Journal article
R3(BΔ23-27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: In vitro and in vivo characterization
C Kuei, S Sutton, P Bonaventure, C Pudiak, J Shelton, J Zhu, D Nepomuceno, J Wu, J Chen, F Kamme, M Seierstad, MD Hack, RAD Bathgate, MA Hossain, JD Wade, J Atack, TW Lovenberg, C Liu
Journal of Biological Chemistry | AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC | Published : 2007
Abstract
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 ag..
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