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Structural Chemistry

, Volume 30, Issue 1, pp 175–184 | Cite as

Structure–activity relationship of polyamine conjugates for uptake via polyamine transport system

  • S. Mohamad Reza Nazifi
  • Hojjat Sadeghi-aliabadi
  • Afshin Fassihi
  • Lotfollah SaghaieEmail author
Review Article
  • 26 Downloads

Abstract

High toxicity of anticancer drugs led to development of targeted drug delivery directly to the specific organs. Polyamine transport system (PTS) of mammalian cells is one of the targets for a cell-selective drug delivery of polyamine–drug conjugates into specific organs. Even without having a 3D structure for mammalian PTS, synthesis of polyamine derivatives and evaluation of their cytotoxic effects are potential practical approaches to find optimal polyamine moieties to be transported from the PTSs. Chinese hamster ovary (CHO) and its mutant cell line (CHO-MG) are two important cells for evaluation of polyamine transportation by polyamine transporters (PAT). If a polyamine conjugate ligand demonstrates a high IC50 ratio on CHO-MG/CHO cells, this indicates a high selectivity of such compound toward PAT. This study discussed the structural requirements (charge, linker, vector, cargo) of polyamine conjugates in order to be transported into the cells by the mean of PTS.

Keywords

Polyamine conjugates Polyamine transport system (PTS) Membrane transporter Chinese hamster ovary (CHO) CHO-MG 

Notes

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • S. Mohamad Reza Nazifi
    • 1
  • Hojjat Sadeghi-aliabadi
    • 1
  • Afshin Fassihi
    • 1
  • Lotfollah Saghaie
    • 1
    Email author
  1. 1.Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical SciencesIsfahan University of Medical SciencesIsfahanIran

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