Bumped Kinase Inhibitors as Castrate Resistant Prostate Cancer Drugs

Abstract

Kinase inhibitors present exciting therapies for cancer including prostate cancer. We have developed a class of kinase inhibitors, bumped kinase inhibitors (BKIs), that have narrow kinase specificity due to their unique binding of the ATP-binding site and activity against androgen receptor (AR) positive prostate cancer cells. Despite of the life extending therapies of the newest drugs targeting the AR e.g. abiraterone and enzalutamide, tumors almost universally acquire resistance, and survival is extended by only four months. Hypotheses 1: BKIs are specific candidates for treatment of AR-driven CRPC. 2: BKIs act directly or indirectly by inhibition of AR Ser81 phosphorylation necessary to activate AR to stimulate transcription.

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Document Details

Document Type
Technical Report
Publication Date
Jan 01, 2022
Accession Number
AD1215030

Entities

People

  • Stephen R Plymate

Organizations

  • University of Washington

Tags

DTIC Thesaurus Topics

  • Acquisition
  • Androgen Receptors
  • Androgens
  • Biochemistry
  • Biomedical Research
  • Cell Line
  • Cells
  • Chemistry
  • Department Of Defense
  • Inhibitors
  • Kinases
  • Law
  • Lead Compounds
  • Medical Personnel
  • Neoplasms
  • Patent Applications
  • Patents
  • Prostate
  • Prostate Cancer
  • Students

Fields of Study

  • Biology

Readers

  • Oncology (Cancer Research).
  • Prostate Cancer Biology.