Immunobiological Aspects of erbB Receptors in Breast Cancer.
Abstract
The studies have begun to identify the specific roles of distinct tyrosines in a receptor oncoprotein that plays a role in breast cancer. By using a variety of mutant forms of p185neu we showed that in vitro and in vivo activity of mutants that have an intrakinase Y right arrow F mutation is dramatically reduced. To date we have successfully analyzed the role of the intrakinase tyrosine at position 882 and determined it is critical for the transforming activity of p185. The studies have consistently revealed that, biochemically and biologically, the tyrosine at 882 is critical for the receptor's activity. At present we believe that the tyrosine 882 may influence substrate access to the active site of the kinase. These results may help in the development of specific kinase inhibitors that can be used to block the activity of p185 homomers or heteromers that are active in the development of breast neoplasia. Our recommendations for future studies are to use this information in the structural design of erbB kinase inhibitors.
Document Details
- Document Type
- Technical Report
- Publication Date
- Aug 01, 1997
- Accession Number
- ADA332853
Entities
People
- Mark I. Greene
Organizations
- University of Pennsylvania