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Fabbri, L.

Publications and source records attributed to Fabbri, L..

2 recordsLinked to original sources

RNA promotes MAPK signaling through direct interaction with BRAF

RNAs are increasingly recognized as direct regulators of protein function, yet whether RNA can control the activation of signaling kinases remains poorly understood. Here we identify RNA as a direct regulator of BRAF, a central kinase in the RAS-RAF-MEK-ERK (MAPK) pathway. Using complementary crosslinking and RNA-protein interaction approaches, we show that BRAF directly binds RNA in cells and that this interaction is enhanced upon MAPK pathway activation. Depletion of intracellular RNA reduces BRAF:CRAF complex assembly and impairs MEK1/2 phosphorylation, indicating that RNA contributes to RAF complex formation and MAPK signal transduction. We identify a positively charged surface within the BRAF kinase domain that mediates RNA binding. A separation-of-function RNA-binding mutant selectively attenuates BRAF-dependent MEK1/2 phosphorylation, demonstrating that RNA binding is required for efficient MAPK signaling. Moreover, artificial recruitment of the RNA-binding-deficient BRAF mutant to an RNA scaffold restores its signaling activity, supporting a direct role for RNA-mediated BRAF complex assembly. These data identify RNA as an active component of RAF kinase regulation and establish RNA-protein interactions as an additional determinant of MAPK pathway activation.

molecular biology↗

Selective mRNA translation determines adaptative mutability of melanoma cells to anti-BRAF/MEK combination therapy

During their inevitable evolution towards acquired resistance to anti-cancer targeted therapies, cancer cells adopt distinct gene expression profiles that allow them to transiently adapt to and tolerate the treatment. Similar to bacterial cells that transiently tolerate antibiotics, cancer cells surviving therapy can increase their mutation rate, enhancing the likelihood of acquiring resistance-conferring mutations and evolving into resistant cells. This adaptive mutability has been linked to transcriptional reprogramming of DNA damage repair mechanisms and effective therapeutic strategies to target such mechanisms are currently lacking. Here we show that translational control mediates the adaptive mutability of melanoma drug-tolerant cells by regulating the translation of the error-prone non-homologous end joining (NHEJ) component 53BP1. The specific inhibition of 5UTR-driven 53BP1 mRNA translation was sufficient to impair NHEJ and mutability. We found that the eIF4A RNA helicase, a key component of the eIF4F translation complex, regulates 53BP1 mRNA translation. Consequently, targeting the eIF4A with two small molecule inhibitors significantly delays the acquisition of resistance to combination of BRAF and MEK inhibitors (BRAFi/MEKi) in BRAFV600-mutant melanoma xenograft models and cell lines by reducing the mutability of drug-tolerant cells. Our results demonstrate that a standard-of-care therapy for melanoma, by engaging non-genetic adaptation driven at the translational level, contributes to the evolution of drug-tolerant melanoma cells toward acquired resistance.

cancer biology↗