An oxidation resistant radioligand for corticotropin-releasing factor receptors

Iman Q. Assil, Mansur E. Shomali, Abdul B. Abou-Samra

Research output: Contribution to journalArticle

Abstract

The methionine residues in Tyr-corticotropin-releasing factor (CRF) and Tyr-sauvagine radioligands are subject to oxidation, which renders them biologically inactive. Therefore [Tyr0 Gln1 Leu17]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.

Original languageEnglish (US)
Pages (from-to)1055-1061
Number of pages7
JournalPeptides
Volume22
Issue number7
DOIs
StatePublished - Jan 1 2001

Keywords

  • Chemical crosslinking
  • Corticotropin-releasing factor receptors
  • Disuccinimidyl suberate
  • Radioligands
  • Sauvagine
  • Urotensin-I

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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