In recent times, we have demonstrated how a class of rare, naturally occurring products, namely oxyprenylated coumarins such as auraptene 1 and umbelliprenin 2 (Figure 1a,b) are able to exert valuable and promising pharmacological activities as neuroprotective, anti-cancer, and anti-inflammatory agents [6,7,8], and to act as effective modulators of lipid and sugar metabolism, being ligands of key receptors such as the farnesoid X receptor (FXR) [9], glucose transporter type 4 (GLUT 4) [10], and peroxisome proliferator-activated receptors (PPARs) [11]. This evidence concerns the gene NR1H4 and cancer.