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Development of Tethered Hsp90 Inhibitors Carrying Radioiodinated Probes to Specifically Discriminate and Kill Malignant Breast Tumor Cells

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Technical Report,01 May 2016,30 Apr 2017

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Duke University Duke United States

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We have proposed to develop tethered Hsp90 inhibitor capable of carrying various radioactive iodine isotopes for early detection and ablation of metastatic breast cancers. These probes specifically target a surface form of heat shock protein 90 eHsp90 that is expressed on malignant cells and internalized. In this report we describe our chemistry efforts to synthesize a non-radioactive tethered Hsp90 inhibitor and methods developed for stannylation of the molecule such that it can be effectively radioiodinated with either 131I or 124I. Two paths of synthesis were developed and optimized. A standard operating procedure was developed and then adapted and modified to provide workable protocols for radioiodination. An inactive control molecule was also developed, which can also be labeled with radioiodine to permit determination of specificity of radio-ligand localization. These molecules will be tested as imaging agents in mouse models of breast cancer.

Subject Categories:

  • Medicine and Medical Research
  • Radiobiology
  • Pharmacology

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