A G-quadruplex-interactive potent small-molecule inhibitor of telomerase exhibiting in vitro and in vivo antitumor activity

Molecular Pharmacology

Volumn 61, Issue 5, 2002, Pages 1154-1162

  Gowan, Sharon M ^a,b   Harrison, John R ^a,b   Patterson, Lisa ^a,b   Valenti, Melanie ^a,b   Read, Martin A ^a,b   Neidle, Stephen ^a,b   Kelland, Lloyd R ^a,b  

^a IMPERIAL CANCER RESEARCH FUND   (United Kingdom)

^b INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

9 [4 (N,N DIMETHYLAMINO)PHENYLAMINO] 3,6 BIS(3 PYRROLODINOPROPIONAMIDO)ACRIDINE; PACLITAXEL; TELOMERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL; COMPLEX FORMATION; COMPUTER MODEL; CONTROLLED STUDY; CYTOTOXICITY; DRUG ACTIVITY; DRUG POTENCY; DRUG PROTEIN BINDING; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MINIMUM INHIBITORY CONCENTRATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN INTERACTION; SENESCENCE; TUMOR CELL LINE; XENOGRAFT;

ACRIDINES; ANIMALS; ANTINEOPLASTIC AGENTS; CELL DIVISION; DISEASE MODELS, ANIMAL; DNA; HUMANS; IMMUNOCOMPROMISED HOST; MICE; MICE, NUDE; NEOPLASM TRANSPLANTATION; NEOPLASMS, EXPERIMENTAL; TELOMERASE; TREATMENT OUTCOME; TUMOR CELLS, CULTURED; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 0036241599     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.61.5.1154     Document Type: Article

References (62)

1. Potl, the putative telomere end-binding protein in fission yeast and humans
2. Telomere maintenance mechanisms as a target for drug development
3. Telomere states and cell fates
4. Switching and signaling at the telomere
5. Evidence for an alternative mechanism for maintaining telomere length in human tumors and tumor-derived cell lines
6. 10H-indolo[3,2-b]quinoline
7. Telomerase activity and survival of patients with node-positive breast cancer
8. Telomerase repressor sequences of chromosome 3 and induction of permanent growth arrest in human breast cancer cells
9. A highly selective telomerase inhibitor limiting human cancer cell proliferation
10. A biomarker that identifies senescent human cells in culture and in aging skin in vivo
11. Telomere maintenance by recombination in human cells
12. NMR-based model of a telomerase-inhibiting compound bound to G-quadruplex DNA
13. The RNA component of human telomerase
14. Potent inhibition of telomerase by small-molecule pentacyclic acridines capable of interacting with G-quadruplexes
15. Inhibition of telomerase limits the growth of human cancer cells
16. The hallmarks of cancer
17. Telomeres shorten during ageing of human fibroblasts
18. A mammalian telomerase-associated protein
19. Human telomerase inhibition by substituted acridine derivatives
20. Isothiazolone derivatives selectively inhibit telomerase from human and rat cancer cells in vitro
21. The shortest telomere, not average telomere length, is critical for cell viability and chromosome stability
22. Inhibition of human telomerase in immortal human cells leads to progressive telomere shortening and cell death
23. Effects of chemopreventive and antitelomerase agents on the spontaneous immortalization of breast epithelial cells
24. Correlating telomerase activity levels with human neuroblastoma outcomes
25. Role of telomerase in cellular proliferation and cancer
26. Ku is associated with the telomere in mammals
27. Effects of cationic porphyrins as G-quadruplex interactive agents in human tumor cells
28. Telomerase inhibitors targeting the vulnerable end of cancer?
29. Telomerase biology and phase I trials
30. G-quadruplex DNAs a target for drug design
31. TIN2, a new regulator of telomere length in human cells
32. Specific association of human telomerase activity with immortal cells and cancer
33. A low threshold level of expression of mutant-template telomerase RNA inhibits human tumor cell proliferation
34. Ethidium derivatives bind to G-quartets, inhibit telomerase and act as fluorescent probes for quadruplexes
35. Telomere dysfunction alters the chemotherapeutic profile of transformed cells
36. Reprogramming of telomerase by expression of mutant telomerase RNA template in human cells leads to altered telomeres that correlate with reduced cell viability
37. G-Quadruplex DNA: A target for drug design
38. Telomerase inhibitors based on quadruplex ligands selected by a fluorescence assay
39. HEST2, the putative human telomerase catalytic subunit gene, is up-regulated in tumor cells and during immortalization
40. FJ5002: A potent telomerase inhibitor identified by exploiting the disease-oriented screening program with COMPARE analysis
41. Telomerase as an anti-cancer target: Current status and future prospects
42. Design, synthesis and evaluation of human telomerase inhibitors based upon a tetracyclic structural motif
43. 1,4- And 2,6-Disubstituted amidoanthracene-9,10-dione derivatives as inhibitors of human telomerase
44. 2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase
45. Human telomerase inhibition by regioisomeric disubstituted amidoanthracene-9, 10-diones
46. The telomerase challenge - An unusual problem in drug discovery
47. Induction of duplex to G-quadruplex transition in the c-myc promoter region by a small molecule
48. cis-Amminedichloro(2-methylpyridine) platinum(II) (AMD473), a novel sterically hindered platinum complex: In vivo activity, toxicology and pharmacokinetics in mice
49. Structure-based design of selective and potent G-quadruplex telomerase inhibitors
50. Molecular modeling studies on G-quadruplex complexes of telomerase inhibitors: Structure-activity relationships
51. Ribozyme-mediated telomerase inhibition induces immediate cell loss but not telomere shortening in ovarian cell
52. In vitro generated antibodies specific for telomeric guanine-quadruplex DNA react with Stylonychia lemnae macronuclei
53. Telomestatin, a novel telomerase inhibitor from Streptomyces anulatus
54. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres
55. Control of telomere length by the human telomeric protein TRF1
56. TRF2 protects human telomeres from end-to-end fusions
57. Effects of reverse transcriptase inhibitors on telomere length and telomerase activity in two immortalized human cell lines
58. Inhibition of human telomerase by a G-quadruplex-interactive compound
59. Cationic porphyrins as telomerase inhibitors: The interaction of tetra-(N-methyl-4-pyridyl)porphine with quadruplex DNA
60. United Kingdom Co-ordinating Committee on Cancer Research (UKCCCR) guidelines for the welfare of animals in experimental neoplasia
61. Inhibition of telomerase by G-quartet DNA structures
62. Telomere shortening and apoptosis in telomerase-inhibited human tumor cells