FSCN1 as a new druggable target in adrenocortical carcinoma.
Carmen RuggieroMariangela TamburelloElisa RossiniSilvia ZiniNelly DurandGiulia CantiniFrancesca CioppiConstanze HantelKatja Kiseljak-VassiliadesMargaret E WiermanLaura-Sophie LandwehrIsabel WeigandMax KurlbaumDaniela ZizioliAndrei TurtoiShengyu YangAlfredo BerrutiMichaela LuconiSandra SigalaEnzo LalliPublished in: International journal of cancer (2023)
Adrenocortical carcinoma (ACC) is a rare endocrine malignancy with a high risk of relapse and metastatic spread. The actin-bundling protein fascin (FSCN1) is overexpressed in aggressive ACC and represents a reliable prognostic indicator. FSCN1 has been shown to synergize with VAV2, a guanine nucleotide exchange factor for the Rho/Rac GTPase family, to enhance the invasion properties of ACC cancer cells. Based on those results, we investigated the effects of FSCN1 inactivation by CRISPR/Cas9 or pharmacological blockade on the invasive properties of ACC cells, both in vitro and in an in vivo metastatic ACC zebrafish model. Here, we showed that FSCN1 is a transcriptional target for β-catenin in H295R ACC cells and that its inactivation resulted in defects in cell attachment and proliferation. FSCN1 knock-out modulated the expression of genes involved in cytoskeleton dynamics and cell adhesion. When Steroidogenic Factor-1 (SF-1) dosage was upregulated in H295R cells, activating their invasive capacities, FSCN1 knock-out reduced the number of filopodia, lamellipodia/ruffles and focal adhesions, while decreasing cell invasion in Matrigel. Similar effects were produced by the FSCN1 inhibitor G2-044, which also diminished the invasion of other ACC cell lines expressing lower levels of FSCN1 than H295R. In the zebrafish model, metastases formation was significantly reduced in FSCN1 knock-out cells and G2-044 significantly reduced the number of metastases formed by ACC cells. Our results indicate that FSCN1 is a new druggable target for ACC and provide the rationale for future clinical trials with FSCN1 inhibitors in patients with ACC.
Keyphrases
- induced apoptosis
- cell cycle arrest
- clinical trial
- crispr cas
- signaling pathway
- squamous cell carcinoma
- small cell lung cancer
- poor prognosis
- cell death
- gene expression
- randomized controlled trial
- bone marrow
- cell migration
- oxidative stress
- amino acid
- genome editing
- high resolution
- small molecule
- binding protein
- placebo controlled
- wild type