Genomic profiling shows that many solid tumors are characterized by specific driver
aberrations, and this has expanded the therapeutic options for many patients. The mitogen …

Highlights•BRAF alterations lead to unbridled activation of the MAPK pathway which can
result in cancer development and progression.•BRAF and MEK inhibitors led to paradigm …

The discovery of BRAF mutations in melanoma has not yet translated into clinical success,
suggesting that BRAF/MEK inhibitors will need to be combined with other agents. In the …

Background Resistance to therapy with BRAF kinase inhibitors is associated with
reactivation of the mitogen-activated protein kinase (MAPK) pathway. To address this …

Abstract The RAS–RAF–MEK–ERK signaling cascade is among the most frequently mutated
pathways in human cancer. Approximately 50% of melanoma patients possess a druggable …

Selective BRAF inhibitors have now been established as a standard of care option for
patients diagnosed with metastatic melanoma whose tumors carry a BRAF mutation. Their …

Mitogen-activated protein kinase (MAPK) activation is a common property of human cancers
and is often due to activating mutations in the BRAF and RAS genes. BRAF kinase domain …

The discovery of activating BRAF mutations in melanomas has led to the investigation of
small molecular inhibitors targeting BRAF mutation and MEK, a downstream protein within …

With the identification of activating mutations in BRAF across a wide variety of malignancies,
substantial effort was placed in designing safe and effective therapeutic strategies to target …

Activating BRAF mutations, leading to constitutive activation of the MAPK signaling pathway,
are common in a variety of human cancers. Several small molecule BRAF inhibitors have …