1R68

Role of the amino sugar in DNA binding of disaccharide anthracyclines: crystal structure of MAR70/d(CGATCG) complex

1R68 の概要

• エントリーDOI: 10.2210/pdb1r68/pdb
• 分子名称: 5'-D(*CP*GP*AP*TP*CP*G)-3', 4'-EPI-4'-(2-DEOXYFUCOSE)DAUNOMYCIN (3 entities in total)
• 機能のキーワード: right handed dna, double helix, drug-dna complex, dna
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 2466.88

構造登録者

Temperini, C.,Cirilli, M.,Aschi, M.,Ughetto, G. (登録日: 2003-10-15, 公開日: 2005-02-22, 最終更新日: 2024-02-14)

主引用文献

Temperini, C.,Cirilli, M.,Aschi, M.,Ughetto, G.
Role of the amino sugar in DNA binding of disaccharide anthracyclines: crystal structure of the complex MAR70/d(CGATCG).
BIOORG.MED.CHEM., 13:1673-1679, 2005

PubMed Abstract: Disaccharide anthracyclines analogues have been shown to exhibit different antitumour activity as compared with parents compounds doxorubicin and daunomycin. Here we report the crystal structure of the disaccharide analog MAR70 complexed with the DNA hexamer d(CGATCG). The structure has been solved at 1.54A resolution and is similar to previous crystallized anthracycline-DNA complexes with both sugar rings of the disaccharide chain lying in the DNA minor groove. Comparison with the structure of MEN10755 another disaccharide anthracycline co-crystallized with the same DNA hexamer suggests a correlation between the position of the amino sugar on the disaccharide chain and the conformation of this moiety when binding to DNA. This is discussed with respect to the influence on drug activity and on the possible interaction with other cellular targets.

PubMed: 15698785
DOI: 10.1016/j.bmc.2004.12.007

実験手法

X-RAY DIFFRACTION (1.2 Å)