2o3m

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2o3m

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Monomeric G-DNA tetraplex from human C-kit promoter

Overview

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.

About this Structure

2O3M is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of an unprecedented G-quadruplex scaffold in the human c-kit promoter., Phan AT, Kuryavyi V, Burge S, Neidle S, Patel DJ, J Am Chem Soc. 2007 Apr 11;129(14):4386-92. Epub 2007 Mar 16. PMID:17362008

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