2000
Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups
BRABEC, Viktor; Kamila NEPLECHOVÁ; Jana KAŠPÁRKOVÁ a Nicholas FARRELLZákladní údaje
Originální název
Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups
Autoři
BRABEC, Viktor; Kamila NEPLECHOVÁ; Jana KAŠPÁRKOVÁ a Nicholas FARRELL
Vydání
Journal of Biological Inorganic Chemistry, Germany, Springer-Verlag, 2000, 0949-8257
Další údaje
Jazyk
angličtina
Typ výsledku
Článek v odborném periodiku
Obor
10610 Biophysics
Stát vydavatele
Česká republika
Utajení
není předmětem státního či obchodního tajemství
Impakt faktor
Impact factor: 3.045
Kód RIV
RIV/00216224:14310/00:00003310
Organizační jednotka
Přírodovědecká fakulta
Změněno: 27. 2. 2001 10:02, prof. RNDr. Viktor Brabec, DrSc.
Anotace
V originále
Recent findings that novel trans-dichloroplatinum(II) complexes exhibit antitumor activity violate the classical structure-activity relationships of platinum(II) complexes. These novel "nonclassical" trans-platinum complexes also comprise those containing planar aromatic amines. The initial studies have shown that these compounds form a considerable amount of DNA interstrand cross-links (up to ~30 %) with a rate markedly higher than clinically ineffective transplatin. The present work has shown that DNA interstrand cross-linking by trans-[PtCl2(NH3)(quinoline)] and trans-[PtCl2(NH3)(thiazole)] is formally equivalent to that by antitumor cisplatin, but different from clinically ineffective transplatin which preferentially forms these adducts between complementary guanine and cytosine residues. This result shows for the first time that the simple chemical modification of structure of an inactive compound alters its DNA binding site into a DNA adduct of an active drug.
Návaznosti
| GA305/99/0695, projekt VaV |
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