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Cell Division: Telomerase Inhibitors | | | Inhibitors
Telomerase is a specialized ribonucleoprotein composed of a catalytic subunit telomerase reverse transcriptase (TERT), and two other subunits known as telomerase associated protein 1 (TP1), and a ~445-nucleotide long telomerase RNA component (TR). Telomerase stabilizes telomere lengths by adding hexameric (TTAGGG) repeats to the ends of chromosomes, thereby circumventing the cumulative damage that normally occurs during mitotic cell division. Telomerase recognizes the G-rich strand of an existing telomere repeat sequence and elongates it in the 5´-to-3´ direction. Progressive loss of telomeres, a key feature of normal cells, is considered to be a major regulator of cellular senescence. Tumor cells overcome this problem by overexpressing telomerase. As cancer cells divide more often, on an average, they possess shorter telomeres than normal cells. Hence, without an active telomerase to maintain telomere length, cancer cells could reach critically short telomere at a faster pace than normal cells. Telomerase activity, which is practically undetectable in normal cells, is detected in the majority of tumor cells. The presence of telomerase activity is correlated with poor clinical outcome in cancer patients. Hence, telomerase inhibitors are considered as potential therapeutic agents for the management of tumor progression.
Promising approaches for telomerase inhibition include the use of mutant dominant/negative versions of human TERT (hTERT) and the use of antisense oligonucleotides directed against the template RNA component (hTR) of the telomerase holoenzyme. These telomerase inhibitors reduce telomerase activity and lead to progressive shortening of telomeres with each cell division, ultimately causing cells to undergo apoptosis.
| | | | | | Inhibitors: Telomerase |
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| 3′-Azido-3′-deoxythymidine |
194348 |
| InSolution™ 3′-Azido-3′-Deoxythymidine, Triphosphate, Tetralithium Salt |
194950 |
| 3′-Deoxy-2′,3′-didehydrothymidine |
257920 |
| Ellipticine, 9-Hydroxy-, Hydrochloride |
324680 |
| (–)-Epigallocatechin Gallate |
324880 |
| H-7, Dihydrochloride |
371955 |
| PP2A2, Bovine Kidney |
539510 |
| PIPER |
528120 |
| Telomerase Inhibitor III, Negative Control, Sodium Salt |
581007 |
| Telomerase Inhibitor III, Sodium Salt |
581004 |
| Telomerase Inhibitor VI, Sodium Salt |
581006 |
| Telomerase Inhibitor IX |
581011 |
| TMPyP4 |
613560 |
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