1k9g
From Proteopedia
(New page: 200px<br /><applet load="1k9g" size="450" color="white" frame="true" align="right" spinBox="true" caption="1k9g, resolution 1.4Å" /> '''Crystal Structure of ...) |
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| - | [[Image:1k9g.gif|left|200px]]<br /><applet load="1k9g" size=" | + | [[Image:1k9g.gif|left|200px]]<br /><applet load="1k9g" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1k9g, resolution 1.4Å" /> | caption="1k9g, resolution 1.4Å" /> | ||
'''Crystal Structure of the Complex of Cryptolepine-d(CCTAGG)2'''<br /> | '''Crystal Structure of the Complex of Cryptolepine-d(CCTAGG)2'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Cryptolepine, a naturally occurring indoloquinoline alkaloid used as an | + | Cryptolepine, a naturally occurring indoloquinoline alkaloid used as an antimalarial drug in Central and Western Africa, has been found to bind to DNA in a formerly unknown intercalation mode. Evidence from competition dialysis assays demonstrates that cryptolepine is able to bind CG-rich sequences containing nonalternating CC sites. Here we show that cryptolepine interacts with the CC sites of the DNA fragment d(CCTAGG)(2) in a base-stacking intercalation mode. This is the first DNA intercalator complex, from approximately 90 solved by X-ray crystallography, to bind a nonalternating (pyrimidine-pyrimidine) DNA sequence. The asymmetry of the drug induces a perfect stacking with the asymmetric site, allowing for the stability of the complex in the absence of hydrogen bonding interactions. The crystal structure of this antimalarial drug-DNA complex provides evidence for the first nonalternating intercalation and, as such, provides a basis for the design of new anticancer or antimalarial drugs. |
==About this Structure== | ==About this Structure== | ||
| - | 1K9G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with DR1 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1K9G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=DR1:'>DR1</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1K9G OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Aymami, J.]] | [[Category: Aymami, J.]] | ||
[[Category: Coll, M.]] | [[Category: Coll, M.]] | ||
| - | [[Category: Lisgarten, J | + | [[Category: Lisgarten, J N.]] |
[[Category: Portugal, J.]] | [[Category: Portugal, J.]] | ||
| - | [[Category: Wright, C | + | [[Category: Wright, C W.]] |
[[Category: DR1]] | [[Category: DR1]] | ||
[[Category: dna intercalator complex]] | [[Category: dna intercalator complex]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:31:34 2008'' |
Revision as of 11:31, 21 February 2008
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Crystal Structure of the Complex of Cryptolepine-d(CCTAGG)2
Overview
Cryptolepine, a naturally occurring indoloquinoline alkaloid used as an antimalarial drug in Central and Western Africa, has been found to bind to DNA in a formerly unknown intercalation mode. Evidence from competition dialysis assays demonstrates that cryptolepine is able to bind CG-rich sequences containing nonalternating CC sites. Here we show that cryptolepine interacts with the CC sites of the DNA fragment d(CCTAGG)(2) in a base-stacking intercalation mode. This is the first DNA intercalator complex, from approximately 90 solved by X-ray crystallography, to bind a nonalternating (pyrimidine-pyrimidine) DNA sequence. The asymmetry of the drug induces a perfect stacking with the asymmetric site, allowing for the stability of the complex in the absence of hydrogen bonding interactions. The crystal structure of this antimalarial drug-DNA complex provides evidence for the first nonalternating intercalation and, as such, provides a basis for the design of new anticancer or antimalarial drugs.
About this Structure
1K9G is a Protein complex structure of sequences from [1] with as ligand. Full crystallographic information is available from OCA.
Reference
The antimalarial and cytotoxic drug cryptolepine intercalates into DNA at cytosine-cytosine sites., Lisgarten JN, Coll M, Portugal J, Wright CW, Aymami J, Nat Struct Biol. 2002 Jan;9(1):57-60. PMID:11731803
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