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Gallium (III) Complexes in Cancer Chemotherapy

Gallium, the group 13 metal, has been found to be potentially useful in fighting against cancers since last century. The trivalent Ga(III) shares most chemical properties except redox activity with Fe(III), so that it acts as a competitive inhibitor of Fe(III) in vitro and in vivo, which contributes...

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Published in:European journal of inorganic chemistry 2022-02, Vol.2022 (6), p.n/a
Main Authors: Peng, Xin‐Xin, Gao, Song, Zhang, Jun‐Long
Format: Article
Language:English
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Summary:Gallium, the group 13 metal, has been found to be potentially useful in fighting against cancers since last century. The trivalent Ga(III) shares most chemical properties except redox activity with Fe(III), so that it acts as a competitive inhibitor of Fe(III) in vitro and in vivo, which contributes to its antineoplastic activity. As an Fe(III) mimic, Ga(III) can be uptaken into cells through transferrin and be stored in ferritin. Furthermore, it disrupts Fe‐dependent processes, for example, by inhibiting the activity of ribonucleotide reductase and Fe‐containing proteins in the respiratory chain. To solve the problems of complex Ga(III) speciation in the circulatory system, a large number of ligands were applied to form Ga(III) complexes, supplying multiple functions. In this review, we summarized the anticancer mechanisms of Ga(III) and introduce numerous Ga(III) complexes with great antineoplastic potential. The trivalent Ga(III) shares most chemical properties except redox activity with Fe(III), so that it acts as a competitive inhibitor of Fe(III) in the human body, which contributes to its antineoplastic activity. As an Fe(III) mimic, Ga(III) can be uptaken into cells through transferrin and be stored in ferritin. Furthermore, it disrupts Fe‐dependent processes by occupying the Fe(III) sites in biomolecules, for example, inhibiting the activity of ribonucleotide reductase and Fe‐containing proteins in the respiratory chain. To solve the problems of complex Ga(III) speciation in the circulatory system, a large number of ligands were applied to form Ga(III) complexes, preventing hydrolysis and precipitation of Ga(III) ions, offering multiple functions and anticancer mechanisms.
ISSN:1434-1948
1099-0682
DOI:10.1002/ejic.202100953