An oxidation resistant radioligand for corticotropin-releasing factor receptors

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

doi:10.1016/S0196-9781(01)00424-7

An oxidation resistant radioligand for corticotropin-releasing factor receptors

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

School of Medicine

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

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 language	English (US)
Pages (from-to)	1055-1061
Number of pages	7
Journal	Peptides
Volume	22
Issue number	7
DOIs	https://doi.org/10.1016/S0196-9781(01)00424-7
State	Published - 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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10.1016/S0196-9781(01)00424-7

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title = "An oxidation resistant radioligand for corticotropin-releasing factor receptors",

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.",

keywords = "Chemical crosslinking, Corticotropin-releasing factor receptors, Disuccinimidyl suberate, Radioligands, Sauvagine, Urotensin-I",

author = "Assil, {Iman Q.} and Shomali, {Mansur E.} and Abou-Samra, {Abdul B.}",

year = "2001",

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doi = "10.1016/S0196-9781(01)00424-7",

language = "English (US)",

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journal = "Peptides",

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T1 - An oxidation resistant radioligand for corticotropin-releasing factor receptors

AU - Assil, Iman Q.

AU - Shomali, Mansur E.

AU - Abou-Samra, Abdul B.

PY - 2001/1/1

Y1 - 2001/1/1

N2 - 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.

AB - 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.

KW - Chemical crosslinking

KW - Corticotropin-releasing factor receptors

KW - Disuccinimidyl suberate

KW - Radioligands

KW - Sauvagine

KW - Urotensin-I

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U2 - 10.1016/S0196-9781(01)00424-7

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AN - SCOPUS:0034969464

SN - 0196-9781

VL - 22

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EP - 1061

JO - Peptides

JF - Peptides

IS - 7

ER -

An oxidation resistant radioligand for corticotropin-releasing factor receptors

Abstract

Keywords

ASJC Scopus subject areas

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