Abstract
e.g. appetite regulation, energy homeostasis, bone formation, circadian rhythm, memory retention, obesity, epilepsy, angiogenesis and cancer (Pedragosa-Badia et al., 2013; Walther et al., 2011). In various tumor tissues the hY2R is overexpressed and promotes tumor growth and vascularization (Lorner and Reubi, 2008). Therefore, the hY2R has great therapeutic potential and antagonists could represent promising drugs for the treatment of neuroblastoma or glioblastoma. Wewere interested in investigating the binding mode of BIIE0246, compound 40 and compound46 at the hY2R (Mittapalli et al., 2012).We generated receptor mutants and tested membrane localization by fluorescence microscopy and signal transduction by inositol phosphate accumulation assay in presence of pNPY and pNPY/antagonist. Here we report on suggested binding modes of three different antagonists on hY2R, which opens up the possibility for the development of more selective compounds.
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