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

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 deve...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-01, Vol.49 (2), p.616-624
Hauptverfasser:	Lang, Manja, De Pol, Silvia, Baldauf, Carsten, Hofmann, Hans-Jörg, Reiser, Oliver, Beck-Sickinger, Annette G
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Binding, Competitive Biological and medical sciences Calcitonin Gene-Related Peptide - chemical synthesis Calcitonin Gene-Related Peptide - chemistry Calcitonin Gene-Related Peptide - pharmacology Contrast media. Radiopharmaceuticals Humans Isotope Labeling Medical sciences Models, Molecular Molecular Sequence Data Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptide Fragments - chemical synthesis Peptide Fragments - chemistry Peptide Fragments - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Protein Structure, Secondary Radioligand Assay Receptors, Calcitonin Gene-Related Peptide - agonists Receptors, Calcitonin Gene-Related Peptide - antagonists & inhibitors Structure-Activity Relationship Tritium
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