Mitogen-activated protein kinase 1 (MAPK1) (MAPK1)

Mitogen-activated protein kinase 1 (MAPK1), also known as ERK2, is a key serine/threonine kinase and the terminal effector of the Ras-Raf-MEK-ERK signaling cascade [1, 6]. It plays a fundamental role in transmitting extracellular signals from cell surface receptors to the nucleus, where it phosphorylates numerous transcription factors to regulate cell growth, proliferation, and survival [9, 10]. Dysregulation or hyperactivation of the ERK/MAPK pathway, often driven by mutations in upstream components like BRAF or KRAS, is a hallmark of many human cancers, including melanoma and colorectal carcinoma [13, 16]. Consequently, MAPK1 is a major therapeutic target, with several small-molecule inhibitors like ulixertinib in clinical development aimed at overcoming resistance to upstream pathway inhibitors [10, 14]. Beyond oncology, it is also implicated in developmental disorders such as Noonan syndrome and various inflammatory processes [2, 7].

Other names

ERK2Extracellular signal-regulated kinase 2P42MAPKPRKM1PRKM2ERT1MAP kinase 1MAP kinase 2

Inhibition of the kinase activity of ERK1/2, thereby blocking the phosphorylation of downstream cytoplasmic and nuclear substrates and interrupting the transmission of mitogenic signals.