title: Imetelstat (GRN163L)--telomerase-based cancer therapy.
abstract: Telomeres and telomerase play essential roles in the regulation of the lifespan of human cells. While normal human somatic cells do not or only transiently express telomerase and therefore shorten their telomeres with each cell division, most human cancer cells typically express high levels of telomerase and show unlimited cell proliferation. High telomerase expression allows cells to proliferate and expand long-term and therefore supports tumor growth. Owing to the high expression and its role, telomerase has become an attractive diagnostic and therapeutic cancer target. Imetelstat (GRN163L) is a potent and specific telomerase inhibitor and so far the only drug of its class in clinical trials. Here, we report on the structure and the mechanism of action of imetelstat as well as about the preclinical and clinical data and future prospects using imetelstat in cancer therapy.
authors.affiliation: Department of Hematology, University Hospital Essen, University of Duisburg-Essen, Hufelandstrasse 55, 45122, Essen, Germany. alexander.roeth@uni-due.de
authors.forename: Alexander
authors.initials: A
authors.lastname: Röth
authors.forename: Calvin B
authors.initials: CB
authors.lastname: Harley
authors.forename: Gabriela M
authors.initials: GM
authors.lastname: Baerlocher
mesh_terms: D000818:Animals; D002986:Clinical Trials as Topic; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D009841:Oligonucleotides; D009842:Oligopeptides / Q000627:therapeutic use*; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology
chemical_list: C505952:GRN163L peptide; D009841:Oligonucleotides; D009842:Oligopeptides; D019098:Telomerase