Synthesis and Ex Vivo Biological Evaluation of Gallium-68 Labelled NODAGA Chelates Assessing Cardiac Uptake and Retention

Radiolabelled lipophilic cations can be used to non-invasively report on mitochondrial dysfunction in diseases such as cardiovascular disease, cardiotoxicity and cancer. Several such lipophilic cations are currently used clinically to...

Mitochondria-Targeted Drugs

Background: Targeting of drugs to the subcellular compartments represents one of the modern trends in molecular pharmacology. The approach for targeting mitochondria was developed nearly 50 years ago, but only in the last decade has it started to become widely used for delivering drugs. A number of pathologies are associated with mitochondrial dysfunction, including cardiovascular, neurological, inflammatory and metabolic conditions. Objective: This mini-review aims to highlight the role of mitochondria in pathophysiological conditions and diseases, to classify and summarize our knowledge about targeting mitochondria and to review the most important preclinical and clinical data relating to the antioxidant lipophilic cations MitoQ and SkQ1. Methods: This is a review of available information in the PubMed and Clinical Trials databases (US National Library of Medicine) with no limiting period. Results and Conclusion: Mitochondria play an important role in the pathogenesis of many diseases and possibly in aging. Both MitoQ and SkQ1 have shown many beneficial features in animal models and in a few completed clinical trials. More clinical trials and research efforts are needed to understand the signaling pathways influenced by these compounds. The antioxidant lipophilic cations have great potential for the treatment of a wide range of pathologies.

Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging

5BMF is a new fluorescent mitochondria-accumulating delocalized lipophilic cations [DLC] that boasts significantly increased anti-cancer effects and low toxicity in comparison to previous DLCs, addressing current hurdles in DLC clinical translation.

Boron-containing delocalised lipophilic cations for the selective targeting of cancer cells

To limit the incidence of relapse, cancer treatments must not promote the emergence of drug resistance in tumour and cancer stem cells.

Correction: Boron-containing delocalised lipophilic cations for the selective targeting of cancer cells

Correction for “Boron-containing delocalised lipophilic cations for the selective targeting of cancer cells” by Gianpiero Calabrese et al., Med. Chem. Commun., 2017, 8, 67–72.