Three-way junction nanoparticles for delivery of tamoxifen and other therapeutics directly to tumor cells.



The Need

Most breast cancers express estrogen receptor alpha (ER α) and antagonists of ER α drugs, such as tamoxifen, have been widely used for their treatment. Unfortunately, up to half of all ER α -positive tumors have intrinsic or acquired endocrine therapy resistance. Recent studies by the present investigators revealed that the ER coactivator Mediator Subunit 1 (MED1) plays a critical role in tamoxifen resistance through cross-talk with HER2.

The Technology

A three-way junction nanoparticle specifically designed and self-assembled to target HER2-overexpressing human cancer by utilizing a HER2 RNA aptamer and to deliver MED1 siRNA to the cancer cells to effectively silence MED1 expression. The inventive nanoparticles specifically bind to HER2-overexpressing breast cancer cells, efficiently deplete MED1 expression and significantly decrease gene transcription. The extended arms of the 3 way motif are readily replaced with siRNAs and other RNA aptamers and the nanoparticles are ultra-compact with a very high Tm value. Proof-of-concept murine models were conducted and results showed that the nanoparticles targeted HER2 overexpressing breast cancer and silenced MED1 expression.

Commercial Applications

  • Cancer therapeutic treatment for
    • breast
    • uterine
    • ovarian
    • stomach
    • bladder
    • lung
    • salivary
  • Treatment for those with primary or acquired resistance to anti-estrogenic agents

Benefits/Advantages

  • Uniform nano-scale size
  • Precise stoichiometry
  • Stable and biocompatible
  • High Tm value
  • Non-toxic following systemic administration



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