Optical and radioiodinated tethered Hsp90 inhibitors reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.

@article{Barrott2013OpticalAR,
  title={Optical and radioiodinated tethered Hsp90 inhibitors reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.},
  author={Jared James Barrott and Philip F Hughes and Takuya Osada and Xiao-yi Yang and Zachary C. Hartman and David R. Loiselle and Neil L. Spector and Leonard M. Neckers and Narasimhan Rajaram and Fangyao Hu and Nimmi Ramanujam and Ganesan Vaidyanathan and Michael R. Zalutsky and H Kim Lyerly and Timothy A. J. Haystead},
  journal={Chemistry & biology},
  year={2013},
  volume={20 9},
  pages={1187-97}
}
Inhibitors of heat-shock protein 90 (Hsp90) have demonstrated an unusual selectivity for tumor cells despite its ubiquitous expression. This phenomenon has remained unexplained, but could be influenced by ectopically expressed Hsp90 in tumors. In this work, we synthesized Hsp90 inhibitors that can carry optical or radioiodinated probes via a polyethyleneglycol tether. We show that these tethered inhibitors selectively recognize cells expressing ectopic Hsp90 and become internalized. The… CONTINUE READING
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