Therapeutics: Protein kinase C (PKC) α (PRKCA); PKC δ (PRKCD); PKC θ (PRKCQ)

In vitro studies have identified bryostatin-derived PKC modulators that could help treat cancer and other indications. Chemical synthesis and in vitro testing identified three bryostatin analogs that bound the PKC isoforms α, δ and θ with Ki values between 1.0 and 2.4 nM. Next steps include evaluating the PKC modulators and additional bryostatin-derived PKC modulators in cellular and animal models of disease.

Leo Pharma A/S markets the PKC modulator Picato ingenol mebutate gel (PEP005 topical) to treat actinic keratosis (AK) and has the gel in Phase II testing to treat basal cell carcinoma and cancer. ...