Protein kinase C epsilon (PKCε) (PKCε)

Protein kinase C epsilon (PKCε) is a member of the novel PKC subfamily of serine/threonine kinases, distinguished by its activation by diacylglycerol (DAG) and its independence from calcium ions [1]. It functions as a versatile signaling molecule involved in diverse cellular processes, including cell survival, migration, and neurotransmitter release [2]. In oncology, PKCε is frequently overexpressed and acts as a pro-oncogene, promoting tumor growth, invasion, and resistance to chemotherapy, which makes it a target for inhibitory strategies [3]. In contrast, in the field of neurology, the activation of PKCε is being investigated for its potential to treat Alzheimer's disease by enhancing synaptic repair and reducing the accumulation of amyloid-beta plaques [4]. Pharmacological modulation of this target is achieved through agents like bryostatin-1, which binds to the C1 domain, or isoform-specific peptides that interfere with its translocation to specific cellular compartments [5]. However, the development of PKCε-targeted therapies faces challenges such as achieving isoform selectivity and managing the potential for tumor promotion during chronic activation [6].

Other names

PRKCEnPKC-epsilonProtein kinase C epsilon typePKCE

Modulation of serine/threonine kinase activity through binding to the C1 domain (activators) or the catalytic domain (inhibitors) to regulate downstream signaling cascades.