Establishment and characterization of bortezomib-resistant U266 cell line: constitutive activation of NF-κB-mediated cell signals and/or alterations of ubiquitylation-related genes reduce bortezomib-induced apoptosis

BMB Rep. 2014 May;47(5):274-9. doi: 10.5483/bmbrep.2014.47.5.134.

Abstract

Bortezomib has been known as the most promising anti-cancer drug for multiple myeloma (MM). However, recent studies reported that not all MM patients respond to bortezomib. To overcome such a stumbling-block, studies are needed to clarify the mechanisms of bortezomib resistance. In this study, we established a bortezomib-resistant cell line (U266/velR), and explored its biological characteristics. The U266/velR showed reduced sensitivity to bortezomib, and also showed crossresistance to the chemically unrelated drug thalidomide. U266/velR cells had a higher proportion of CD138 negative subpopulation, known as stem-like feature, compared to parental U266 cells. U266/velR showed relatively less inhibitory effect of prosurvival NF-κB signaling by bortezomib. Further analysis of RNA microarray identified genes related to ubiquitination that were differentially regulated in U266/velR. Moreover, the expression level of CD52 in U266 cells was associated with bortezomib response. Our findings provide the basis for developing therapeutic strategies in bortezomib-resistant relapsed and refractory MM patients.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Boronic Acids / pharmacology*
  • Bortezomib
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm* / genetics
  • Drug Resistance, Neoplasm* / physiology
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Multiple Myeloma / drug therapy*
  • Multiple Myeloma / genetics
  • Multiple Myeloma / metabolism
  • NF-kappa B / metabolism*
  • Pyrazines / pharmacology*
  • Signal Transduction / drug effects
  • Syndecan-1 / metabolism
  • Thalidomide / pharmacology
  • Ubiquitination

Substances

  • Antineoplastic Agents
  • Boronic Acids
  • NF-kappa B
  • Pyrazines
  • SDC1 protein, human
  • Syndecan-1
  • Thalidomide
  • Bortezomib