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BRAF and MEK Inhibitors: Use and Resistance in BRAF-Mutated Cancers.


ABSTRACT: The mitogen activated protein kinase/extracellular signal-related kinase (MAPK/ERK) signaling pathway serves an integral role in growth, proliferation, differentiation, migration, and survival of all mammalian cells. Aberrant signaling of this pathway is often observed in several types of hematologic and solid malignancies. The most frequent insult to this signaling cascade, leading to its constitutive activation, is to the serine/threonine kinase rapidly accelerating fibrosarcoma (RAF). Considering this, the development and approval of various small-molecule inhibitors targeting the MAPK/ERK pathway has become a mainstay of treatment as either mono- or combination therapy in these cancers. Although effective initially, a major clinical barrier with these inhibitors is the relapse of patie

SUBMITTER: Sanchez JN 

PROVIDER: S-EPMC6080616 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature