Oxali(IV)Fluors: Fluorescence Responsive Oxaliplatin(IV) Complexes Identify a Hypoxia-Dependent Reduction in Cancer Cells.

Platinum(IV) anticancer agents have demonstrated the potential to overcome the limitations associated with the widely used Pt(II) chemotherapeutics, cisplatin, carboplatin, and oxaliplatin. In order to identify therapeutic scenarios where this type of chemotherapy can be applied, an improved understanding on the intracellular reduction of Pt(IV) complexes is needed. Here, we report the synthesis of two fluorescence responsive oxaliplatin(IV)(OxPt) complexes, OxaliRes and OxaliNap.

Small-Molecule Polθ Inhibitors Provide Safe and Effective Tumor Radiosensitization in Preclinical Models.

Purpose: DNA polymerase theta (Polθ, encoded by the POLQ gene) is a DNA repair enzyme critical for microhomology mediated end joining (MMEJ). Polθ has limited expression in normal tissues but is frequently overexpressed in cancer cells and, therefore, represents an ideal target for tumor-specific radiosensitization. In this study we evaluate whether targeting Polθ with novel small-molecule inhibitors is a feasible strategy to improve the efficacy of radiotherapy.

A fluorescent probe strategy for the detection and discrimination of hydrogen peroxide and peroxynitrite in cells.

Aryl boronate fluorescent probes allow the non-invasive study of dynamic cellular processes involving the reactive species, hydrogen peroxide (HO) and peroxynitrite (ONOO). However, the ability of these probes to differentiate between these two species remains unclear. Here, we report a boronate-functionalised hemicyanine dye (HD-BPin) as a potential strategy to distinguish between HO at 704 nm (red channel) and ONOO at 460 nm (blue channel) in solution and in cells.