TABLE 3

Ligands of Mrgprs

Some structures are shown on the bottom of the table. The EC50 values are different depending on the assay system used in each publication and can only be taken as estimation concerning the specificity of the receptors.

MrgprLigandsStructure or Peptide SequenceEC50References
µM
MasAngiotensin-(1–7)DRVYIHPN.D., kD: 0.08nMDong et al., 2001; Santos et al., 2003; Jankowski et al., 2011
NPFFFLFQPQRF-amide0.4
AngioprotectinPEVYIHPN.D.
mMrgprA1FLRFFLRF-amide0.02–0.4Dong et al., 2001; Han et al., 2002; Wang et al., 2006
NPFFFLFQPQRF-amide0.2–2.1
Salusin-βAIFIFIRWLLKLGHHGRAPP0.30
mMrgprA3Chloroquinesee below0.028Liu et al., 2009
mMrgprA4NPAFAGEGLNSQFWSLAAPQRF-amide0.06Dong et al., 2001
ACTH39 amino acids0.2
mMrgprA9Adeninesee below0.01von Kügelgen et al., 2008
mMrgprA10Adeninesee below0.01Thimm et al., 2013
rMrgprAAdeninesee below0.02Bender et al., 2002; Gorzalka et al., 2005
mMrgprX1γ1-MSHYVMGHFRWDRF-amide0.017Han et al., 2002; Liu et al., 2011; He et al., 2014
γ2-MSHYVMGHFRWDRFG0.011
FLRFFLRF-amide0.157
NPFFFLFQPQRF-amide0.054
SLGRLSLGRL10.1
BAM22YGGFMRRVGRPEWWMDYQKRYG0.026
BAM8–22VGRPEWWMDYQKRYG0.053
Antho-RFamidepEGFR-amide0.016
rMrgprX1BAM22,YGGFMRRVGRPEWWMDYQKRYG0.155Grazzini et al., 2004; He et al., 2014
BAM8–22,VGRPEWWMDYQKRYG0.12
γ1-MSHYVMGHFRWDRF-amide0.063
γ2-MSHYVMGHFRWDRFG0.037
MrgprD (rat, mouse, and human)β-Alaninesee below14–44Shinohara et al., 2004; Lautner et al., 2013
GABAsee below165- > 300
AlamandineARVYIHP
hMRGPRX7γ1-MSHYVMGHFRWDRF-amide0.46Lembo et al., 2002
SNSR3BAM22,YGGFMRRVGRPEWWMDYQKRYG0.013
BAM8–22VGRPEWWMDYQKRYG0.028
hMRGPRX1γ1-MSHYVMGHFRWDRF-amide0.6Lembo et al., 2002; Tatemoto et al., 2006; Hager et al., 2008; Liu et al., 2009; Kashem et al., 2011
Compound 48/80see below70
BAM22,YGGFMRRVGRPEWWMDYQKRYG0.016
BAM8–22VGRPEWWMDYQKRYG0.014–0.04
Chloroquinesee below0.3
hMRGPRX2MCDMCICKNGKPLPGFIGKICRKICMMEETH-amide1.25Robas et al., 2003; Kamohara et al., 2005; Nothacker et al., 2005; Tatemoto et al., 2006; Subramanian et al., 2013
PACAP38 amino acids1.64
Substance PRPKPEEFFGLM-amide2.4–8.0
Platelet factor-470 amino acids8.96
VIPHSDAVFTDNYTRLRKQMAVKKYLNSILN2.63
Cortistatin-14PCKNFFWKTFSSCK0.03–0.06
PAMP-12FRKKWNKWALSR3.75
Compound 48/80see below0.06
SomatostatinAGCKNFFWKTFTSC0.03–5.70
β-Defensins> 40 amino acidsN.D.
Cathelicidines35–40 amino acids65
Embedded ImageEmbedded ImageEmbedded ImageEmbedded ImageEmbedded Image
ChloroquineAdenineβ-AlanineGABACompound 48/80
  • N.D., not determined; NPAF, neuropeptide AF; NPFF, neuropeptide FF.