2l7v

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[[Image:2l7v.png|left|200px]]
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==Quindoline/G-quadruplex complex==
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<StructureSection load='2l7v' size='340' side='right' caption='[[2l7v]], [[NMR_Ensembles_of_Models | 10 NMR models]]' scene=''>
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== Structural highlights ==
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[[2l7v]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2L7V OCA]. <br>
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<b>Activity:</b> <span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span><br>
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== Publication Abstract from PubMed ==
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Unimolecular parallel-stranded G-quadruplex structures are found to be prevalent in gene promoters. The nuclease hypersensitivity element III(1) (NHE III(1)) of the c-MYC promoter can form transcriptionally active and silenced forms, and the formation of DNA G-quadruplex structures has been shown to be critical for c-MYC transcriptional silencing. The solution structure of a 2:1 quindoline-G-quadruplex complex has been solved and shows unexpected features, including the drug-induced reorientation of the flanking sequences to form a new binding pocket. While both 3' and 5' complexes show overall similar features, there are identifiable differences that emphasize the importance of both stacking and electronic interactions. For the first time, we describe the importance of the shape of the ligand as well as the two flanking bases in determining drug binding specificity. These structures provide important insights for the structure-based rational design of drugs that bind to unimolecular parallel G-quadruplexes commonly found in promoter elements.
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Solution Structure of a 2:1 Quindoline-c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design.,Dai J, Carver M, Hurley LH, Yang D J Am Chem Soc. 2011 Nov 9;133(44):17673-80. Epub 2011 Oct 14. PMID:21967482<ref>PMID:21967482</ref>
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The line below this paragraph, containing "STRUCTURE_2l7v", creates the "Structure Box" on the page.
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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or leave the SCENE parameter empty for the default display.
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{{STRUCTURE_2l7v| PDB=2l7v | SCENE= }}
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===Quindoline/G-quadruplex complex===
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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== References ==
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<references/>
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The line below this paragraph, {{ABSTRACT_PUBMED_21967482}}, adds the Publication Abstract to the page
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</StructureSection>
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(as it appears on PubMed at http://www.pubmed.gov), where 21967482 is the PubMed ID number.
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{{ABSTRACT_PUBMED_21967482}}
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==About this Structure==
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[[2l7v]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2L7V OCA].
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==Reference==
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<ref group="xtra">PMID:021967482</ref><references group="xtra"/>
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[[Category: Carver, M.]]
[[Category: Carver, M.]]
[[Category: Dai, J.]]
[[Category: Dai, J.]]

Revision as of 08:41, 30 April 2014

Quindoline/G-quadruplex complex

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