http://www.cnr.it/ontology/cnr/individuo/prodotto/ID27798
Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma. (Articolo in rivista)
- Type
- Label
- Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma. (Articolo in rivista) (literal)
- Anno
- 2010-01-01T00:00:00+01:00 (literal)
- Alternative label
Zuco V, Supino R, Favini E, Tortoreto M, Cincinelli R, Croce AC, Bucci F, Pisano C, Zunino F. (2010)
Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma.
in Biochemical pharmacology
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- Zuco V, Supino R, Favini E, Tortoreto M, Cincinelli R, Croce AC, Bucci F, Pisano C, Zunino F. (literal)
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- Rivista
- Note
- ISI Web of Science (WOS) (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- Valentina Zuco a, Rosanna Supino a, Enrica Favini a, Monica Tortoreto a, Raffaella Cincinelli a,
Anna Cleta Croce b, Federica Bucci c, Claudio Pisano c, Franco Zunino a,*
a Fondazione IRCCS Istituto Nazionale Tumori, 20133 Milan, Italy
b Consiglio Nazionale delle Ricerche, Pavia, Italy
c Sigma-Tau, 00044 Pomezia (Rome), Italy (literal)
- Titolo
- Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma. (literal)
- Abstract
- ST1968 (namitecan), a novel 7-modified hydrophilic camptothecin, was found to be effective against
tumor models relatively resistant to topotecan and irinotecan. Based on this observation, this study was
designed to investigate the cellular and antitumor effects of ST1968 in a subline of A431, squamous cell
carcinoma, selected for resistance to topotecan (A431/TPT). This model was characterized by a slow
growth rate, associated with downregulation of EGFR and topoisomerase I. In contrast to other
camptothecins (SN38 and gimatecan), ST1968 was able to overcome almost completely the resistance at
cellular level. The cellular pharmacokinetics indicated a comparable accumulation and retention of
ST1968 in sensitive and resistant cells, in spite of expression of the efflux transporter, P-glycoprotein, in
resistant cells. The uptake and retention of topotecan were dramatically reduced in both tumor cell lines,
but more evident in the resistant one. In contrast to topotecan, ST1968 retained an outstanding efficacy
in vivo against the resistant tumor (A431/TPT). The results are consistent with the interpretation that
ST1968 was able to overcome the most relevant mechanisms associated with the development of
topotecan resistance (i.e., slow proliferation and target downregulation) owing to its peculiar
pharmacokinetic behaviour.
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