Christopher G Parker, Christian A Kuttruff, Andrea Galmozzi, Lars Jørgensen, Chien-Hung Yeh, Daniel J Hermanson, Yujia Wang, Marta Artola, Steven J McKerrall, Christopher M Josyln, Bjarne Nørremark, Georg Dünstl, Jakob Felding, Enrique Saez, Phil S Baran, Benjamin F Cravatt
The diterpenoid ester ingenol mebutate (IngMeb) is the active ingredient in the topical drug Picato, a first-in-class treatment for the precancerous skin condition actinic keratosis. IngMeb is proposed to exert its therapeutic effects through a dual mode of action involving (i) induction of cell death that is associated with mitochondrial dysfunction followed by (ii) stimulation of a local inflammatory response, at least partially driven by protein kinase C (PKC) activation. Although this therapeutic model has been well characterized, the complete set of molecular targets responsible for mediating IngMeb activity remains ill-defined...
December 27, 2017: ACS Central Science