Peptides binding to class A GPCRs with key regions important for activity
Peptide | Receptor | Sequence 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 Activity | Peptide Terminal End Inside the Helical Bundle | Reference |
---|---|---|---|---|---|
Angiotensin | AT1, AT2 | ![]() | -COOH | C-end | Rioux et al., 1975; Karnik 2000; Asada et al., 2018 |
Apelin | APLNR | ![]() | -COOH | C-end | Murza et al., 2012; Ma et al., 2017 |
Bradykinin | B1, B2 | ![]() | -COOH | C-end | Rhaleb et al., 1990; Jarnagin et al., 1996; Ha et al., 2006 |
Complement Peptides | ![]() | -COOH | C-end | Mollison et al., 1989; Higginbottom et al., 2005; Klos et al., 2013; Liu et al., 2018 | |
C3a | C3a | ||||
C5a | C5a1, C5a2 | ||||
Endothelin | ETA ETB | ![]() | -COOH | C-end | Rovero et al., 1990; Shihoya et al., 2016 |
Neurotensin | NTS1, NTS2 | ![]() | -COOH | C-end | Labbe-Jullie et al., 1998; White et al., 2012; Kleczkowska and Lipkowski, 2013) |
C-end of Chain B | Bathgate et al., 2013; Hu et al., 2017; Patil et al., 2017; Wong et al., 2018 | ||||
H2 relaxin | RXFP1 | ![]() | |||
Insulin-like peptide 3 (INSL3) | RXFP2 | ![]() ![]() | |||
H3 relaxin | RXFP3 | ![]() | C-end of Chain B | ||
INSL5 | RXFP4 | ![]() | C-end of chain B | ||
Cholecystokinin gastrin | CCK1 CCK2 | ![]() ![]() | -CONH2 | C-end | Morley et al., 1965; Jensen et al., 1982; Black and Kalindjian, 2002; Archer-Lahlou et al., 2005; Dufresne et al., 2006 |
Orexin | OX1, OX2 | ![]() | -CONH2 | C-end | Darker et al., 2001; Ammoun et al., 2003; Lang et al., 2004; Heifetz et al., 2013 |
Neuropeptide Y | NPY1, 2, 4, and 5 | ![]() | -CONH2 | C-end | Boublik et al., 1989; Xu et al., 2013, 2018; Yang et al., 2018 |
Prolactin-releasing peptide | PrRP | ![]() | -CONH2 | C-end | Boyle et al., 2005; Findeisen et al., 2011; Rathmann et al., 2012 |
Pyroglutamylated RFamide peptide | QRFP | ![]() | -CONH2 | C-end | Findeisen et al., 2011 |
Neuropeptide FF | NPFF1-2 | ![]() | -CONH2 | C-end | Findeisen et al., 2011 |
Metastin/kisspeptin | KISS1R | ![]() | -CONH2 | C-end | Kotani et al., 2001; Findeisen et al., 2011 |
Vasopressin | V1A, V1B, V2 | ![]() | -CONH2 | Cyclic end | Jard and Bockaert, 1975; Mouillac et al., 1995; Chini and Fanelli, 2000 |
Oxytocin | OT | ![]() | -CONH2 | Cyclic end | Jard and Bockaert, 1975; Chini and Fanelli, 2000; Gimpl and Fahrenholz, 2001 |
Neuromedin B | BB1 | ![]() | -CONH2 | C-end | Mervic et al., 1991; Lin et al., 1995; Jensen et al., 2008 |
Gastrin-relesing peptide | BB2 | ![]() | |||
Bombesin | BB3 | ![]() | |||
Neuromedin-U | NMU1-2 | ![]() | -CONH2 | C-end | Brighton et al., 2004; Kawai et al., 2014 |
Substance-P/K, neurokinin, tachykinin | NK1, NK2, NK3 | ![]() | -CONH2 | C-end | Couture et al., 1979; Ganjiwale et al., 2011 |
Neurokinin A | |||||
Neurokinin B | |||||
Thyrotropin-releasing hormone | TRH1 | ![]() | -CONH2 | All | Chang et al., 1971; Engel and Gershengorn, 2007 |
Opioid peptides endorphins | DOR, KOR, MOR, NOP | ![]() | H2N- | N-end | Morley 1983; Koehl et al., 2018 |
Neuropeptides B/W | NPBW1-2 | ![]() | N-end | Kanesaka et al., 2007 | |
Neuropeptide S | NPSR1 | ![]() | N-end | Roth et al., 2006 | |
N-formyl peptide | FPR1-3 | ![]() | O=HC-NH- | N-end | Prossnitz and Ye, 1997 |
Adrenocorticotropic hormone | MC1–5 | ![]() | O=HC-NH- | FRW | Schwyzer, 1977; Matsunaga et al., 1989; Schioth et al., 1997; Audinot et al., 2001; Haskell-Luevano et al., 2001 |
Melanocortins (α, β, and γ) | |||||
Motilin | MLNR | ![]() | N-end | Poitras et al., 1992; Xu et al., 2005 | |
Ghrelin | GHSR | ![]() | N-end | Charron et al., 2017 | |
Gonadotropin-releasing hormone | GNRHR | ![]() | CONHCHO- | N-end | Hoffmann et al., 2000; Padula, 2005; Barran et al., 2005 |
Galanin | GAL1-3 | ![]() | H2N- | N-end | Church et al., 2002; Lang et al., 2015 |
Urotensin | UT | ![]() | Cyclic portion | Labarrere et al., 2003; Merlino et al., 2013 | |
Melanin-concentrating hormone | MCH1-2 | ![]() | Cyclic portion | Matsunaga et al., 1989; Schioth et al., 1997; Audinot et al., 2001 | |
Somatostatin | SST1-5 | ![]() | Cyclic portion | Vale et al., 1978; Martin-Gago et al., 2013 | |
Fragments of a tethered ligand | PAR1-4 | ![]() | Gerszten 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.