Table 1 Cryo-EM structures of small (<100 kDa) apo/inactive-state GPCRs
From: Strategic advances for cryo-EM structural studies of small (<100 kDa) GPCRs
S. no. | Membrane protein (GPCRs) | Antagonist/ inverse agonist | Fusion protein | Organism | M.W. (GPCR) KDa | Resolution (Å) | PDB ID | References |
|---|---|---|---|---|---|---|---|---|
1. | ADGRE5 (Adhesion receptor) | Apo | BRIL | Escherichia coli | 92 | 3.2 | 8IKJ | |
2. | Β2AR (Adrenoreceptor) | CHEMBL1160734 (Antagonist) | BRIL | Escherichia coli | 46 | 3.4 | 8JJO | |
3. | A2AR (Adenosine receptor) | ZM-241385 (Antagonist) | BRIL | Escherichia coli | 45 | 3.4 | 7T32 | |
4. | GPRC5D (Orphan receptor) | Apo | BRIL | Escherichia coli | 39 | 3.4 | 8YZK | |
5. | OR52E4 (Odorant receptor) | Apo | BRIL | Escherichia coli | 35 | 3.6 | 8W77 | |
6. | HRH1 (Histamine receptor) | Astemizole (Antagonist) | BRIL | Escherichia coli | 56 | 3.0 | 8X5Y | |
7. | ETA (Endothelin receptor) | Zibotentan (Antagonist) | BRIL, Anti-BRIL Fab | Escherichia coli, Homo sapiens | 49 | 3.2 | 8XVL | |
8. | CCR6 (Chemokine receptor) | OXM2 (Antagonist) | BRIL, Anti-BRIL Fab | Escherichia coli, Homo sapiens | 43 | 3.0 | 9D3E | |
9. | AT1 (Angiotensin receptor) | AT118-H Nanobody (Antagonist) | BRIL, Anti-BRIL Fab | Escherichia coli, Synthetic construct | 41 | 3.0 | 8TH3 | |
10. | MCHR1 (Melanin-concentrating hormone receptor) | CHEMBL242004 (Antagonist) | BRIL, Antibody Fab chain | Escherichia coli, Synthetic construct | 39 | 3.4 | 8YNT | |
11. | FZD5 (Frizzled receptor) | Apo | BRIL, Anti-BRIL Fab, Anti-Fab nanobody | Escherichia coli, Homo sapiens, Synthetic construct | 65 | 3.7 | 6WW2 | |
12. | CXCR3 (Chemokine receptor) | AMG487 (Antagonist) | BRIL, Nanobody-6 | Escherichia coli, Lama glama | 41 | 3.0 | 8K2W | |
13. | SMO (Frizzled receptor) | Apo* | PGS | Pyrococcus abyssi GE5 | 87 | 3.7 | 8CXO | |
14. | CNR1 (Cannabinoid receptor) | MRI-1891 (Inverse agonist) | PGS | Pyrococcus abyssi GE5 | 53 | 3.1 | 9BA0 | |
15. | ETB (Endothelin receptor) | Apo | Calcineurin | Homo sapiens | 50 | 3.3 | 9KDG | |
16. | β2AR (Adrenoreceptor) | Carazolol (Inverse agonist) | Calcineurin | Homo sapiens | 46 | 3.5 | 9CHX | |
17. | ADA1A (Adrenoreceptor) | Tamsulosin (Antagonist) | Nanobody-6 | Lama glama | 51 | 3.4 | 7YMJ | |
18. | CXCR3 (Chemokine receptor) | CHEMBL1921858 (Antagonist) | Nanobody-6 | Lama glama | 41 | 3.6 | 8HNN | |
19. | OPRM (μ Opioid receptor) | Naloxone (Antagonist) | Nanobody-6 | Lama glama | 44 | 3.2 | 9BJK | |
20. | NTR1 (Neurotensin receptor) | SR-48692 (Inverse Agonist) | Nanobody-6 | Lama glama | 46 | 2.4 | 7UL2 | |
21. | SSR (Somatostatin receptor) | Apo | Nanobody-6 | Lama glama | 41 | 3.1 | 7UL5 | |
22. | HRH2 (Histamine receptor) | CHEMBL902 (Antagonist) | Nanobody-6M, NabFab | Synthetic construct | 40 | 3.0 | 7UL3 | |
23. | OPRM (μ Opioid receptor) | Alvimopan (Antagonist) | Megabody-6 | Synthetic construct | 44 | 2.8 | 7UL4 | |
24. | OPRM (μ opioid receptor) | Apo* | NabFab, Anti-Fab Nb | Synthetic construct, Lama glama | 44 | 3.2 | 8QOT | |
25. | CCR8 (Chemokine receptor) | mAb1 (Antagonist) | Fab | Oryctolagus cuniculus | 41 | 2.9 | 8TLM |
