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Identification of the Key Residue of Calcitonin Gene Related Peptide (CGRP) 27-37 to Obtain Antagonists with Picomolar Affinity at the CGRP Receptor

Lang, Manja ; De Pol, Silvia ; Baldauf, Carsten ; Hofmann, Hans-Jörg ; Reiser, Oliver ; Beck-Sickinger, Annette G.


Calcitonin gene related peptide (CGRP) plays an important role in the CNS and in the cardiovascular system. To identify high-affinity antagonists in competitive binding studies, we identified a novel radioactive tracer, [³H-propionyl-K²⁴]-hαCGRP 8-37, which was labeled in solution by a recently developed strategy using photolabile protecting groups at reactive side chains. This tracer was shown ...


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