BRABEC, Viktor, Kamila NEPLECHOVÁ, Jana KAŠPÁRKOVÁ and Nicholas FARRELL. Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups. Journal of Biological Inorganic Chemistry. Germany: Springer-Verlag, 2000, vol. 2000, No 5, p. 364-368. ISSN 0949-8257. |
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@article{328911, author = {Brabec, Viktor and Neplechová, Kamila and Kašpárková, Jana and Farrell, Nicholas}, article_location = {Germany}, article_number = {5}, language = {eng}, issn = {0949-8257}, journal = {Journal of Biological Inorganic Chemistry}, title = {Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups}, volume = {2000}, year = {2000} }
TY - JOUR ID - 328911 AU - Brabec, Viktor - Neplechová, Kamila - Kašpárková, Jana - Farrell, Nicholas PY - 2000 TI - Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups JF - Journal of Biological Inorganic Chemistry VL - 2000 IS - 5 SP - 364 EP - 364 PB - Springer-Verlag SN - 09498257 N2 - 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. ER -
BRABEC, Viktor, Kamila NEPLECHOVÁ, Jana KAŠPÁRKOVÁ and Nicholas FARRELL. Steric control of DNA interstrand cross-link sites of trans platinum complexes: specificity can be dictated by planar nonleaving groups. \textit{Journal of Biological Inorganic Chemistry}. Germany: Springer-Verlag, 2000, vol.~2000, No~5, p.~364-368. ISSN~0949-8257.
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