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Beschreibung

Full-length human GPR73 cDNA, encoding PK1, Prokineticins, also known as endocrine gland vascular endothelial growth factors (EG-VEGF), are two ~10 kD secreted proteins originally described to mediate angiogenesis and gastrointestinal smooth muscle contraction (Li et al., 2001, LeCouter et al., 2003). Subsequently, prokineticins have been found to mediate central nervous system functions including circadian rhythms and olfactory bulb development (Cheng et al., 2002, Ng et al., 2005). Two Gq-coupled receptors, PK1 and PK2 (also known as GPR73a and GPR73b), mediate cellular responses to prokineticins (Lin et al., 2002). Chemicon's PK1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression, thus, they are ideal HTS tools for screening of antagonists of PK1 interactions and its ligands. The membrane preparations exhibit a Kd of 0.11 nM for [125I]-Mamba Intestinal Toxin-1 (MIT-1). With 0.2 nM [125I]-MIT-1, 2.5 µ,g/well and 5 µ,g/well PK1 Membrane Prep typically yield greater than 5-fold signal-to-background ratio.