Development of Specific Inhibitors for Breast Cancer-Associated Variants of ErbB2
Abstract
The receptor tyrosine kinase HER2/ErbB2 is one of the most highly mutated tyrosine kinases in breast cancer. Several mutations within the ErbB2 kinase domain have been identified in breast cancer patients, but in most cases it is not known whether these mutations increase kinase activity and signaling. The first objective of this project is to provide data linking ErbB2 mutations to their degree of kinase activation. The second objective is to use computational screening methods to identify compounds that can selectively target and inhibit those ErbB2 mutants verified as active. The third objective is to experimentally test a subset of the most promising compounds for the ability to experimentally inhibit specific ErbB2 mutants. The research team consists of two principal investigators at the same institution: Dr. Todd Miller (Initiating PI, Grant Number BC132617) whom has expertise in tyrosine kinase signaling, and Dr. Robert C. Rizzo (Partnering PI, Grant Number, BC132617P1) whom has expertise in computational modeling procedures. This report, prepared by Partnering PI Rizzo and his team, will primarily focus on the computational progress. The Initiating PI Miller has submitted a separate report.
Document Details
- Document Type
- Technical Report
- Publication Date
- Oct 01, 2015
- Accession Number
- ADA624304
Entities
People
- Robert C Rizzo
Organizations
- State University of New York