2O3M

Monomeric G-DNA tetraplex from human C-kit promoter

2O3M の概要

• エントリーDOI: 10.2210/pdb2o3m/pdb
• 関連するPDBエントリー: 2A5P
• 分子名称: 5'-D(*AP*GP*GP*GP*AP*GP*GP*GP*CP*GP*CP*TP*GP*GP*GP*AP*GP*GP*AP*GP*GP*G)-3' (1 entity in total)
• 機能のキーワード: g-tetrad;parallel g-quadruplex; edgewise, single-residue cha reversal, 5-nucleotide snap-back loops;broken strand topolog, dna
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 7028.52

構造登録者

Phan, A.T.,Kuryavyi, V.V.,Burge, S.,Neidle, S.,Patel, D.J. (登録日: 2006-12-01, 公開日: 2007-05-22, 最終更新日: 2023-12-27)

主引用文献

Phan, A.T.,Kuryavyi, V.V.,Burge, S.,Neidle, S.,Patel, D.J.
Structure of an unprecedented G-quadruplex scaffold in the human c-kit promoter.
J.Am.Chem.Soc., 129:4386-4392, 2007

PubMed Abstract: The c-kit oncogene is an important target in the treatment of gastrointestinal tumors. A potential approach to inhibition of the expression of this gene involves selective stabilization of G-quadruplex structures that may be induced to form in the c-kit promoter region. Here we report on the structure of an unprecedented intramolecular G-quadruplex formed by a G-rich sequence in the c-kit promoter in K+ solution. The structure represents a new folding topology with several unique features. Most strikingly, an isolated guanine is involved in G-tetrad core formation, despite the presence of four three-guanine tracts. There are four loops: two single-residue double-chain-reversal loops, a two-residue loop, and a five-residue stem-loop, which contain base-pairing alignments. This unique structural scaffold provides a highly specific platform for the future design of ligands specifically targeted to the promoter DNA of c-kit.

PubMed: 17362008
DOI: 10.1021/ja068739h

実験手法

SOLUTION NMR