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• W2154577215 startingPage "616" @default.
• W2154577215 abstract "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 to be as potent as commercially available 125I-tracers for the determination of agonists and to have increased sensitivity for antagonists. We applied it to investigate the predicted turn structures centered at Pro29 and Pro34. The substitution at positions 29 and 34 by turn-inducing amino acid mimetica showed that these turns are highly diverse. At position 29, a hydrophobic residue is preferred that constricts the secondary structure, whereas position 34 is required to stabilize the conformation of the backbone. All high-affinity analogues showed antagonistic properties with potency similar to CGRP 8−37." @default.
• W2154577215 created "2016-06-24" @default.
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• W2154577215 date "2005-12-22" @default.
• W2154577215 modified "2023-10-14" @default.
• W2154577215 title "Identification of the Key Residue of Calcitonin Gene Related Peptide (CGRP) 27−37 to Obtain Antagonists with Picomolar Affinity at the CGRP Receptor" @default.
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• W2154577215 doi "https://doi.org/10.1021/jm050613s" @default.
• W2154577215 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16420047" @default.
• W2154577215 hasPublicationYear "2005" @default.
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