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See detailLa 3'-deoxy-3'-[18F] fluorothymidine ([18F]-FLT) est-elle le prochain traceur utilise en routine pour la TEP apres le [18F]-FDG?
Couturier, Olivier; Leost, Francoise; Campone, Mario et al

in Bulletin du Cancer (2005), 92(9), 789-98

Positron emission tomography (PET) with [18F]-FDG is now firmly established as a clinical tool in oncology. Its applications are however limited in some indications, due to the lack of specificity of its ... [more ▼]

Positron emission tomography (PET) with [18F]-FDG is now firmly established as a clinical tool in oncology. Its applications are however limited in some indications, due to the lack of specificity of its uptake mechanism for tumors, or the low avidity of some cancer types such as prostate. Alternative tracers are thus being developed, in order to fill up this void. Proliferation as a biological target is particularly attractive in cancer imaging. From that perspective, fluorothymidine ([18F]-FLT or FLT) has generated a strong interest among the scientific community, especially since the radiosynthesis process has been improved and simplified, thus making possible to envision a routine use for the tracer. This article aims at summarizing the status of the current scientific data regarding FLT. The uptake mechanism of FLT is well known, relying on the thymidine kinase 1 (TK1) enzymatic activity, and thus on DNA synthesis. Preclinical studies have shown a clear relationship between tracer accumulation and level of tumor proliferation, even though DNA salvage pathwayss intervene in the process and may complicate the interpretation of the results. Several clinical studies suggest a good specificity for tumor, albeit with a lower sensitivity than with FDG. In all likelihood however, the future of FLT lies in the evaluation of antitumor response and possibly the pretherapeutic prognostic characterization, rather than in the diagnosis and staging of malignancies. Although the scientific data regarding this issue remain limited, initial results are encouraging. Further significant work remains to be done in order to fully assess the clinical performances of the tracer, on the one hand, and to determine its place relative to FDG and other emerging tracers, on the other hand. Until these studies are completed, FLT should be considered as a promising tracer, but remaining at an experimental stage of its development. [less ▲]

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See detail3,6-Disubstitued coumarins as mechanism-based inhibitors of thrombin and factor Xa
Frederick, R.; Robert, S.; Charlier, C. et al

in Journal of Medicinal Chemistry (2005), 48

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See detail3,7-Dimethyl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide zwitterion
Dupont, L.; Pirotte, Bernard ULg; De Tullio, Pascal ULg et al

in Acta Crystallographica (1995), C51

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See detailLes 3-alkylamino-2-méthyl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes en tant que nouveaux agents myorelâchants
Pirotte, Bernard ULg; Ouedraogo, R.; Fang, Z. Y. et al

Poster (1996, January 12)

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See detail3-Alkylamino-7-halogeno-4H-1,2,4-benzothiadiazine 1,1-dioxides as new potent KATP channels activators
De Tullio, Pascal ULg; Somers, F.; Boverie, S. et al

Poster (1998, September)

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See detail3-Alkylamino-7-halogeno-4H-1,2,4-benzothiadiazine 1,1-dioxides as new potent KATP channels activators
De Tullio, Pascal ULg; Somers, F.; Boverie, S. et al

in European Journal of Pharmaceutical Sciences (1998), suppl.1

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See detail3-Alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potent KATP-channel activators: structural study and influence of stereochemistry
De Tullio, Pascal ULg; Khelili, S.; Ouedraogo, R. et al

in Pharmacy and Pharmacology Communications (1999), 5

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