Targeting Prostate Cancer with Bifunctional Modulators of the Androgen Receptor

Abstract

The overall goal of this research project is to develop and implement a conceptually innovative strategy for down-regulating androgen receptor: the creation of bifunctional molecules that simultaneously bind to the androgen receptor and to bromodomain proteins Brd4. In this way, genes that are typically regulated by androgen receptor and glucocorticoid receptor will be extrinsically controlled. In this final year of funding, we completed the functional characterization of agonist and antagonist-based bi-functional recruiters. Importantly, we have a suite of recruiters that show context specificity. In the extension period of the work, we are completing RNAseq experiments to gain a complete understanding of the context specificity of this exciting class of molecules.

Open PDF

Document Details

Document Type
Technical Report
Publication Date
Oct 01, 2014
Accession Number
ADA620319

Entities

People

  • Aaron Van Dyke
  • Anna K. Mapp
  • James Carolan
  • Steven Sturlis

Organizations

  • University of Michigan

Tags

DTIC Thesaurus Topics

  • Androgen Receptors
  • Androgens
  • Biological Sciences
  • Biomedical Research
  • Cell Line
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Epithelial Cells
  • Inhibitors
  • Molecules
  • Neoplasms
  • Prostate
  • Prostate Cancer
  • Proteins
  • Small Molecules
  • Targeting

Fields of Study

  • Biology

Readers

  • Molecular Genetics
  • Prostate Cancer Biology.
  • Systems Analysis and Design