Table 9.
CR3 as a potential therapeutic target.
| Ligand | Site on CR3 | Site on ligand | Function | |
|---|---|---|---|---|
| Imprime PGG | – | – | Activate anti-cancer innate immune effector functions | (153–156) |
| Gu-4 | Lectin binding site | Oligosaccharides | Inhibition of leukocyte adhesion and transendothelial migration | (297) |
| Hydroxyethyl starch | – | – | Reducing migration, and chemotaxis of activated PMN | (298) |
| Antagonists | ||||
| Abciximab | – | – | Blocking of different CR3 functions | (299) |
| Leumidin | – | Inhibition of neutrophil adhesion | (300, 301) | |
| Covalent small molecule | Inhibiting CR3:iC3b | – | Anti-inflammatory by reduced neutrophil emigration | (302) |
| Gupta group | Inhibited binding to fibrinogen, IC50 < 1 µM | – | – | (303) |
| XVA143 | Antagonists to the I-like domain, inhibiting binding of iC3b and ICAM-1, IC50 0.9 µM | – | – | (304) |
| Simvastatin | αMI (MIDAS) and other residues | Carboxylic acid | Inhibition of monocyte binding to iC3b | (48) |
| E/DDGW | Competes with MMP-9 | – | – | (204) |
| CP[CFLLGC]C | Divalent cation dependent, competes with ICAM-1, vWF and collagen | – | Inhibits leukocyte adhesion to ICAM-1 | (305) |
| GYRDGYAGPILYN | Competes with ICAM-1 | – | – | (306) |
| Agonists | ||||
| 2-thioxothiazolidin-4-one | Competing with DDGW peptide, enhanced binding of fibrinogen and proMMP-9 | – | – | (307) |
| Leukoadherins (LA-1/ADH-503) | EC50 10- 40 µM, increasing binding to fibrinogen | – | – | (34, 308–314) |