Inhibition of Her2 Transcription by Small Organic Molecules
Abstract
Overexpression of the Her2 protein has been found in -30% of breast tumors, and the inhibition of Her2 expression may be an effective way to treat Her2-positive patients. In the first year, the P.I. and co-workers discovered adamanolol, a drug-like compound that impairs the viability of Her2 positive breast cancer cell lines by reducing the expression of Her2. In the second year of funding, we conducted structure-activity relationship studies of adamanolol derivatives and designed a second-generation compound we named "wrenchnolol." The wrench-shaped structure of wrenchnolol permitted detailed biochemical and biophysical analysis of the compound including evaluation of dissociation constants, subcellular localization, binding selectivity in cells. Wrenchnolol is a chemically tractable compound that is suited for mechanistic analysis and for further application.
Document Details
- Document Type
- Technical Report
- Publication Date
- Apr 01, 2004
- Accession Number
- ADA425740
Entities
People
- Motonari Uesugi
- Yongmun Choi
Organizations
- Baylor College of Medicine