Table 2.
“Non-PKC” phorbol ester/DAG receptors in cancer
| Class | Isotypes | Phorbol ester binding* | Activity | Roles in cancer |
|---|---|---|---|---|
|
| ||||
| Protein kinase D | PKD1 | + | Protein kinases | Diverse roles in promotion or suppression of tumorigenesis and metastasis, primarily in solid tumors |
| PKD2 | + | |||
| PKD3 | + | |||
|
| ||||
| RasGRP | RasGRP1 | + | Ras/Rap1 Guanine nucleotide Exchange Factors (GEFs) | Diverse roles in oncogenesis of blood cancers and solid tumors |
| RasGRP2 | − | |||
| RasGRP3 | + | |||
| RasGRP4 | + | |||
|
| ||||
| Chimaerin | α1-chimaerin | + | Rac GTPase Activating Proteins (GAPs) | Tumor suppression in glioma and breast cancer |
| α2-chimaerin | + | |||
| β1-chimaerin | + | |||
| β2-chimaerin | + | |||
| β3-chimaerin | + | |||
|
| ||||
| Munc-13 | Munc-13-1 | + | Coordination of vesicle docking, priming and fusion | Unknown |
| Munc-13-2 | ? | |||
| Munc-13-3 | ? | |||
| Munc-13-4 | ? | |||
|
| ||||
| Diacylglycerol-kinase | DGKα | − | Lipid kinases | Limited knowledge for phorbol ester-responsive DGKs |
| DGKβ | + | |||
| DGKγ | + | |||
| DGKδ | − | |||
| DGKε | − | |||
| DGKη | − | |||
| DGKκ | − | |||
| DGKθ | − | |||
| DGKι | − | |||
| DGKζ | − | |||
*
Not all DGKs have been examined for phorbol ester binding, but structural predictions on C1 domains suggest that other tan DGKβ and DGKγ all other DGKs should be insensitive to phorbol esters.