An oxidation resistant radioligand for corticotropin-releasing factor receptors

The methionine residues in Tyr-corticotropin-releasing factor (CRF) and Tyr-sauvagine radioligands are subject to oxidation, which renders them biologically inactive. Therefore [Tyr 0, Gln 1, Leu 17]sauvagine (YQLS), in which the methionine was replaced with leucine was synthesized and labeled with...

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Veröffentlicht in:	Peptides (New York, N.Y. : 1980) N.Y. : 1980), 2001-07, Vol.22 (7), p.1055-1061
Hauptverfasser:	Assil, Iman Q., Shomali, Mansur E., Abou-Samra, Abdul.B.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Amphibian Proteins Animals Brain - metabolism Cells, Cultured Chemical crosslinking Chloramines - pharmacology Corticotropin-releasing factor receptors COS Cells Cross-Linking Reagents - pharmacology Cyclic AMP - metabolism Disuccinimidyl suberate DNA, Complementary - metabolism Dose-Response Relationship, Drug Iodine - pharmacology Leucine - chemistry Ligands Mass Spectrometry Methionine - chemistry Mice Molecular Sequence Data Oxygen - metabolism Peptide Hormones Peptides - chemistry Peptides - pharmacology Protein Binding Radioligands Receptors, Corticotropin-Releasing Hormone - chemistry Receptors, Corticotropin-Releasing Hormone - metabolism Sauvagine Sequence Homology, Amino Acid Succinimides - pharmacology Tyrosine - chemistry Urotensin-I Urotensins - metabolism Vasodilator Agents - pharmacology
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Zusammenfassung:	The methionine residues in Tyr-corticotropin-releasing factor (CRF) and Tyr-sauvagine radioligands are subject to oxidation, which renders them biologically inactive. Therefore [Tyr 0, Gln 1, Leu 17]sauvagine (YQLS), in which the methionine was replaced with leucine was synthesized and labeled with 125Iodine using chloramine-T. Mass spectroscopy revealed that chloramine-T-treatment did not oxidize YQLS. 125I-YQLS bound with high affinity to cells expressing the murine CRF receptor 1 (CRFR1), CRF receptor 2 (CRFR2), and the mouse brain regions known to express both CRF receptors. 125I-YQLS chemically cross-linked to CRFR1. In conclusion, 125I-YQLS is oxidation-resistant, high affinity radioligand that can be chemically cross-linked to the CRF receptors.
ISSN:	0196-9781 1873-5169
DOI:	10.1016/S0196-9781(01)00424-7