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R3(B{Delta}23–27)R/I5 Chimeric Peptide

A Selective Antagonist for GPCR135 and GPCR142 over Relaxin Receptor LGR7

In Vitro and In Vivo Characterization

Both relaxin-3 and its receptor (GPCR135) are expressed predominantly in brain regions known to play important roles in processing sensory signals. Recent studies have shown that relaxin-3 is involved in the regulation of stress and feeding behaviors. The mechanisms underlying the involvement of relaxin-3/GPCR135 in the regulation of stress, feeding, and other potential functions remain to be studied. Because relaxin-3 also activates the relaxin receptor (LGR7), which is also expressed in the brain, selective GPCR135 agonists and antagonists are crucial to the study of the physiological functions of relaxin-3 and GPCR135 in vivo. Previously, we reported the creation of a selective GPCR135 agonist (a chimeric relaxin-3/INSL5 peptide designated R3/I5). In this report, we describe the creation of a high affinity antagonist for GPCR135 and GPCR142 over LGR7. This GPCR135 antagonist, R3(BDelta23–27)R/I5, consists of the relaxin-3 B-chain with a replacement of Gly23 to Arg, a truncation at the C terminus (Gly24-Trp27 deleted), and the A-chain of INSL5. In vitro pharmacological studies showed that R3(BDelta23–27)R/I5 binds to human GPCR135 (IC50 = 0.67 nM) and GPCR142 (IC50 = 2.29 nM) with high affinity and is a potent functional GPCR135 antagonist (pA2 = 9.15) but is not a human LGR7 ligand. Furthermore, R3(BDelta23–27)R/I5 had a similar binding profile at the rat GPCR135 receptor (IC50 = 0.25 nM, pA2 = 9.6) and lacked affinity for the rat LGR7 receptor. When administered to rats intracerebroventricularly, R3(BDelta23–27)R/I5 blocked food intake induced by the GPCR135 selective agonist R3/I5. Thus, R3(BDelta23–27)R/I5 should prove a useful tool for the further delineation of the functions of the relaxin-3/GPCR135 system.

Kuei et al. J Biol Chem. 2007 Aug 31;282(35):25425-35.

 

Mass Spec Analysis of R3(B{Delta}23–27)R/I5 Chimeric Peptide (# 035-66)

Mass Spec Analysis of 035-66

HPLC Analysis of R3(B{Delta}23–27)R/I5 Chimeric Peptide (# 035-66)

HPLC Analysis of 035-66 

Sequence of R3(B{Delta}23–27)R/I5 Chimeric Peptide (# 035-66)

%035-66%;%035-67%;%035-68%;%035-73%


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