An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes

Bioorg Med Chem Lett. 1998 Apr 7;8(7):811-6. doi: 10.1016/s0960-894x(98)00095-x.

Abstract

In this paper we describe an approach to selectively deliver compounds to trypanosomes using an adenosine transporter which is unique to the trypanosome. Various polyamine analogues have been attached to known substrates of this adenosine transporter. The compounds prepared interact specifically with the adenosine transporter, some with a similar efficiency to berenil, a known substrate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / metabolism*
  • Animals
  • Biological Transport
  • Carrier Proteins / metabolism*
  • Indicators and Reagents
  • Kinetics
  • Polyamines / chemical synthesis*
  • Polyamines / chemistry
  • Polyamines / pharmacology*
  • Protozoan Proteins / metabolism*
  • Structure-Activity Relationship
  • Trypanocidal Agents / chemical synthesis*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / pharmacology
  • Trypanosoma brucei brucei / drug effects
  • Trypanosoma brucei brucei / metabolism*

Substances

  • Carrier Proteins
  • Indicators and Reagents
  • Polyamines
  • Protozoan Proteins
  • Trypanocidal Agents
  • Adenosine