Wheelan Justin, Spigelman Melissa, Cirinelli Angelo, Reilly James, Molina Carlos A
Department of Biology, Montclair State University, Montclair, NJ 07043,USA.
Biol Open. 2025 Aug 15;14(8). doi: 10.1242/bio.061904. Epub 2025 Aug 14.
Melanoma, the most lethal form of skin cancer, is commonly associated with mutations in the BRAF gene, particularly BRAFV600E, which drives tumor proliferation via the ERK1/2 signaling cascade. While BRAF inhibitors initially demonstrate efficacy, therapeutic resistance remains a significant challenge. Emerging evidence implicates the cAMP signaling pathway, particularly the cAMP response element-binding protein (CREB) and its repressor, inducible cAMP early repressor (ICER), in melanoma progression and drug resistance. ICER, a transcriptional repressor regulated via Ras/MAPK-mediated phosphorylation and ubiquitination, is degraded in melanoma, undermining its tumor-suppressive role. In a brafV600E; p53 (loss of function) transgenic zebrafish (Danio rerio) model, we investigated the role of a ubiquitin-resistant ICER mutant (S35-41A-ICER) in tumor progression. Transgenic fish expressing S35-41A-ICER exhibited extended survival and reduced tumor invasiveness compared to wild-type ICER. RNA sequencing revealed dysregulation of CREB/CREM targets and compensatory pathways, including Rap1 and PI3K/AKT signaling, as well as candidate gene targets of ICER regulation, including the protein kinase A catalytic subunit prkacaa. Our findings suggest that a ubiquitin resistant ICER mitigates melanoma progression and represses oncogenic pathways in a brafV600E melanoma context.
黑色素瘤是皮肤癌中最致命的一种,通常与BRAF基因的突变有关,尤其是BRAFV600E,它通过ERK1/2信号级联驱动肿瘤增殖。虽然BRAF抑制剂最初显示出疗效,但治疗耐药性仍然是一个重大挑战。新出现的证据表明,cAMP信号通路,特别是cAMP反应元件结合蛋白(CREB)及其阻遏物——诱导型cAMP早期阻遏物(ICER),在黑色素瘤进展和耐药性中发挥作用。ICER是一种通过Ras/MAPK介导的磷酸化和泛素化进行调控的转录阻遏物,在黑色素瘤中会降解,从而削弱其肿瘤抑制作用。在一个brafV600E;p53(功能缺失)转基因斑马鱼(Danio rerio)模型中,我们研究了泛素抗性ICER突变体(S35 - 41A - ICER)在肿瘤进展中的作用。与野生型ICER相比,表达S35 - 41A - ICER的转基因鱼生存期延长,肿瘤侵袭性降低。RNA测序揭示了CREB/CREM靶点和补偿通路的失调,包括Rap1和PI3K/AKT信号通路,以及ICER调控的候选基因靶点,包括蛋白激酶A催化亚基prkacaa。我们的研究结果表明,在brafV600E黑色素瘤背景下,泛素抗性ICER可减轻黑色素瘤进展并抑制致癌通路。