TAM receptors Tyro3 and Mer as novel targets in colorectal cancer

Oncotarget. 2016 Aug 30;7(35):56355-56370. doi: 10.18632/oncotarget.10889.

Abstract

Purpose: CRC remains the third most common cancer worldwide with a high 5-year mortality rate in advanced cases. Combined with chemotherapy, targeted therapy is an additional treatment option. However as CRC still escapes targeted therapy the vigorous search for new targets is warranted to increase patients´ overall survival.

Results: In this study we describe a new role for Gas6/protein S-TAM receptor interaction in CRC. Gas6, expressed by tumor-infiltrating M2-like macrophages, enhances malignant properties of tumor cells including proliferation, invasion and colony formation. Upon chemotherapy macrophages increase Gas6 synthesis, which significantly attenuates the cytotoxic effect of 5-FU chemotherapy on tumor cells. The anti-coagulant protein S has similar effects as Gas6.In CRC patient samples Tyro3 was overexpressed within the tumor. In-vitro inhibition of Tyro3 and Mer reduces tumor cell proliferation and sensitizes tumor cells to chemotherapy. Moreover high expression of Tyro3 and Mer in tumor tissue significantly shortens CRC patients´ survival.

Experimental design: Various in vitro models were used to investigate the role of Gas6 and its TAM receptors in human CRC cells, by stimulation (rhGas6) and knockdown (siRNA) of Axl, Tyro3 and Mer. In terms of a translational research, we additionally performed an expression analysis in human CRC tissue and analyzed the medical record of these patients.

Conclusions: Tyro3 and Mer represent novel therapeutic targets in CRC and warrant further preclinical and clinical investigation in the future.

Keywords: Gas6; Mer; colorectal cancer; macrophages; tyro3.

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Animals
  • Antimetabolites, Antineoplastic / pharmacology
  • Antimetabolites, Antineoplastic / therapeutic use*
  • Axl Receptor Tyrosine Kinase
  • Blood Proteins / metabolism
  • Cell Line, Tumor
  • Cell Proliferation
  • Coculture Techniques
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / mortality
  • Colorectal Neoplasms / pathology*
  • Female
  • Fluorouracil / pharmacology
  • Fluorouracil / therapeutic use
  • Follow-Up Studies
  • Gene Expression Profiling
  • Gene Knockdown Techniques
  • Humans
  • Intercellular Signaling Peptides and Proteins / metabolism*
  • Kaplan-Meier Estimate
  • Macrophages / drug effects
  • Macrophages / pathology
  • Male
  • Mice
  • Middle Aged
  • Protein S
  • Proto-Oncogene Proteins / genetics
  • Proto-Oncogene Proteins / metabolism
  • RNA Interference
  • RNA, Small Interfering / metabolism
  • Receptor Protein-Tyrosine Kinases / genetics
  • Receptor Protein-Tyrosine Kinases / metabolism*
  • Recombinant Proteins / metabolism
  • Signal Transduction
  • c-Mer Tyrosine Kinase / genetics
  • c-Mer Tyrosine Kinase / metabolism*

Substances

  • Antimetabolites, Antineoplastic
  • Blood Proteins
  • Intercellular Signaling Peptides and Proteins
  • PROS1 protein, human
  • Protein S
  • Proto-Oncogene Proteins
  • RNA, Small Interfering
  • Recombinant Proteins
  • growth arrest-specific protein 6
  • MERTK protein, human
  • Receptor Protein-Tyrosine Kinases
  • TYRO3 protein, human
  • c-Mer Tyrosine Kinase
  • Fluorouracil
  • Axl Receptor Tyrosine Kinase