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2-Methoxyestradiol-3,17-IO/I,IO/I-bis-sulfamate Inhibits Proliferation and Invasion via Senescence Pathway Induction in Human BRAFi-Resistant Melanoma Cells

Franco, Ylana Adami ; de Moraes, Manoel Oliveira ; Carvalho, Larissa A. C ; Dohle, Wolfgang ; da Silva, Renaira Oliveira ; Noma, Isabella Harumi Yonehara ; Lima, Keli ; Potter, Barry V. L ; Machado-Neto, João A ; Maria-Engler, Silvya Stuchi

International journal of molecular sciences, 2023-07, Vol.24 (14) [Periódico revisado por pares]

MDPI AG

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  • Título:
    2-Methoxyestradiol-3,17-IO/I,IO/I-bis-sulfamate Inhibits Proliferation and Invasion via Senescence Pathway Induction in Human BRAFi-Resistant Melanoma Cells
  • Autor: Franco, Ylana Adami ; de Moraes, Manoel Oliveira ; Carvalho, Larissa A. C ; Dohle, Wolfgang ; da Silva, Renaira Oliveira ; Noma, Isabella Harumi Yonehara ; Lima, Keli ; Potter, Barry V. L ; Machado-Neto, João A ; Maria-Engler, Silvya Stuchi
  • Assuntos: Analysis ; Apoptosis ; Cancer ; Care and treatment ; Estrogen ; Health aspects ; Melanoma ; Polymerization ; Proteins ; Vemurafenib
  • É parte de: International journal of molecular sciences, 2023-07, Vol.24 (14)
  • Descrição: The endogenous estradiol derivative 2-Methoxyestradiol (2-ME) has shown good and wide anticancer activity but suffers from poor oral bioavailability and extensive metabolic conjugation. However, its sulfamoylated derivative, 2-methoxyestradiol-3,17-O,O-bis-sulfamate (STX140), has superior potential as a therapeutic agent, acts by disrupting microtubule polymerization, leading to cell cycle arrest and apoptosis in cancer cells and possesses much better pharmaceutical properties. This study investigated the antiproliferative and anti-invasive activities of STX140 in both SKMEL-28 naïve melanoma (SKMEL28-P) cells and resistant melanoma cells (SKMEL-28R). STX140 inhibited cell proliferation in the nanomolar range while having a less pronounced effect on human melanocytes. Additionally, STX140 induced cell cycle arrest in the G2/M phase and sub-G1, reduced migration, and clonogenic potential in monolayer models, and inhibited invasion in a 3D human skin model with melanoma cells. Furthermore, STX140 induced senescence features in melanoma and activated the senescence machinery by upregulating the expression of senescence genes and proteins related to senescence signaling. These findings suggest that STX140 may hold potential as a therapeutic agent for melanoma treatment.
  • Editor: MDPI AG
  • Idioma: Inglês
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  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

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