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Research ArticleArticle

Relaxin-3/Insulin-Like Peptide 5 Chimeric Peptide, a Selective Ligand for G Protein-Coupled Receptor (GPCR)135 and GPCR142 over Leucine-Rich Repeat-Containing G Protein-Coupled Receptor 7

Changlu Liu, Jingcai Chen, Chester Kuei, Steven Sutton, Diane Nepomuceno, Pascal Bonaventure and Timothy W. Lovenberg
Molecular Pharmacology January 2005, 67 (1) 231-240; DOI: https://doi.org/10.1124/mol.104.006700
Changlu Liu
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Jingcai Chen
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Chester Kuei
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Steven Sutton
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Diane Nepomuceno
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Pascal Bonaventure
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Timothy W. Lovenberg
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Abstract

Relaxin-3, the most recently identified member of relaxin/insulin family, is an agonist for leucine-rich repeat-containing G protein-coupled receptor (LGR)7, GPCR135, and GPCR142. LGR7 can be pharmacologically differentiated from GPCR135 and GPCR142 by its high affinity for relaxin. Selective ligands that specifically activate GPCR135 or GPCR142 are highly desirable for studying their functional roles. We have created chimeric peptides that consist of the B-chain of human relaxin-3 in combination with various A-chains from other members of the relaxin/insulin family. Pharmacological characterization of these chimeric peptides indicates the A-chain from relaxin-1, relaxin-2, insulin-like peptide (INSL)3, and INSL6 does not change the pharmacological properties of relaxin-3 significantly. In contrast, substitution of the relaxin-3 A-chain with the A-chain from INSL5 results in a chimeric peptide that selectively activates GPCR135 and GPCR142 over LGR7. This study demonstrates that the A-chains among some of the insulin/relaxin family members are pharmacologically exchangeable. The relaxin-3/INSL5 chimeric peptide is a potential tool to study in vivo function of GPCR135. In addition, because of the substitution of a very hydrophobic peptide (the A-chain of relaxin-3) with a very hydrophilic peptide (the A-chain from INSL5), the radiolabeled 125I-relaxin-3/INSL5 chimera is a suitable ligand (high-affinity, low-nonspecific binding) for receptor autoradiographic studies on tissue sections.

  • Received August 30, 2004.
  • Accepted September 30, 2004.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 67 (1)
Molecular Pharmacology
Vol. 67, Issue 1
1 Jan 2005
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Relaxin-3/Insulin-Like Peptide 5 Chimeric Peptide, a Selective Ligand for G Protein-Coupled Receptor (GPCR)135 and GPCR142 over Leucine-Rich Repeat-Containing G Protein-Coupled Receptor 7
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Research ArticleArticle

Relaxin-3/Insulin-Like Peptide 5 Chimeric Peptide, a Selective Ligand for G Protein-Coupled Receptor (GPCR)135 and GPCR142 over Leucine-Rich Repeat-Containing G Protein-Coupled Receptor 7

Changlu Liu, Jingcai Chen, Chester Kuei, Steven Sutton, Diane Nepomuceno, Pascal Bonaventure and Timothy W. Lovenberg
Molecular Pharmacology January 1, 2005, 67 (1) 231-240; DOI: https://doi.org/10.1124/mol.104.006700

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Research ArticleArticle

Relaxin-3/Insulin-Like Peptide 5 Chimeric Peptide, a Selective Ligand for G Protein-Coupled Receptor (GPCR)135 and GPCR142 over Leucine-Rich Repeat-Containing G Protein-Coupled Receptor 7

Changlu Liu, Jingcai Chen, Chester Kuei, Steven Sutton, Diane Nepomuceno, Pascal Bonaventure and Timothy W. Lovenberg
Molecular Pharmacology January 1, 2005, 67 (1) 231-240; DOI: https://doi.org/10.1124/mol.104.006700
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