2. Academic Validation
  3. 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

  • Tumour Biol. 2016 Sep;37(9):11835-11842. doi: 10.1007/s13277-016-5036-8.
Michelle Pusey 1,  Sophie Bail 1,  Yan Xu 2,  Olesia Buiakova 2,  Mariya Nestor 3,  Jing-Jing Yang 3,  Lyndi M Rice 4
Affiliations

Affiliations

  • 1 Oncoveda, Cancer Signaling and Cell Cycle Team, Medical Diagnostic Laboratories, LLC, 1000 Waterview Drive, Room 345, Hamilton, NJ, 08691, USA.
  • 2 Invivotek, LLC, 16 Black Forest Road, Hamilton, NJ, 08691, USA.
  • 3 Pathology Department, Members of Genesis Biotechnology Group, LLC, Medical Diagnostic Laboratories LLC, 2439 Kuser Road, Hamilton, NJ, 08690, USA.
  • 4 Oncoveda, Cancer Signaling and Cell Cycle Team, Medical Diagnostic Laboratories, LLC, 1000 Waterview Drive, Room 345, Hamilton, NJ, 08691, USA. lrice@oncoveda.com.
PMID: 27048286 DOI: 10.1007/s13277-016-5036-8
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.

Keywords

ABL-127; Endometrial cancer; PME-1; PP2A.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-108317
    99.91%, PME-1抑制剂
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