SRSF protein kinase 3 (SRPK3)

SRSF protein kinase 3 (SRPK3) is a serine/threonine protein kinase that specifically phosphorylates serine residues within regions rich in arginine/serine dipeptides (RS domains) of splicing factors, most notably the SR protein family. SRPK3 is a member of the SRPK family, along with SRPK1 and SRPK2, and plays essential roles in regulating alternative splicing and muscle development. Unlike SRPK1 and SRPK2, which are established therapeutic targets, the pathogenic and therapeutic relevance of SRPK3 is still under investigation. Recent studies implicate SRPK3 in certain subtypes of breast cancer, particularly triple-negative breast cancer, where increased expression correlates with poor prognosis and proliferation dependency. Selective SRPK3 inhibitors (e.g., BP152) have demonstrated anti-proliferative activity in cancer cell models, highlighting the potential of SRPK3 as a novel drug target. However, a full mechanistic understanding and clinical validation are not yet established. SRPK3 mutations and dysregulation are also associated with congenital myopathies and intellectual developmental disorder, X-linked 114.

Other names

MSSK1STK23Muscle-specific serine kinase 1Serine/threonine-protein kinase 23Serine/arginine-rich protein-specific kinase 3SR-protein-specific kinase 3SFRS protein kinase 3

ATP-competitive inhibition of kinase activity; Blockade of phosphorylation of SR proteins alters splicing patterns and reduces cell proliferation (especially in breast cancer cell lines).