Explore MAPK

Understanding the MAPK pathway as it relates to oncology

The mitogen-activated protein kinase (MAPK) pathway plays a role in the regulation of gene expression, cellular growth, and survival.¹ Abnormal MAPK signaling may lead to increased or uncontrolled cell proliferation and resistance to apoptosis.²

Research into the MAPK pathway has shown it to be important in some cancers.² Based on these findings, we are investigating further ways to impact MAPK signaling.

The MAPK signaling pathway plays a role in the regulation of gene expression, cellular growth, and survival²

The mitogen-activated protein kinase (MAPK) pathway includes the signaling molecules Ras, Raf, MEK, and ERK. Normally, extracellular growth factors activate the pathway by binding to receptor tyrosine kinases. This mobilizes a cascade of signaling via the MAPK pathway signaling molecules. Ultimately, activation of the MAPK pathway leads to the transcription of genes that encode proteins involved in the regulation of essential cellular functions, such as cell growth, cell proliferation, and cell differentiation.^1,3

The MAPK signaling cascade—Ras, Raf, MEK, and ERK¹

First: MAPK signaling begins with the activation of the protein Ras by receptor tyrosine kinases.¹

Activated Ras causes the membrane recruitment and activation of Raf proteins.³

Then: Raf phosphorylates MEK, a separate protein kinase in the pathway.^1-3

Next: MEK phosphorylates ERK, which can directly and indirectly activate many transcription factors.^1,4

Finally: The activation of these transcription factors by ERK leads to the expression of genes encoding proteins that regulate cell proliferation and survival.^2,4