vivo at the concentrations tested; however, depletion of PME-1 with shRNA in an endometrial cancer xenograft model significantly reduced tumor growth. Thus, discovery of more potent PME-1 inhibitors may be beneficial for the treatment of endometrial cancer.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1073529415	ABL127		1073529-41-5	Price

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