Definition

An orally bioavailable inhibitor of mitogen-activated protein (MAP) kinase-activated protein kinase 2 (MAPKAPK2; MK2), with potential antineoplastic and chemosensitization activities. Upon oral administration, MK2 inhibitor ATI-2231 targets and binds to the p38MAPK-MK2 complex, thereby inhibiting the p38MAPK phosphorylation and activation of MK2. This inhibits p38MAPK/MK2-mediated signaling pathway, and abrogates the repair of damaged DNA. This may lead to an accumulation of damaged DNA, inhibition of cell cycle arrest, and induction of apoptosis, and may potentiate the cytotoxicity of DNA-damaging agents. MK2, a cell cycle checkpoint kinase, plays an important role in DNA repair.