A wortmannin-cetuximab as a double drug Academic Article uri icon

Overview

MeSH Major

  • Androstadienes
  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Drug Design

abstract

  • Double drugs are obtained when two pharmacologically active entities are covalently joined to improve potency. We conjugated the viridin Wm with a self-activating linkage to cetuximab and demonstrated the retention of immunoreactivity by the conjugate. Though cetuximab lacked a growth inhibitory activity against A549 cells, the Wm-cetuximab conjugate had an antiproliferative IC(50) of 155 nM in vitro. The chemistry of attaching a self-releasing Wm to clinically approved antibodies is general and, in selected instances, may yield antibody-based double drugs with improved efficacy.

publication date

  • November 18, 2009

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3386608

Digital Object Identifier (DOI)

  • 10.1021/bc900176a

PubMed ID

  • 19883074

Additional Document Info

start page

  • 2185

end page

  • 9

volume

  • 20

number

  • 11