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Telomerase inhibitors and activators act on telomerase, the reverse transcriptase that extends telomeres. Telomerase activity was first found in 1985 in Tetrahymena extracts, as a terminal transferase that adds telomeric repeats. The human enzyme pairs telomerase reverse transcriptase (TERT) with an RNA template. A 1994 study detected telomerase activity in most immortal cell lines and tumors but rarely in normal somatic tissues. BIBR 1532 inhibits the enzyme directly, while Braco-19, RHPS4 and TMPyP4 tosylate stabilize telomeric G-quadruplex DNA. 6-Thio-dG is a nucleoside that telomerase incorporates into telomeres, and epithalon is listed as an activator. The set also includes the topoisomerase inhibitors amsacrine and GENZ-644282.
Synonyms: AlaGluAspGly
Epithalon is a synthetic tetra-peptide (Ala-Glu-Asp-Gly),which regulated pineal secretion processes, presumably, via protooncogenes.
6-thio-dG is a nucleoside analog and telomerase substrate.
