Inhibitors of tyrosine kinase receptor dimerization
US8404838B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 10, 2011 |
| Grant date | Mar 26, 2013 |
| Priority date | — |
| Expiry date | Jun 10, 2031 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG16C20/50
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.