Targeting of multidrug-resistant human ovarian carcinoma cells with anti-P-glycoprotein antibody conjugates

Macromol Biosci. 2012 Apr;12(4):502-14. doi: 10.1002/mabi.201100350. Epub 2012 Jan 25.

Abstract

A monoclonal antibody (mAb) to P-glycoprotein (Pgp), UIC2, is used as a targeting moiety for N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer/drug [(meso chlorin e(6) mono(N-2-aminoethylamide) (Mce(6)) or doxorubicin (DOX)] conjugates to investigate their cytotoxicity towards the Pgp-expressing human ovarian carcinoma cell line A2780/AD. The binding, internalization, and subcellular trafficking of a fluorescein labeled UIC2 targeted HPMA copolymer are studied and show localization to the plasma membrane with limited internalization. The specificity of the UIC2-targeted HPMA copolymer/drug conjugates are confirmed using the sensitive cell line A2780 that does not express Pgp.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Acrylic Resins / chemistry*
  • Acrylic Resins / metabolism
  • Acrylic Resins / pharmacology
  • Antibodies, Monoclonal / chemistry*
  • Antibodies, Monoclonal / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Carcinoma / drug therapy
  • Carcinoma / pathology
  • Cell Line, Tumor / drug effects
  • Cell Membrane / drug effects*
  • Cell Membrane / metabolism
  • Cell Survival / drug effects
  • Doxorubicin / chemistry*
  • Doxorubicin / pharmacology
  • Drug Carriers
  • Drug Resistance, Neoplasm
  • Endocytosis / drug effects
  • Female
  • Fluorescein
  • Humans
  • Immunoconjugates / chemistry*
  • Immunoconjugates / pharmacology
  • Ovarian Neoplasms / drug therapy
  • Ovarian Neoplasms / pathology

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Acrylic Resins
  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Drug Carriers
  • Immunoconjugates
  • Doxorubicin
  • Fluorescein