Telomere Targeted Agents Bibliography

Uncapping by the G-Quadruplex Ligand RHPS4 Inhibits Clonogenic Tumour Cell Growth In Vitro and In Vivo Consistent with a Cancer Stem Cell Targeting Mechanism. Phatak P, Cookson JC, Dai F, Smith V, Gartenhaus RB, Stevens MFG, Burger AM. British Journal of Cancer, 2007, 96, 1223-1233.

Telomere Damage Promotes Antitumoral Activity of the G-quadruplex Ligand RHPS4. Salvati E, Leonetti C, Rizzo A, Scarsella M, Mottolese M, Galati R, Sperduti I, Stevens M, D'Incalci M, Blasco M, Chiorino G, Horard B, Gilson E, Stoppacciaro A, Zupi G, Biroccio A. Journal of Clinical Investigation, 2007 [in press]

Synthetic strategies to a telomere-targeted pentacyclic heteroaromatic salt. Hutchinson I, Stevens MFG. Organic and Biomolecular Chemistry, 2007, 5, 114-120.

Structure-specific recognition of quadruplex DNA by organic cations: Influence of shape, substituents and charge. White EW, Tanious F, Ismail MA, Reszka AP, Neidle S, Boykin DW, Wilson WD. Biophysical Chemistry, 2007, 126, 140-153.

TRF2 inhibition triggers apoptosis and reduces tumorigenicity of human melanoma cells. Biroccio A, Rizzo A, Elli R, Koering C-E, Belleville A, Benassi B, Leonetti C, Stevens MF, D'Incalci M, Zupi G, Gilson E. European Journal of Cancer, 2006, 42, 1881-1088.

Pharmacodynamics of the G-quadruplex-stabilizing telomerase inhibitor 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in vitro: activity in human tumor cells correlates with telomere length and can be enhanced, or antagonized, with cytotoxic agents. Cookson JC, Dai F, Smith V, Heald RA, Laughton CA, Stevens MF, Burger AM. Molecular Pharmacology, 2005, 68, 551-558.

Antitumor polycyclic acridines. 17. Synthesis and pharmaceutical profiles of pentacyclic acridinium salts designed to destabilize telomeric integrity. Cookson JC, Heald RA, Stevens MF. Journal of Medicinal Chemistry, 2005, 48, 7198-7207.

Biological activity of the G-quadruplex ligand RHPS4 (3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate) is associated with telomere capping alteration. Leonetti C, Amodei S, D'Angelo C, Rizzo A, Benassi B, Antonelli A, Elli R, Stevens MF, D'Incalci M, Zupi G, Biroccio A. Molecular Pharmacology, 2004, 66,1138-1146.

Synthesis and properties of bioactive 2- and 3-amino-8-methyl-8H-quino[4,3,2-kl]acridine and 8,13-dimethyl-8H-quino[4,3,2-kl]acridinium salts.Hutchinson I, McCarroll AJ, Heald RA, Stevens MF. Organic and Biomolecular Chemistry, 2004, 2, 220-228.

Drug recognition and stabilisation of the parallel-stranded DNA quadruplex d(TTAGGGT)4 containing the human telomeric repeat. Gavathiotis E, Heald RA, Stevens MF, Searle MS. Journal of Molecular Biology, 2003, 334, 25-36.

Antitumour polycyclic acridines. Palladium(0) mediated syntheses of quino[4,3,2-kl]acridines bearing peripheral substituents as potential telomere maintenance inhibitors. Heald RA, Stevens MF. Organic and Biomolecular Chemistry, 2003, 1, 3377-3389.

Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts. Heald RA, Modi C, Cookson JC, Hutchinson I, Laughton CA, Gowan SM, Kelland LR, Stevens MF. Journal of Medicinal Chemistry, 2002, 45, 590-597.

Potent inhibition of telomerase by small-molecule pentacyclic acridines capable of interacting with G-quadruplexes. Gowan SM, Heald R, Stevens MF, Kelland LR. Molecular Pharmacology, 2001, 60, 981-988.

Recognition and Stabilization of Quadruplex DNA by a Potent New Telomerase Inhibitor: NMR Studies of the 2:1 Complex of a Pentacyclic Methylacridinium Cation with d(TTAGGGT)(4). Gavathiotis E, Heald RA, Stevens MF, Searle MS. Angewandte Chemie International Edition (English), 2001, 40, 4749-4751.

Review Article

Shay JW, Wright EW. Telomerase therapeutics for cancer: challenges and new directions. Nature Reviews Drug Discovery. 5 (7) 577-84.