TABLE 2

Peptides binding to class A GPCRs with key regions important for activity

PeptideReceptorSequence of a Peptide or Short Active Peptide Fragment (Peptide Region Important for Activity is Highlighted in Grey, Cysteine Involved in the Disulfide Bridges Are in Bold.)End Group Important for ActivityPeptide Terminal End Inside the Helical BundleReference
AngiotensinAT1, AT2Embedded Image-COOHC-endRioux et al., 1975; Karnik 2000; Asada et al., 2018
ApelinAPLNREmbedded Image-COOHC-endMurza et al., 2012; Ma et al., 2017
BradykininB1, B2Embedded Image-COOHC-endRhaleb et al., 1990; Jarnagin et al., 1996; Ha et al., 2006
Complement PeptidesEmbedded Image-COOHC-endMollison et al., 1989; Higginbottom et al., 2005; Klos et al., 2013; Liu et al., 2018
C3aC3a
C5aC5a1, C5a2
EndothelinETA ETBEmbedded Image-COOHC-endRovero et al., 1990; Shihoya et al., 2016
NeurotensinNTS1, NTS2Embedded Image-COOHC-endLabbe-Jullie et al., 1998; White et al., 2012; Kleczkowska and Lipkowski, 2013)
C-end of Chain BBathgate et al., 2013; Hu et al., 2017; Patil et al., 2017; Wong et al., 2018
H2 relaxinRXFP1Embedded Image
Insulin-like peptide 3 (INSL3)RXFP2Embedded ImageEmbedded Image
H3 relaxinRXFP3Embedded ImageC-end of Chain B
INSL5RXFP4Embedded ImageC-end of chain B
Cholecystokinin gastrinCCK1
CCK2
Embedded ImageEmbedded Image-CONH2C-endMorley et al., 1965; Jensen et al., 1982; Black and Kalindjian, 2002; Archer-Lahlou et al., 2005; Dufresne et al., 2006
OrexinOX1, OX2Embedded Image-CONH2C-endDarker et al., 2001; Ammoun et al., 2003; Lang et al., 2004; Heifetz et al., 2013
Neuropeptide YNPY1, 2, 4, and 5Embedded Image-CONH2C-endBoublik et al., 1989; Xu et al., 2013, 2018; Yang et al., 2018
Prolactin-releasing peptidePrRPEmbedded Image-CONH2C-endBoyle et al., 2005; Findeisen et al., 2011; Rathmann et al., 2012
Pyroglutamylated RFamide peptideQRFPEmbedded Image-CONH2C-endFindeisen et al., 2011
Neuropeptide FFNPFF1-2Embedded Image-CONH2C-endFindeisen et al., 2011
Metastin/kisspeptinKISS1REmbedded Image-CONH2C-endKotani et al., 2001; Findeisen et al., 2011
VasopressinV1A, V1B, V2Embedded Image-CONH2Cyclic endJard and Bockaert, 1975; Mouillac et al., 1995; Chini and Fanelli, 2000
OxytocinOTEmbedded Image-CONH2Cyclic endJard and Bockaert, 1975; Chini and Fanelli, 2000; Gimpl and Fahrenholz, 2001
Neuromedin BBB1Embedded Image-CONH2C-endMervic et al., 1991; Lin et al., 1995; Jensen et al., 2008
Gastrin-relesing peptideBB2Embedded Image
BombesinBB3Embedded Image
Neuromedin-UNMU1-2Embedded Image-CONH2C-endBrighton et al., 2004; Kawai et al., 2014
Substance-P/K, neurokinin, tachykininNK1, NK2, NK3Embedded Image-CONH2C-endCouture et al., 1979; Ganjiwale et al., 2011
Neurokinin A
Neurokinin B
Thyrotropin-releasing hormoneTRH1Embedded Image-CONH2AllChang et al., 1971; Engel and Gershengorn, 2007
Opioid peptides endorphinsDOR, KOR, MOR, NOPEmbedded ImageH2N-N-endMorley 1983; Koehl et al., 2018
Neuropeptides B/WNPBW1-2Embedded ImageN-endKanesaka et al., 2007
Neuropeptide SNPSR1Embedded ImageN-endRoth et al., 2006
N-formyl peptideFPR1-3Embedded ImageO=HC-NH-N-endProssnitz and Ye, 1997
Adrenocorticotropic hormoneMC1–5Embedded ImageO=HC-NH-FRWSchwyzer, 1977; Matsunaga et al., 1989; Schioth et al., 1997; Audinot et al., 2001; Haskell-Luevano et al., 2001
Melanocortins (α, β, and γ)
MotilinMLNREmbedded ImageN-endPoitras et al., 1992; Xu et al., 2005
GhrelinGHSREmbedded ImageN-endCharron et al., 2017
Gonadotropin-releasing hormoneGNRHREmbedded ImageCONHCHO-N-endHoffmann et al., 2000; Padula, 2005; Barran et al., 2005
GalaninGAL1-3Embedded ImageH2N-N-endChurch et al., 2002; Lang et al., 2015
UrotensinUTEmbedded ImageCyclic portionLabarrere et al., 2003; Merlino et al., 2013
Melanin-concentrating hormoneMCH1-2Embedded ImageCyclic portionMatsunaga et al., 1989; Schioth et al., 1997; Audinot et al., 2001
SomatostatinSST1-5Embedded ImageCyclic portionVale et al., 1978; Martin-Gago et al., 2013
Fragments of a tethered ligandPAR1-4Embedded ImageGerszten et al., 1994
  • BB1, BB2, BB3, bombesin receptors; C3a, C5a1, C5a2, complement peptide receptors; CCK1, CCK2, cholecystokinin receptors; ETA, ETB, endothelin receptors; FPR1, FPR2, FPR3, N-formyl peptide receptors; GAL1, GAL2, GAL3, galanin receptors; GHSR, ghrelin receptor; GNRHR, gonadotropin-releasing hormone receptor; MC5, melanocyte-stimulating hormone receptor; MCH1, MCH2, melanin-concentrating hormone receptors; MLNR, motilin receptor; NPBW1, NPBW2, neuropeptide B/W receptors; NPFF1, NPFF2, neuropeptide FF receptor; NPSR1, neuropeptide S receptor; PrRP, prolactin-releasing peptide receptor; QRFP, pyroglutamylated RFamide peptide receptor; SST1, SST2, SST3, SST4, SST5, somatostatin receptors; TRH1, thyrotropin-releasing hormone receptor; UT, urotensin receptor; V1A, V1B, V2, vasopressin receptors.