TABLE 8.
Kokumi sensation receptor agonists, allosteric modulators with concentrations used in cell based assays.
| Agonist | Type/nature | Conc. (mM unless stated otherwise) | Binding pocket | References |
|---|---|---|---|---|
| Ca2+ | Orthosteric agonist/cation | 1 a | VFT | (Brown et al., 1993; Conigrave et al., 2000; Breitwieser, 2006) |
| Mg2+ | Orthosteric agonist/cation | 10 a | VFT | (Brown et al., 1993) |
| Gd3+ | Orthosteric agonist/cation | 0.02 a | VFT | (Brown et al., 1993) |
| Al3+ | Orthosteric agonist/cation | 0.5 | VFT | (Brown et al., 1993) |
| Sr2+ | Orthosteric agonist/cation | 0.5 | VFT | (Brown et al., 1993) |
| Mn2+ | Orthosteric agonist/cation | 0.5 | VFT | (Brown et al., 1993) |
| Ni2+ | Orthosteric agonist/cation | 0.5 | VFT | (Brown et al., 1993) |
| Ba2+ | Orthosteric agonist/cation | 0.2 | VFT | (Brown et al., 1993) |
| Spermine | Orthosteric agonist/polyamine | 0.15 a | VFT | Quinn et al., 1997) |
| Spermidine | Orthosteric agonist/polyamine | 0.002 a | VFT | (Nemeth et al., 2018) |
| Neomycin | Orthosteric agonist/aminoglycoside antibiotic | 0.06 a | VFT | (Katz et al., 1992) |
| Gentamicin | Orthosteric agonist/aminoglycoside antibiotic | 0.15 a | VFT | Katz et al., 1992) |
| Kanamycin | Orthosteric agonist/aminoglycoside antibiotic | 0.1 | VFT | (Katz et al., 1992) |
| Amyloid β-peptides | Orthosteric agonist/Peptide | 0.001–0.04 | — | (Ye et al., 1997) |
| Poly-Lysine | Orthosteric agonist/peptide | 0.03 µM a | VFT | (Brown et al., 1991; Nemeth et al., 2018) |
| Poly L-arginine | Orthosteric agonist/peptide | 0.004 µM a | VFT | Brown et al., 1991; Nemeth et al., 2018) |
| Lysozyme | Agonist/protein | 0.59 a | ND | (Yamamoto et al., 2020) |
| Thaumatin | Agonist/protein | 0.07 a | ND | (Yamamoto et al., 2020) |
| Aromatic L-amino acids (Trp, Phe, His, Ala, Ser) | PAMs | 10 | VFT | (Conigrave et al., 2000; Mun et al., 2004; Geng et al., 2016) |
| Anions (SO4 2-) | NAM | 10 | VFT | (Geng et al., 2016) |
| Cinacalcet | PAM/phenylalkylamine | 0.051 µM a | TMD | (Miedlich et al., 2002; Petrel et al., 2004; Nemeth et al., 2004) |
| Calindol | PAM/phenylalkylamine | 0.31 µM a | TMD | Miedlich et al., 2002; Petrel et al., 2004) |
| NPS R-568 | PAM/phenylalkylamine | 0.5 µM a | TMD | (Miedlich et al., 2002; Petrel et al., 2004) |
| NPS R-467 | PAM/phenylalkylamine | 0.01 | TMD | (Miedlich et al., 2002; Petrel et al., 2004) |
| γ-Glu-Val-Gly | PAM/Peptide | 0.041 µM a | — | (Ohsu et al., 2010) |
| γ-Glu-Cys-Gly (Glutathione) | PAM/Peptide | 76.5 µM a | VFT | (Ohsu et al., 2010; Wang et al., 2006 |
| γ-Glu-Ala | PAM/Peptide | 3.65 µM a | ND | (Wang et al., 2006; Ohsu et al., 2010) |
| γ -Glu-Val | PAM/Peptide | 1.34 µM a | ND | (Wang et al., 2006; Ohsu et al., 2010) |
| γ -Glu-Cys | PAM/Peptide | 0.45 µM a | VFT | (Ohsu et al., 2010; Wang et al., 2006) |
| γ -Glu-α-aminobutyryl-Gly (Opthalmic acid) | PAM/Peptide | 0.018 µM a | ND | (Ohsu et al., 2010) |
| NPS2143 | NAM | 0.0003 (IC50) | TMD | (Gowen et al., 2000; Petrel et al., 2004) |
| Calhex 231 | Mixed PAM/NAM | 0.1–1 µM (PAM); 3–10 µM (NAM) | TMD | (Petrel et al., 2003; Petrel et al., 2004; Gregory et al., 2018) |
Where VFT, venus flytrap domain; TMD, transmembrane domain; ND, not determined.
a
shows EC50 value.