Novel tryptophan 2,3-dioxygenase-targeted ruthenium(ii)-indole complex activates immunotherapy <i>in vitro</i> and <i>in vivo</i>.

ABSTRACT: Immunotherapy targeting immune checkpoints has emerged as a promising strategy in cancer treatment; however, the heterogeneous and dynamic tumor microenvironment (TME) imposes critical constraints on therapeutic outcomes. Tryptophan 2,3-dioxygenase (TDO), often dysregulated in malignant tissues, plays a pivotal role in shaping an immunosuppressive milieu by depleting tryptophan, thereby hindering anti-tumor immune response. To counteract this immune evasion mechanism, we designed a novel indole-coordinated ruthenium(ii) arene complex (In-Ru), aimed at bolstering tumor immunotherapy and thwarting immune evasion by targeting TDO expression. Our findings reveal that In-Ru exerts markedly potent anti-proliferative effects against HepG2 cells. It achieves this by specifically localizing to the

SUBMITTER: Shen ZQ 

PROVIDER: S-EPMC12308519 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature