Abstract

The Front Cover shows the major antineoplastic mechanisms of gallium compounds. Gallium, whose name originates from the Latin word “Gallus (the Rooster)”, has been considered as one of the main-group elements potentially used in chemotherapy for decades. Gallium compounds, such as Ga(NO3)3, inhibit tumors by relying on the similarity between Ga3+ and Fe3+, the latter of which plays a crucial role in enzyme catalysis and redox homeostasis. Ga3+ ions enter the cells through transferrin-mediated endocytosis and are released after acidification of endosomes. Later on, they interrupt Fe-dependent processes; for example, they inhibit the activity of ribonucleotide reductase (leading to cell cycle arrest) and Fe-containing proteins in the respiratory chain (leading to the generation of ROS). To solve the problem of complex Ga(III) speciation in the circulatory system, a large number of ligands were applied to form Ga(III) complexes, supplying multiple theranostic functions and novel modes of action. More information can be found in the Review by J.-L. Zhang and co-workers.

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