Table I.
Crystal structures of GPCRs.
| Receptor | Engineereda | Ligand Typeb | Ligand | Year | Ref | PDB ID (resolution, Å) |
|---|---|---|---|---|---|---|
| A2A Adenosine A2AAR (HUMAN) | ICL3 fusion | IAG | ZM241385 | 2008 | [15] | 3EML (2.6) |
| AGO* | UK-432097 | 2011 | [47] | 3QAK (2.71) | ||
| Point mutations | AGO* | Adenosine | 2011 | [29] | 2YDO (3.0) | |
| NECA | 2YDV (2.6) | |||||
| ANT | ZM241385 | 2011 | [77] | 3PWH (3.30) | ||
| caffeine | 2011 | 3REY (3.31) | ||||
| IAG | ZM241385 | 2011 | 3RFM (3.60) | |||
| β1 Adrenergic β1AR (TURKEY) | Point mutations, partial ICL3 deletion | IAG | Cyanopindolol | 2008 | [14] | 2VT4 (2.7) |
| PAG | Dobutamine | 2011 | [78] | 2Y00 (2.5), 2Y01 (2.6) | ||
| AGO | Carmoterol | 2Y02 (2.6) | ||||
| AGO | Isoprenaline | 2Y03 (2.85) | ||||
| PAG | Salbutamol | 2Y04 (3.05) | ||||
| IAG | Carazolol | 2011 | [61] | 2YCW (3.0) | ||
| Cyanopindolol | 2YCX (3.25), 2YCY (3.15), 2YCZ (3.65) | |||||
| β2 Adrenergic β2AR (HUMAN) | ICL3 fusion | IAG | Not Resolved + Fabd | 2007 | [13] | 2R4R (3.4), 2R4S (3.4) |
| IAG | Carazolol | 2007 | [11, 12] | 2RH1 (2.4) | ||
| IAG | Timolol | 2008 | [23] | 3D4S (2.8) | ||
| IAG | ICI118551 | 2010 | [24] | 3NY8 (2.84) | ||
| IAG | Compd #1[44] | 3NY9 (2.84) | ||||
| ANT | Alprenolol | 3NYA (3.16) | ||||
| IAG | Not Resolved + Fabd | 2010 | [79] | 3KJ6 (3.4) | ||
| AGO* | BI-167107 +Nanobodye | 2011 | [26] | 3P0G (3.5) | ||
| AGO | FAUC50c | 2011 | [80] | 3PDS (3.5) | ||
| N-term fusion | AGO* | BI-167107 + Gαβγ + nanobody | 2011 | [25] | 3SN6 (3.2) | |
| Chemokine CXCR4 (HUMAN) | ICL3 fusion | ANT | IT1t | 2010 | [16] | 3ODU (2.5), 3OE6 (3.2), 3OE8 (3.1), 3OE9 (3.1) |
| ANT | CVX15 peptide | 3OE0 (2.9) | ||||
| Dopamine D3R (HUMAN) | ICL3 fusion | ANT | Eticlopride | 2010 | [17] | 3PBL (2.89) |
| Histamine H1R (HUMAN) | ICL3 fusion | IAG | Doxepin | 2011 | [18] | 3RZE (3.1) |
| Rhodopsin (BOVINE) | IAG | 11-cis retinalc | 2000 2004 |
[9]f [81] |
1F88 (2.8) 1U19 (2.2) 1GZM (2.65), L9H (2.6), 1HZX (2.8), 2I35(3.8), 2I36(4.), 2I37 (4.), 2J4Y(3.4), 3C9L(2.65), 3C9M (3.4), 3OAX (2.6) |
|
| 9-cis retinalc | 2007 | [82] | 2PED (2.95) | |||
| AGO | All-trans retinalc | 2006 | [83] | 2G87 (2.6), 2HPY (2.8) | ||
| E113Q | AGO* | All-trans retinalc +GαPeptidee | 2011 | [48] | 2X72 (3.0) | |
| 2011 | [49] | 3PQR (2.85), 3PXO (3.0) | ||||
| Opsin (BOVINE) | APO* | 2008 | [50] | 3CAP (2.9) | ||
| APO* | GαPeptidee | 2008 | [51] | 3DQB (3.2) | ||
| Rhodopsin (SQUID) | IAG | 11-cis retinalc | 2008 | [84] | 2ZIY (3.7) | |
| 2008 | [85] | 2Z73 (2.5) |
a
All non-rhodopsin GPCRs have truncated/modified N and C-termini
b
Co-crystallized ligand types: IAG inverse agonist, , ANT-antagonist, AGO – agonist, PAG – partial agonist, APO – no ligand.
c
Covalently bound ligand
d
Monoclonal antibody assisted crystallization
e
G-protein mimic, bound on the intracellular side
f
For the dark state bRho, only the references for the first and the highest resolution structures are shown.
*
Activated form of receptor