DEVELOPMENT OF A SMALL MOLECULE SELECTIVE EPHA2 INHIBITOR

Project Members:	Stephanie Heinzlmeir, Guillaume Médard
Cooperation:	Harald Schwalbe, Frankfurt; Xiaofeng Liu, Shanghai
Contact:	stephanie.heinzlmeir[at]tum.de

EphA2 is a receptor tyrosine kinase implicated in a number of cancer processes and has been identified as a potential therapeutic target. Many biological studies have been hampered by the absence of a selective small molecule EphA2 inhibitor. The project aims at discovering such inhibitors, which could also become drug candidates. The medicinal chemistry program involves the design of inhibitors using CADD methods, the synthesis of potential inhibitors via organic chemistry, the structural analysis of the protein-ligands complexes via NMR spectroscopy and X-ray crystallography, and the evaluation of the compounds' potency and selectivity by our kinobeads technology.