IndraLab

Statements

BRAF bound to RAF1 activates ERK. 5 / 5
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"A recent study reported that a subset of MEK inhibitors that are inactive in RAS-mutant cancers (AZD6244, GDC-0973) promotes BRAF and CRAF heterodimer formation allowing feedback activation of MEK and ERK, whereas RAS active MEK inhibitors (GDC-0623, G-573) stabilize a nonproductive RAF and MEK complex preventing MEK feedback activation."
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"Interestingly, this version of BRAF still bound to CRAF, indicating that it is not drug binding per se, but inhibition of BRAF activity, that drives BRAF binding to CRAF and paradoxical activation of MEK and ERK."
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"Studies of RAF inhibitors in cancer led to the discovery of complex compensatory interactions between BRAF and RAF1 that drive a paradoxical increase in ERK1/2 activation [112,113,114]."
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"Biochemical analysis further revealed that addition of RGS to HeLa cells inhibits the heterodimerization of c-Raf and B-Raf, thereby inhibiting the activation of MEK and ERK pathway."
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"Targeting MEK downstream of BRAF and CRAF heterodimers using PD0325901 subsequent to RAF inhibitor treatment reduced ERK1/2 rebound and simultaneous treatment of tumor xenografts with both RAF and MEK inhibitors led to more pronounced tumor growth inhibition than either treatment alone."
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