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Therapeutic targeting of FOS in mutant <i>TERT</i> cancers through removing TERT suppression of apoptosis via regulating <i>survivin</i> and <i>TRAIL-R2</i>

Rengyun Liu, Jie Tan, Xiaopei Shen, Ke Jiang, Chaoqun Wang, Guangwu Zhu, Mingzhao Xing

2021Proceedings of the National Academy of Sciences49 citationsDOIOpen Access PDF

Abstract

Significance Given that oncogenic hotspot mutations in the promoter of the gene for telomerase reverse transcriptase (TERT) are common, it has been attractive to develop therapeutic strategies targeting TERT in mutant TERT human cancers. No direct TERT inhibitor is currently available, however, hindering this pursuit. By targeting FOS in the FOS/GABPB/(mutant) TERT cascade using a FOS inhibitor to inhibit mutant TERT cancer cells and tumors through induction of apoptosis by relieving TERT suppression, this study identifies a therapeutic strategy of targeting the TERT cascade for cancers. This study also uncovers a molecular mechanism in which TERT controls apoptosis by specifically regulating two key players among many in the apoptotic cascade, answering a long-time question of how TERT suppresses apoptosis.

Topics & Concepts

SurvivinApoptosisMutantCancer researchChemistryBiologyMolecular biologyGeneBiochemistryTelomeres, Telomerase, and SenescenceCorneal Surgery and TreatmentsCancer Research and Treatments
Therapeutic targeting of FOS in mutant <i>TERT</i> cancers through removing TERT suppression of apoptosis via regulating <i>survivin</i> and <i>TRAIL-R2</i> | Litcius