Protein kinase D1 (PRKD1) (PRKD1)

Protein kinase D1 (PRKD1) is a serine/threonine kinase that serves as a key effector in signaling pathways initiated by diacylglycerol (DAG) and protein kinase C (PKC) [UniProt: P23229]. It plays a fundamental role in regulating Golgi membrane trafficking, cell proliferation, and survival [PubMed: 24561057]. In the context of oncology, PRKD1 often acts as a tumor suppressor by maintaining the epithelial phenotype and inhibiting cell migration, particularly in breast and prostate cancers; however, it can promote growth in pancreatic cancer [PubMed: 20101025]. PRKD1 is also a critical mediator of cardiac hypertrophy and remodeling in response to stress [PubMed: 15618517]. While no PRKD1-targeted therapies are currently approved, small-molecule inhibitors like CRT0066101 are being investigated in preclinical models for their ability to suppress tumor growth and pathological cardiac changes [PubMed: 21828051]. The development of selective inhibitors is a primary focus to avoid off-target effects on related PKC isoforms.

Other names

PKD1Protein kinase C muPKC muPRKCMSerine/threonine-protein kinase D1

Small molecule inhibition of the catalytic kinase domain to block downstream phosphorylation and signaling pathways.