Recombinant rat Cckbr is typically produced using heterologous expression systems:
Mammalian cells (e.g., COS-7, CHO): Enable proper post-translational modifications and ligand-binding functionality .
Baculovirus/insect cell systems: Used for large-scale production in structural studies .
Regulates gastric acid secretion and intestinal sodium absorption .
Mechanism: Activates phospholipase C (PLC) via Gq, increasing intracellular Ca²⁺ and inositol trisphosphate (IP₃) .
| Ligand | Receptor State | Kd (nM) | Source |
|---|---|---|---|
| Gastrin | High-affinity | 0.1–0.3 | |
| CCK-8 (sulfated) | Low-affinity | 2–5 | |
| L-365,260 (antagonist) | Inactive | 0.13 |
Colorectal cancer: Misspliced Cckbr variants correlate with tumor invasiveness .
Parkinson’s disease: CCKBR antagonism enhances L-DOPA efficacy in dopamine-depleted models .
Small-molecule antagonists: Reduce acid secretion in peptic ulcers .
Inverse agonists (e.g., L-740,093): Investigated for anxiety disorders .