A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB: 1Y6A complex–Medicinal chemistry consequences of a TKs analysis

…, M García-Caballero, F Gregáň, M Melicherčík…

Index: Lintnerova, Lucia; Garcia-Caballero, Melissa; Gregan, Fridrich; Melichercik, Milan; Quesada, Ana R.; Dobias, Juraj; Lac, Jan; Salisova, Marta; Bohac, Andrej European Journal of Medicinal Chemistry, 2014 , vol. 72, p. 146 - 159

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Citation Number: 10

Abstract

Abstract VEGFR2 is an important mediator of angiogenesis and influences fate of some cancer stem cells. Here we analysed all 34 structures of VEGFR2 TK available from PDB database. From them a complex PDB: 1Y6A has an exceptional AAZ ligand bound to TK in form of two conformers (U-and S-shaped). This observation inspired us to develop three chimeric bispyridyl VEGFR2 inhibitors by combining structural features of both AAZ ...