Search bioRxiv⌕ Search

Biology subjects

Bley, N.

Publications and source records attributed to Bley, N..

5 recordsLinked to original sources

Targeting IGF2BP1 Creates a Mitotic Vulnerability in Colorectal Carcinoma

Background Mitotic dysregulation is a common feature of colorectal cancer (CRC), yet the contribution of post-transcriptional mechanisms remain incompletely understood. We investigated how the oncofetal RNA-binding protein IGF2BP1 supports mitotic integrity and exposes therapeutic vulnerabilities in CRC. Methods We integrated patient cohort analyses with genetic and pharmacological perturbation of IGF2BP1, transcriptomics, proteomics, RNA-binding assays and functional studies. Xenografts assessed tumor formation, while BTYNB-paclitaxel responses were examined in CRC cell lines and patient-derived organoids. Results IGF2BP1 expression was elevated in CRC, increased with tumor stage, and associated with poor survival and proliferative gene signatures. Genetic depletion or pharmacological inhibition of IGF2BP1 impaired cell viability, induced mitotic abnormalities, and promoted apoptosis, whereas its re-expression enhanced tumor formation in vivo. Integrated molecular analyses identified the chromosomal passenger complex (CPC) as a previously unrecognized downstream target of IGF2BP1. IGF2BP1 bound transcripts encoding CPC components and its depletion consistently reduced their expression across multiple cancer cell models. BTYNB disrupted IGF2BP1 association with INCENP, CDCA8, and BIRC5 transcripts and accelerated INCENP mRNA decay. Functionally, INCENP depletion recapitulated the mitotic defects and impaired viability observed upon IGF2BP1 inhibition. Exploiting this mitotic vulnerability, BTYNB synergized with paclitaxel in CRC cell lines and across four independent IGF2BP1-positive patient-derived organoid models. Conclusions Our findings uncover an IGF2BP1-dependent post-transcriptional regulatory mechanism sustaining CPC expression and mitotic integrity in CRC. Targeting this mechanism exposes a therapeutically exploitable mitotic vulnerability and provides a rationale for combining IGF2BP1 inhibition with microtubule-targeting agents.

cancer biology↗

The long non-coding RNA FAM30A regulates the Musashi2-RUNX1 axis and is required for LSC function in AML cells

High expression of the long non-coding RNA (lncRNA) FAM30A has been previously associated with leukemic stem cell (LSC) activity and poor prognosis in both adult and paediatric acute myeloid leukaemia (AML) patients, yet it has not been functionally studied. This study provides the first cellular characterization of FAM30A focussing on an internal tandemly organised region, referred to as FAM30A repeats. FAM30A levels correlated with canonical AML LSC signatures and FAM30A depletion decreased cell viability as well as increased sensitivity to chemotherapeutics. It also inhibited colony formation, promoted granulocytic differentiation and abrogated leukemic engraftment in murine bone marrow in vivo. Overexpression of FAM30A repeats in this setting enhanced stemness, proliferation, chemoresistance, and engraftment thus highlighting the biological relevance of this region for LSC biology. On the molecular level, FAM30A repeats interact with the pro-LSC regulator Musashi-2 (MSI2), positively influencing expression of its targets including RUNX1 isoforms. We herein uncover that this FAM30A-MSI2-RUNX1 regulatory loop is of potential relevance for LSC maintenance in AML. These findings provide valuable insights into FAM30As cellular role and highlight its targeting potential for eliminating LSCs and improving treatment outcomes in AML patients.

cancer biology↗

RAVER1 interconnects lethal EMT and miR/RISC activity by the control of alternative splicing

The RAVER1 protein was proposed to serve as a co-factor in guiding the PTBP-dependent control of alternative splicing (AS). Whether RAVER1 solely acts in concert with PTBPs and how it affects cancer cell fate remained elusive. Here we provide the first comprehensive investigation of RAVER1-controlled AS in cancer cell models and reveal a pro-oncogenic role of RAVER1 in tumor growth. This unravels that RAVER1 guides AS in synergy with PTBPs but more prominently serves PTBP1-independent roles in splicing. In cancer cells, one major function of RAVER1 is the control of proliferation and apoptosis, which involves the modulation of AS events within the miR/RISC pathway. Associated with this regulatory role, RAVER1 antagonizes lethal, TGFB-driven epithelial-mesenchymal-transition (EMT) by limiting TGFB signaling. RAVER1-modulated splicing events affect the insertion of protein interaction modules in factors guiding miR/RISC-dependent gene silencing. Most prominently, in all three human TNRC6 proteins, RAVER1 controls AS of GW-enriched motifs, which are essential for AGO2-binding. Disturbance of RAVER1-guided AS events in TNRC6 proteins and other facilitators of miR/RISC activity compromise miR/RISC activity which is essential to restrict TGFB signaling and lethal EMT.

