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Enabling ScFvs as multi-drug carriers: A dendritic approach

Academic Article
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Overview

authors

  • Sun, C. Z.
  • Wirsching, P.
  • Janda, Kim

publication date

  • April 2003

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • To enable scFvs as multi-drug carriers, we designed and synthesized dendritic linker molecules bearing up to nine chlorambucil residues at the branch ends. A maleimide group was used at the focal point of the dendron for easy linkage to the scFv. Originally designed molecules showed poor water solubility. To address this problem, a lysine residue with an unprotected carboxylic acid group was inserted into the dendron branches. The new molecules showed excellent water solubility and are now suitable for conjugation. Such dendritic molecules will allow studies to understand the relationship between the drug/antibody ratio and the potency of the immunoconjugates. The dendritic approach could also be applied to drugs other than chlorambucil and carriers other than scFvs to greatly increase the drug/carrier ratio.

subject areas

  • Chlorambucil
  • Cross-Linking Reagents
  • Drug Carriers
  • Drug Delivery Systems
  • Humans
  • Immunoconjugates
  • Immunoglobulin Fragments
  • Solubility
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(03)00057-9

PubMed ID

  • 12659762
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Additional Document Info

start page

  • 1761

end page

  • 1768

volume

  • 11

issue

  • 8

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