Table 1.
ECL2 ‘hot-spot’ residues of family A GPCRs interacting with bound ligand
| ECL2 residues interacting with ligand | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Receptor | Ligand | C − 3 | C − 2 | C − 1 | C0 | C + 1 | C + 2 | C + 3 | C + 4 |
| rhodopsin | 11-cis-retinal | Ser186 | Gly188 | Ile189 | Tyr191 | ||||
| β1AR | cyanopindolol | Phe201 | Thr203 | ||||||
| β2AR | carazolol | Phe193 | |||||||
| A2AR | ZM241385 | Phe168 | Glu169 | ||||||
| D3R | eticlopride | Ile183 | |||||||
| CXCR4 | IT1t | Arg183 | Ile185 | Cys186 | Asp187 | ||||
| CXCR4 | CVX15 | Asp187 | Arg188 | Tyr190 | |||||
ECL2 residues forming interactions with the named ligand are cited by their residue number for each receptor listed (Palczewski et al., 2000; Li et al., 2004; Cherezov et al., 2007; Jaakola et al., 2008; Warne et al., 2008; Chien et al., 2010; Wu et al., 2010). ECL2 residue nomenclature (C + 1, C + 2 etc.) uses a standard nomenclature in which the ECL2 Cys forming the well-conserved disulfide bond to TM3 is designated as the reference residue C0 (see text for details).