What are ERK inhibitors?

What are ERK inhibitors?

ERK1 and ERK2 (also known as MAPK3 and MAPK1) are 44 and 42 kDa Ser/Thr kinases, respectively. They are part of the Ras-Raf-ERK signal transduction cascade often found downstream of growth factor receptor activation.

Is Ulixertinib FDA approved?

xCures recently announced that the FDA granted its IND immediate Expanded Access Program for the ERK inhibitor ulixertinib to treat patients with MAPK pathway aberrant cancer.

What is p38 MAPK?

p38 mitogen-activated protein kinases are a class of mitogen-activated protein kinases (MAPKs) that are responsive to stress stimuli, such as cytokines, ultraviolet irradiation, heat shock, and osmotic shock, and are involved in cell differentiation, apoptosis and autophagy.

Is MEK inhibitor 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.

Is ERK a protein?

RAF, and ERK (also known as MAPK) are both serine/threonine-selective protein kinases. MEK is a serine/tyrosine/threonine kinase.

What type of protein is p38?

p38 proteins are a class of mitogen-activated protein kinases (MAPKs) that are major players during inflammatory responses, especially in macrophages. p38, also called RK or cytokinin-specific binding protein (CSBP), was identified in 1994 and is the mammalian ortholog of the yeast Hog1p MAP kinase [14].

What is Mirdametinib?

Mirdametinib (PD-0325901) is an orally delivered, highly selective small-molecule inhibitor of the dual specificity kinases, MEK1 and MEK2 (MAPK/ERK Kinase) which prevents the phosphorylation and subsequent activation of mitogen-activated protein kinase (MAPK).

Which is the first ERK inhibitor for cancer?

In this issue of Cancer Discovery, Sullivan and colleagues report on the phase I clinical trial of the ERK inhibitor ulixertinib and provide the first clinical evidence that ERK inhibitors are active against cancers harboring diverse BRAF mutations, as well as melanomas with BRAF–MEK inhibitor resistance ( 4 ).

Are there any clinical trials for Akt / ERK inhibitors?

Akt / ERK inhibitor ONC201 may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. This phase I trial studies the side effects of ONC 201 as maintenance therapy in treating patients with acute myeloid leukemia or myelodysplastic syndrome after receiving a donor stem cell transplant.

What are the side effects of ERK inhibitors?

To date, common adverse events associated with ERK inhibitors include diarrhea, nausea, fatigue, and rash. ERK inhibitors have demonstrated preliminary antitumor activity and may be most effective against cancers with RAS, RAF, or MAPK pathway alterations.

Are there any drugs that block ERK signaling?

Among them, BAY 43-9006 (Raf inhibitor), and PD184352, PD0325901 and ARRY-142886 (MEK1/2 inhibitors) have reached the clinical trial stage.