Metal ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor.

@article{Gerlach2003MetalIE,
  title={Metal ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor.},
  author={Lars Ole Gerlach and Janus S Jakobsen and Kasper P. Jensen and Mette R Rosenkilde and Renato T Skerlj and Ulf Ryde and Gary J Bridger and Thue W. Schwartz},
  journal={Biochemistry},
  year={2003},
  volume={42 3},
  pages={
          710-7
        }
}
The affinity of AMD3100, a symmetrical nonpeptide antagonist composed of two 1,4,8,11-tetraazacyclotetradecane (cyclam) rings connected through a 1,4-dimethylene(phenylene) linker to the CXCR4 chemokine receptor was increased 7, 36, and 50-fold, respectively, by incorporation of the following: Cu(2+), Zn(2+), or Ni(2+) into the cyclam rings of the compound. The rank order of the transition metal ions correlated with the calculated binding energy between free acetate and the metal ions… CONTINUE READING
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