Identification of KLK10 as a therapeutic target to reverse trastuzumab resistance in breast cancer

Oncotarget. 2016 Nov 29;7(48):79494-79502. doi: 10.18632/oncotarget.13104.

Abstract

Trastuzumab, the first antibody widely used in anti-HER2 targeted therapy, dramatically improved the overall outcome of HER2 positive breast cancer patients. However, trastuzumab resistance emerged as a major problem in its clinical application. In order to explore mechanisms underlying trastuzumab resistance, we performed RNA-Seq to analyze the gene expression variation in trastuzumab resistant breast cancer cell line. The sequencing result was then combined with the relevant data in TCGA database to conduct a co-expression analysis. We found a series of differentially expressed genes with potential contributions to trastuzumab resistance. Among them, KLK10 was verified to be a potential therapeutic target for reversing trastuzumab resistance. In summary, this study provides a new clue to screen molecular targets and predictive biomarkers for trastuzumab resistance.

Keywords: HER2; KLK10; breast cancer; trastuzumab resistance.

MeSH terms

  • Antineoplastic Agents, Immunological / pharmacology*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Computational Biology
  • Databases, Genetic
  • Dose-Response Relationship, Drug
  • Drug Discovery / methods*
  • Drug Resistance, Neoplasm / drug effects*
  • Female
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Kallikreins / genetics
  • Kallikreins / metabolism*
  • Molecular Targeted Therapy
  • RNA Interference
  • Receptor, ErbB-2 / antagonists & inhibitors*
  • Receptor, ErbB-2 / genetics
  • Receptor, ErbB-2 / metabolism
  • Signal Transduction / drug effects
  • Time Factors
  • Transfection
  • Trastuzumab / therapeutic use*

Substances

  • Antineoplastic Agents, Immunological
  • ERBB2 protein, human
  • Receptor, ErbB-2
  • KLK10 protein, human
  • Kallikreins
  • Trastuzumab