Background:

α-Amyloid Precursor Protein Modulator is a benzolactam derived PKC activator.

Protein kinase C (PKC) belongs to a family of protein kinase enzymes involved in phosphorylating serine and threonine of other proteins. The PKC enzymes have been involved in regulating the function of other proteins. Protein kinase C plays an important role in several signal transduction cascades. Protein kinase C has been involved in modulating membrane structure events, mediating immune responses, regulating transcription, learning and memory, and regulating cell growth [2].

α-Amyloid Precursor Protein Modulator activated PKC with the Ki value of 11.9 nM for PKCα that efficiently enhanced non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848. α-Amyloid Precursor Protein Modulator displayed a marked loss of tumor promoting activity [1].

参考文献:
[1] Kozikowski A P, Nowak I, Petukhov P A, et al.  New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPα[J]. Journal of medicinal chemistry, 2003, 46(3): 364-373.
[2] Stabel S, Parker P J.  Protein kinase C[J]. Pharmacology & therapeutics, 1991, 51(1): 71-95.