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Rhodium(ii)–fluorophore conjugates have strong rhodium-based fluorescence quenching that can be harnessed to report on a conjugate's cellular uptake and the intracellular decomposition rate. Information gleened from this study allowed the design of an improved STAT3 metalloinhibitor. [ABSTRACT FROM AUTHOR]

Nearly 40 % of children with acute myeloid leukemia (AML) suffer relapse arising from chemoresistance, often involving upregulation of the oncoprotein STAT3 (signal transducer and activator of transcription 3). Herein, rhodium(II)-catalyzed, proximity-driven modification identifies the STAT3 coiled-coil domain (CCD) as a novel ligand-binding site, and we describe a new naphthalene sulfonamide inhibitor that targets the CCD, blocks STAT3 function, and halts its disease-promoting effects in vitro, in tumor growth models, and in a leukemia mouse model, validating this new therapeutic target for resistant AML. [ABSTRACT FROM AUTHOR]

The article presents comment on the study that explores the development of an engineered signal transducer and activator of transcription 3 (STAT3) decoy oligodeoxynucleotide (dODN) that is stable in serum taken by target cells. Details of the improtant role played by STAT3 target genes and its clever system into a viable therapeutic molecule are provided. The findings of the study which showed the potential fo STAT3 in alleviating acute myeloid leukemia (AML) are offered.