Activated Ras as a Direct Therapeutic Target for Neurofibromatosis Type 1: An Innovative Approach for Identifying Classes of Inhibitors
Abstract
Neurofibromatosis Type 1 (NF1) arises from the aberrant activation of Ras, a GTPases important controlling mitogenic potential. In an effort to control the aberrant activation of Ras to treat NF1 as well as other cancer, a high throughput screen was developed to screen for small molecule inhibitors of Ras activation by Sos1, a ubiquitous guanine nucleotide exchange factor that catalyzes the activation of Ras. Using this screen, several initial leads have been identified. Future work will define the efficacy and modes of action of these compounds to inhibit Sos1-catalyzed activation of Ras prior to more extensive quantitative structure-activity relationships.
Document Details
- Document Type
- Technical Report
- Publication Date
- Dec 01, 2006
- Accession Number
- ADA465849
Entities
People
- John Sondek
Organizations
- University of North Carolina at Chapel Hill