Is myricerone caffeoyl ester ( 50-235 ) a non-peptide antagonist selective for human ETA receptors?
The antagonist 50-235 exhibits nanomolar affinity for human ETA receptors and 500-fold selectivity for ETA compared with ETB receptors. Its novel non-peptide structure demonstrates that the carbon-nitrogen bond is not crucial for endothelin antagonist activity, and might provide important information for the development of therapeutic agents for conditions in which endothelins may be pathophysiologically relevant.
SU11652 is a potent FLT3 inhibitor which selectively targets FLT3-ITD-positive cells. It should serve as a good candidate for development of therapeutic drugs to treat AML.