Effective Targeting of Melanoma Cells by Combination of Mcl-1 and Bcl-2/Bcl-x_L/Bcl-w Inhibitors.

ABSTRACT: Recent advances in melanoma therapy have significantly improved the prognosis of metastasized melanoma. However, large therapeutic gaps remain that need to be closed by new strategies. Antiapoptotic Bcl-2 proteins critically contribute to apoptosis deficiency and therapy resistance. They can be targeted by BH3 mimetics, small molecule antagonists that mimic the Bcl-2 homology domain 3 (BH3) of proapoptotic BH3-only proteins. By applying in vitro experiments, we aimed to obtain an overview of the possible suitability of BH3 mimetics for future melanoma therapy. Thus, we investigated the effects of ABT-737 and ABT-263, which target Bcl-2, Bcl-x_L and Bcl-w as well as the Bcl-2-selective ABT-199 and the Mcl-1-selective S63845, in a panel of four BRAF-mutated and BRAF-W

SUBMITTER: Peng Z 

PROVIDER: S-EPMC10970841 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature