Table 1.
PKC-θ inhibitor in human diseases and clinical trials.
| Mechanism of inhibition | Potential drug | Target | Disease treatment | Clinical trial |
|---|---|---|---|---|
| ATP competitor | Sotrastaurin (AEB071) | cPKCs: PKC-α and PKC-β and nPKCs: PKC-θ, PKC-δ, PKC-ϵ, PKC-η | Psoriasis, renal transplantation, uveal melanoma, and large B-cell lymphoma. | phase I and phase II |
| R524 | PKC-θ and PKC-α | GvHD | N/A | |
| Enzastaurin (Ly317615) | PKC-θ and PKC-β | Multiple myeloma, large B-cell lymphoma, maybe GvHD | phase II | |
| Compound C20 (C20) | PKC-θ | Rheumatoid arthritis (RA) | N/A | |
| Compound C27 (C27) | PKC-θ | N/A | N/A | |
| Phosphorylation inhibitor | 4-hydroxy-3-methoxycinnamaldehyde (4H3MC) | PKC-α, PKC-θ, and PKCs/λ | Maybe in T cell-mediated immune diseases | N/A |
| CGX1079 and CGX0471 | PKC-θ’s T538 phosphorylation | HIV infection | N/A | |
| Nuclear translocation inhibitor | N/A | PKC-θ | N/A | N/A |