title: Targeting human telomerase for cancer therapeutics.
abstract: The enzyme telomerase is involved in the replication of telomeres, specialized structures that cap and protect the ends of chromosomes. Its activity is required for maintenance of telomeres and for unlimited lifespan, a hallmark of cancer cells. Telomerase is overexpressed in the vast majority of human cancer cells and therefore represents an attractive target for therapy. Several approaches have been developed to inhibit this enzyme through the targeting of its RNA or catalytic components as well as its DNA substrate, the single-stranded 3'-telomeric overhang. Telomerase inhibitors are chemically diverse and include modified oligonucleotides as well as small diffusable molecules, both natural and synthetic. This review presents an update of recent investigations pertaining to these agents and discusses their biological properties in the context of the initial paradigm that the exposure of cancer cells to these agents should lead to progressive telomere shortening followed by a delayed growth arrest response.
authors.affiliation: Laboratoire de Biophysique, Muséum National d'Histoire Naturelle USM503, INSERM U 565, CNRS UMR 5153, 43, rue Cuvier, 75231, Paris cedex 05, France.
authors.forename: Lionel
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authors.lastname: Guittat
authors.forename: Patrizia
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authors.lastname: Alberti
authors.forename: Dennis
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authors.lastname: Gomez
authors.forename: Anne
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authors.lastname: De Cian
authors.forename: Gaëlle
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authors.lastname: Pennarun
authors.forename: Thibault
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authors.lastname: Lemarteleur
authors.forename: Chafke
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authors.lastname: Belmokhtar
authors.forename: Rajaa
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authors.lastname: Paterski
authors.forename: Hamid
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authors.lastname: Morjani
authors.forename: Chantal
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authors.lastname: Trentesaux
authors.forename: Eliane
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authors.lastname: Mandine
authors.forename: François
authors.initials: F
authors.lastname: Boussin
authors.forename: Patrick
authors.initials: P
authors.lastname: Mailliet
authors.forename: Laurent
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authors.lastname: Lacroix
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Riou
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Mergny