Article: Mitochondria-targeted metformins: anti-tumour and redox signalling mechanisms.
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2016 Volume 7, Issue 2, Page(s) 20160109
Abstract: ... in a new class of mitochondria-targeted metformin analogues with significantly enhanced anti-tumour ... potential. Using this approach, we synthesized various mitochondria-targeted metformin analogues ... Reports suggest that metformin exerts anti-cancer effects in diabetic individuals ...
| Abstract | Reports suggest that metformin exerts anti-cancer effects in diabetic individuals with pancreatic cancer. Thus, metformin is currently being repurposed as a potential drug in cancer treatment. Studies indicate that potent metformin analogues are required in cancer treatment because of the low bioavailability of metformin in humans at conventional antidiabetic doses. We proposed that improved mitochondrial targeting of metformin by attaching a positively charged lipophilic triphenylphosphonium group will result in a new class of mitochondria-targeted metformin analogues with significantly enhanced anti-tumour potential. Using this approach, we synthesized various mitochondria-targeted metformin analogues with different alkyl chain lengths. Results indicate that the antiproliferative effects increased with increasing alkyl chain lengths (100-fold to 1000-fold). The lead compound, mito-metformin |
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| Language | English |
| Publishing date | 2016-12-06 |
| Publishing country | England |
| Document type | Journal Article ; Review |
| ISSN | 2042-8898 |
| ISSN | 2042-8898 |
| DOI | 10.1098/rsfs.2016.0109 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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