Development of Coactivator-Dependent, First-in-Class Therapies for Breast Cancer

Abstract

By integrating multiple signaling pathways that cancer cells rely on for growth and survival, p160 steroid receptor coactivator (SRC) family members (SRC-1, SRC-2/TIF2/GRIP1, SRC- 3/AIB1/pCIP/RAC3) represent emerging targets for anti-cancer drug development. During this reporting period, we have characterized and published our work on two potent and selective small molecule inhibitors (SMIs), bufalin and verrucarin A, against SRCs from high throughput screening efforts. Cryo-electron microscopic analyses of DNA/estrogen receptor/SRC-3 protein complexes achieved by our group are providing powerful new insights into understanding the conformation of intact, full length proteins in a complex and should provide valuable new information on the mechanism of action of SRC SMIs as well.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2014
Accession Number
ADA614113

Entities

People

  • Bert W. O’malley

Organizations

  • Baylor College of Medicine

Tags

DTIC Thesaurus Topics

  • Antineoplastic Agents
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Epithelial Cells
  • Gene Expression
  • Glucose Metabolism Disorders
  • Medical Personnel
  • Oncology

Fields of Study

  • Biology
  • Chemistry

Readers

  • Breast cancer cell signaling and growth regulation.
  • Molecular and Cellular Biochemistry
  • Prostate Cancer Biology.

Technology Areas

  • Microelectronics