Accession Number:

ADA614113

Title:

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

Descriptive Note:

Annual rept. 15 Aug 2013-14 Aug 2014

Corporate Author:

BAYLOR COLL OF MEDICINE HOUSTON TX

Personal Author(s):

Report Date:

2014-09-01

Pagination or Media Count:

66.0

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-2TIF2GRIP1, SRC- 3AIB1pCIPRAC3 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 DNAestrogen receptorSRC-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.

Subject Categories:

  • Biochemistry
  • Anatomy and Physiology
  • Medicine and Medical Research
  • Pharmacology
  • Organic Chemistry

Distribution Statement:

APPROVED FOR PUBLIC RELEASE