molecular biology↗

IGF2BP1 induces high-risk neuroblastoma and forms a druggable feedforward loop with MYCN promoting 17q oncogene expression

BackgroundNeuroblastoma is the most common solid tumor in infants accounting for approximately 15% of all cancer-related deaths. Over 50% of high-risk neuroblastoma relapse, emphasizing the need of novel drug targets and therapeutic strategies. In neuroblastoma, chromosomal gains at chromosome 17q, including IGF2BP1, and MYCN amplification at chromosome 2p are associated with adverse outcome. Recent, pre-clinical evidence indicates the feasibility of direct and indirect targeting of IGF2BP1 and MYCN in cancer treatment. MethodsCandidate oncogenes on 17q were identified by profiling the transcriptomic/genomic landscape of 100 human neuroblastoma samples and public gene essentiality data. Molecular mechanisms and gene expression profiles underlying the oncogenic and therapeutic target potential of the 17q oncogene IGF2BP1 and its cross-talk with MYCN were characterized and validated in human neuroblastoma cells, xenografts and PDX as well as novel IGF2BP1/MYCN transgene mouse models. ResultsWe reveal a novel, druggable feedforward loop of IGF2BP1 (17q) and MYCN (2p) in high-risk neuroblastoma. This promotes 2p/17q chromosomal gains and unleashes an oncogene storm resulting in fostered expression of 17q oncogenes like BIRC5 (survivin). Conditional, sympatho- adrenal transgene expression of IGF2BP1 induces neuroblastoma at a 100% incidence. IGF2BP1- driven malignancies are reminiscent to human high-risk neuroblastoma, including 2p/17q-syntenic chromosomal gains and upregulation of Mycn, Birc5, as well as key neuroblastoma circuit factors like Phox2b. Co-expression of IGF2BP1/MYCN reduces disease latency and survival probability by fostering oncogene expression. Combined inhibition of IGF2BP1 by BTYNB, MYCN by BRD inhibitors or BIRC5 by YM-155 is beneficial in vitro and, for BTYNB, also in vivo. ConclusionWe reveal a novel, druggable neuroblastoma oncogene circuit settling on strong, transcriptional/post-transcriptional synergy of MYCN and IGF2BP1. MYCN/IGF2BP1 feed-forward regulation promotes an oncogene storm harboring high therapeutic potential for combined, targeted inhibition of IGF2BP1, MYCN expression and MYCN/IGF2BP1-effectors like BIRC5.

cancer biology↗

IGF2BP1 is a targetable SRC/MAPK-dependent driver of invasive growth in ovarian cancer

Epithelial-to-mesenchymal transition (EMT) is a hallmark of aggressive, mesenchymal-like high-grade serous ovarian carcinoma (HG-SOC). The SRC kinase is a key driver of cancer-associated EMT promoting adherens junction (AJ) disassembly by phosphorylation-driven internalization and degradation of AJ proteins. Here we show, that the IGF2 mRNA binding protein 1 (IGF2BP1) is up-regulated in mesenchymal-like HG-SOC and promotes SRC activation by a previously unknown protein-ligand-induced, but RNA-independent mechanism. IGF2BP1-driven invasive growth of ovarian cancer cells essentially relies on the SRC-dependent disassembly of AJs. Concomitantly, IGF2BP1 enhances ERK2 expression in a RNA-binding dependent manner. Together this reveals a post-transcriptional mechanism of interconnected stimulation of SRC/ERK signaling in ovarian cancer cells. The IGF2BP1-SRC/ERK2 axis is targetable by the SRC-inhibitor saracatinib and MEK-inhibitor selumetinib. However, due to IGF2BP1-directed stimulation only combinatorial treatment effectively overcomes the IGF2BP1-promoted invasive growth in 3D culture conditions as well as intraperitoneal mouse models. In conclusion, we reveal an unexpected role of IGF2BP1 in enhancing SRC/MAPK-driven invasive growth of ovarian cancer cells. This provides a rational for the therapeutic benefit of combinatorial SRC/MEK inhibition in mesenchymal-like HG-SOC. Graphical Abstract O_FIG_DISPLAY_L [Figure 1] M_FIG_DISPLAY C_FIG_DISPLAY

cancer biology↗