Development of a Radioligand to Detect Glucocorticoid Receptor Expression in Enzalutamide-Resistant Prostate Cancer with Positron Emission Tomography

Abstract

The purpose of this project is to develop radioligands to measure glucocorticoid receptor (GR) expression in enzalutamide resistant prostate cancer. GR was recently identified in a preclinical model of acquired resistance to enzalutamide, and its expression was confirmed in drug resistant patient specimens. As spontaneous GR overexpression is one of several potential mechanisms of resistance to enzalutamide, we are leading an effort to develop a translational imaging assay to detect those patients with resistance due to GR overexpression. A small library of two steroidal and one non-steroidal radioligand to GR have been developed. All three are potent and selective GR ligands in vitro. Moreover, we have shown that one steroidal radioligand is stable in vivo and can specifically target GR in normal and cancerous tissues.

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Document Details

Document Type
Technical Report
Publication Date
Dec 01, 2017
Accession Number
AD1089464

Entities

People

  • Michael J. Evans

Organizations

  • University of California, San Francisco

Tags

DTIC Thesaurus Topics

  • Biomedical Research
  • Department Of Defense
  • Detection
  • Emission
  • Medical Personnel
  • Molecules
  • Neoplasms
  • Nuclear Medicine
  • Positron Emission Tomography
  • Positron Emissions
  • Positrons
  • Professional Development
  • Prostate
  • Prostate Cancer
  • Resistance
  • Tissues
  • Tomography

Fields of Study

  • Biology

Readers

  • Medical Imaging.
  • Prostate Cancer Biology.