Bcl2L13 is a ceramide synthase inhibitor in glioblastoma.
Therapy resistance is a major limitation to the successful treatment of cancer. Here, we identify Bcl2-like 13 (Bcl2L13), an atypical member of the Bcl-2 family, as a therapy susceptibility gene with elevated expression in solid and blood cancers, including glioblastoma (GBM). We demonstrate that mitochondria-associated Bcl2L13 inhibits apoptosis induced by ... a wide spectrum of chemo- and targeted therapies upstream of Bcl2-associated X protein activation and mitochondrial outer membrane permeabilization in vitro and promotes GBM tumor growth in vivo. Mechanistically, Bcl2L13 binds to proapoptotic ceramide synthases 2 (CerS2) and 6 (CerS6) via a unique C-terminal 250-aa sequence located between its Bcl-2 homology and membrane anchor domains and blocks homo- and heteromeric CerS2/6 complex formation and activity. Correspondingly, CerS2/6 activity and Bcl2L13 abundance are inversely correlated in GBM tumors. Thus, our genetic and functional studies identify Bcl2L13 as a regulator of therapy susceptibility and point to the Bcl2L13-CerS axis as a promising target to enhance responses of therapy-refractory cancers toward conventional and targeted regimens currently in clinical use.
Mesh Terms:
Antineoplastic Agents, Apoptosis, Blotting, Western, Cloning, Molecular, Computational Biology, DNA Primers, Drug Resistance, Gene Expression Regulation, Enzymologic, Gene Library, Glioblastoma, Humans, Membrane Proteins, Oxidoreductases, Polymerase Chain Reaction, Proto-Oncogene Proteins c-bcl-2, Saccharomyces cerevisiae, Sphingosine N-Acyltransferase, Tumor Suppressor Proteins, Two-Hybrid System Techniques
Antineoplastic Agents, Apoptosis, Blotting, Western, Cloning, Molecular, Computational Biology, DNA Primers, Drug Resistance, Gene Expression Regulation, Enzymologic, Gene Library, Glioblastoma, Humans, Membrane Proteins, Oxidoreductases, Polymerase Chain Reaction, Proto-Oncogene Proteins c-bcl-2, Saccharomyces cerevisiae, Sphingosine N-Acyltransferase, Tumor Suppressor Proteins, Two-Hybrid System Techniques
Proc Natl Acad Sci U S A
Date: Apr. 15, 2014
PubMed ID: 24706805
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