What are ERK inhibitors?
What are ERK inhibitors?
ERK is a cell signal that is believed to drive the growth of many cancers. Merck started developing ERK inhibitors in 2013 to plug a gap in the treatment of melanomas and other cancers with BRAF mutations. Targeted treatments for these cancers are available, but patients often become resistant and their cancer returns.
What is ERK in cancer?
Therefore, ERK is associated with key cell cycle checkpoint proteins to induce cell cycle arrest, and serves a protective role in response to radiation cytotoxicity. Previous studies have demonstrated that ERK signaling serves a radioprotective role in cancer therapy and contributes to radioresistance (9,29,70).
What is ERK function?
ERK cascade plays a crucial role in multiple cellular processes such as cell proliferation, differentiation, adhesion, migration and survival. Therefore, it is essential for many physiological events including development, immunity, metabolism, and memory formation.
Does ERK cause cancer?
Due to the importance of the ERK cascade, ERK disorders are harmful to cells and ultimately to the body. Excessive activation of upstream proteins and kinases in the ERK pathway has been shown to induce various diseases, including cancer, inflammation, developmental disorders and neurological disorders (18–22).
Is ERK an oncogene?
Additionally, the Raf-MEK-ERK pathway is a key downstream effector of the Ras small GTPase, the most frequently mutated oncogene in human cancers.
Is ERK a MAP kinase?
Mitogen-activated ERK kinase, a family of seven human MAP kinase kinases, with dual specificity for tyrosine and serine/threonine residues. Components of four signaling pathways: ERK1/2 (MEK1/2), p38 (MEK3/6, and sometimes MEK4), JNK (MEK4/7), and ERK5 (MEK5). ERK1/2 are the only known substrates of MEK1/2.
Are MEK inhibitors chemotherapy?
A new class of chemotherapeutic agents, MEK inhibitors, has recently been developed and is proving to be an effective treatment for a number of cancers. A pattern of ocular adverse events has followed these drugs through clinical trials and their association with retinopathy is only just beginning to be recognized.