Fattore, Luigi; Malpicci, Debora; Milite, Ciro; Castellano, Sabrina; Sbardella, Gianluca; Botti, Gerardo; Ascierto, Paolo A.; Mancini, Rita; Ciliberto, Gennaro published the artcile< Reverse transcriptase inhibition potentiates target therapy in BRAF-mutant melanomas: effects on cell proliferation, apoptosis, DNA-damage, ROS induction and mitochondrial membrane depolarization>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is melanoma BRAF reverse transcriptase target therapy apoptosis DNA damage; DSBs; Drug resistance; Melanoma; Mitochondrial membrane depolarization; Reverse transcriptase inhibitors; Target therapy.
Abstract: Target therapies based on BRAF and MEK inhibitors (MAPKi) have changed the therapeutic landscape for metastatic melanoma patients bearing mutations in the BRAF kinase. However, the emergence of drug resistance imposes the necessity to conceive novel therapeutic strategies capable to achieve a more durable disease control. Their activation can be efficiently controlled with reverse transcriptase inhibitors (RTIs) frequently used in the treatment of AIDS. These drugs have demonstrated anti-proliferative effects in several cancer models, including also metastatic melanoma. However, to our knowledge no previous study investigated the capability of RTIs to mitigate drug resistance to target therapy in BRAF-mutant melanomas. In this short report we show that the non-nucleoside RTI, SPV122 in combination with MAPKi strongly inhibits BRAF-mutant melanoma cell growth, induces apoptosis, and delays the emergence of resistance to target therapy in vitro. Mechanistically, this combination strongly induces DNA double-strand breaks, mitochondrial membrane depolarization and increased ROS levels. Our results shed further light on the mol. activity of RTI in melanoma and pave the way to their use as a novel therapeutic option to improve the efficacy of target therapy. [media not available: see fulltext] Graphical abstract: [graphic not available: see fulltext].
Cell Communication and Signaling published new progress about Apoptosis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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