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Merck

Recent patents on anti-telomerase cancer therapy.

Recent patents on anti-cancer drug discovery (2011-08-23)
Apurva Agrawal, Shweta Dang, Reema Gabrani
RESUMEN

Telomerase, a specialised RNA-directed DNA polymerase extends and stabilises the telomeres at the ends of the eukaryotic chromosomes. The progressive loss of telomeres results in limited number of cell divisions and has been linked to the mechanism of human cellular ageing. Tumour cells marked by indefinite proliferation have stable telomere length maintained by telomerase. The differential expression of the telomerase enzyme in normal and cancer cells have led to the evolution of tumour specific anti-telomerase approaches which inhibit the telomerase enzyme activity so as to destabilise and shorten the telomeres leading to senescence in cancer cells. In the current review, we have selected nine tumour specific anti-telomerase approaches based on their mechanism of action or the target components of the human telomerase enzyme: Antisense-oligonucleotides, hammerhead ribozymes, dominant negative hTERT, reverse-transcriptase inhibitors, immunotherapy, G-quadruplex stabilisers, gene therapy, small molecule inhibitors and RNA interference. Recent research developments for each of the anti-telomerase approaches with the detailed analysis of specific granted patents from the perspective of different claims and downstream applications have been provided. A comprehensive list of patents for the different anti-telomerase approaches which includes information regarding the authors and institutional ownership along with the year of issue of the patent has also been provided.

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Roche
7-Deaza-2′-deoxy-guanosine-5′-triphosphate, 95% (7-Deaza-dGTP, HPLC), ≤4% (7-Deaza-dGDP, HPLC), solution, 10 mM
Sigma-Aldrich
7-Deaza-2′-deoxyguanosine 5′-triphosphate lithium salt, 10 mM in H2O