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Titolo:
Sequence specificity and reactivity of the binding of phenazine-tethered platinum complexes to DNA
Autore:
Perrin, LC; Cullinane, C; McFadyen, WD; Phillips, DR;
Indirizzi:
La Trobe Univ, Dept Biochem, Bundoora, Vic 3083, Australia La Trobe Univ Bundoora Vic Australia 3083 , Bundoora, Vic 3083, Australia Univ Melbourne, Sch Chem, Parkville, Vic 3052, Australia Univ Melbourne Parkville Vic Australia 3052 arkville, Vic 3052, Australia
Titolo Testata:
ANTI-CANCER DRUG DESIGN
fascicolo: 3, volume: 14, anno: 1999,
pagine: 243 - 252
SICI:
0266-9536(199906)14:3<243:SSAROT>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVE TRANSCRIPTION; CROSS-LINKS; CISPLATIN; CIS-DICHLORO(ETHYLENEDIAMINE)PLATINUM(II); CIS-DIAMMINEDICHLOROPLATINUM(II); INVITRO; AGENTS; CELLS; SITES;
Keywords:
cisplatin; DNA binding; DNA platination; kinetics; phenazine-tethered platinum;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Phillips, DR La Trobe Univ, Dept Biochem, Bundoora, Vic 3083, Australia LaTrobe Univ Bundoora Vic Australia 3083 ic 3083, Australia
Citazione:
L.C. Perrin et al., "Sequence specificity and reactivity of the binding of phenazine-tethered platinum complexes to DNA", ANTI-CAN DR, 14(3), 1999, pp. 243-252

Abstract

An in vitro transcription assay was used to probe the sequence specificityof the binding of phenazine-tethered platinum complexes to DNA, It was found that when compared to cis-dichloro(ethylenediamine)platinum(II), the number of RNA polymerase blockage sites was increased by similar to 50% and the blockage sites were broadened by 1-3 nucleotides by the presence of the phenazine ligand. The rate of platination was also enhanced by the presence of the intercalator, and the increase in the kinetics of platination resulted in increased levels of adducts formed (i.e. high drug occupancy) as detected under conditions of active transcription. The level of platination by derivative 3 was 20-fold greater than that of the reference compound, whichlacked a tethered intercalating phenazine group.

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Documento generato il 30/09/20 alle ore 04:39:10