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000418101 1001_ $$aTröster, Alix$$b0
000418101 245__ $$aNVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family
000418101 260__ $$aWeinheim [u.a.]$$bWiley-VCH$$c2018
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000418101 520__ $$aErythropoietin‐producing hepatocellular (EPH) receptors are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates intracellular kinase activity. EPHs are key players in bidirectional intercellular signaling, controlling cell morphology, adhesion, and migration. They are increasingly recognized as cancer drug targets. We analyzed the binding of NVP‐BHG712 (NVP) to EPHA2 and EPHB4. Unexpectedly, all tested commercially available NVP samples turned out to be a regioisomer (NVPiso) of the inhibitor, initially described in a Novartis patent application. They only differ by the localization of a single methyl group on either one of two adjacent nitrogen atoms. The two compounds of identical mass revealed different binding modes. Furthermore, both in vitro and in vivo experiments showed that the isomers differ in their kinase affinity and selectivity.
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000418101 7001_ $$aHeinzlmeir, Stephanie$$b1
000418101 7001_ $$00000-0002-3314-2617$$aBerger, Benedict-Tilman$$b2
000418101 7001_ $$aGande, Santosh L.$$b3
000418101 7001_ $$aSaxena, Krishna$$b4
000418101 7001_ $$aSreeramulu, Sridhar$$b5
000418101 7001_ $$0P:(DE-H253)PIP1025964$$aLinhard, Verena$$b6
000418101 7001_ $$aNasiri, Amir H.$$b7
000418101 7001_ $$00000-0001-5296-6251$$aBolte, Michael$$b8
000418101 7001_ $$aMüller, Susanne$$b9
000418101 7001_ $$aKuster, Bernhard$$b10
000418101 7001_ $$00000-0002-4782-4029$$aMédard, Guillaume$$b11$$eCorresponding author
000418101 7001_ $$0P:(DE-H253)PIP1016055$$aKudlinzki, Denis$$b12$$eCorresponding author
000418101 7001_ $$0P:(DE-H253)PIP1019273$$aSchwalbe, Harald$$b13$$eCorresponding author
000418101 773__ $$0PERI:(DE-600)2209649-8$$a10.1002/cmdc.201800398$$gVol. 13, no. 16, p. 1629 - 1633$$n16$$p1629 - 1633$$tChemMedChem$$v13$$x1860-7179$$y2018
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