1qv8
From Proteopedia
(New page: 200px<br /><applet load="1qv8" size="450" color="white" frame="true" align="right" spinBox="true" caption="1qv8, resolution 2.5Å" /> '''B-DNA Dodecamer d(CGC...) |
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| - | [[Image:1qv8.gif|left|200px]]<br /><applet load="1qv8" size=" | + | [[Image:1qv8.gif|left|200px]]<br /><applet load="1qv8" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1qv8, resolution 2.5Å" /> | caption="1qv8, resolution 2.5Å" /> | ||
'''B-DNA Dodecamer d(CGCGAATTCGCG)2 complexed with proamine'''<br /> | '''B-DNA Dodecamer d(CGCGAATTCGCG)2 complexed with proamine'''<br /> | ||
==Overview== | ==Overview== | ||
| - | New analogues of the minor groove binding ligand Hoechst 33342 have been | + | New analogues of the minor groove binding ligand Hoechst 33342 have been investigated in an attempt to improve radioprotective activity. The synthesis, DNA binding, and in vitro radioprotective properties of methylproamine, the most potent derivative, are reported. Experiments with V79 cells have shown that methylproamine is approximately 100-fold more potent than the classical aminothiol radioprotector WR1065. The crystal structures of methylproamine and proamine complexes with the dodecamer d(CGCGAATTCGCG)(2) confirm that the new analogues also are minor groove binders. It is proposed that the DNA-bound methylproamine ligand acts as a reducing agent by an electron transfer mechanism, repairing transient radiation-induced oxidizing species on DNA. |
==About this Structure== | ==About this Structure== | ||
| - | 1QV8 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with BBZ as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1QV8 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=BBZ:'>BBZ</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QV8 OCA]. |
==Reference== | ==Reference== | ||
In vitro studies with methylproamine: a potent new radioprotector., Martin RF, Broadhurst S, Reum ME, Squire CJ, Clark GR, Lobachevsky PN, White JM, Clark C, Sy D, Spotheim-Maurizot M, Kelly DP, Cancer Res. 2004 Feb 1;64(3):1067-70. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=14871839 14871839] | In vitro studies with methylproamine: a potent new radioprotector., Martin RF, Broadhurst S, Reum ME, Squire CJ, Clark GR, Lobachevsky PN, White JM, Clark C, Sy D, Spotheim-Maurizot M, Kelly DP, Cancer Res. 2004 Feb 1;64(3):1067-70. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=14871839 14871839] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Clark, G | + | [[Category: Clark, G R.]] |
| - | [[Category: Squire, C | + | [[Category: Squire, C J.]] |
[[Category: BBZ]] | [[Category: BBZ]] | ||
[[Category: b-dna]] | [[Category: b-dna]] | ||
[[Category: minor groove binder]] | [[Category: minor groove binder]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:44:01 2008'' |
Revision as of 12:44, 21 February 2008
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B-DNA Dodecamer d(CGCGAATTCGCG)2 complexed with proamine
Overview
New analogues of the minor groove binding ligand Hoechst 33342 have been investigated in an attempt to improve radioprotective activity. The synthesis, DNA binding, and in vitro radioprotective properties of methylproamine, the most potent derivative, are reported. Experiments with V79 cells have shown that methylproamine is approximately 100-fold more potent than the classical aminothiol radioprotector WR1065. The crystal structures of methylproamine and proamine complexes with the dodecamer d(CGCGAATTCGCG)(2) confirm that the new analogues also are minor groove binders. It is proposed that the DNA-bound methylproamine ligand acts as a reducing agent by an electron transfer mechanism, repairing transient radiation-induced oxidizing species on DNA.
About this Structure
1QV8 is a Protein complex structure of sequences from [1] with as ligand. Full crystallographic information is available from OCA.
Reference
In vitro studies with methylproamine: a potent new radioprotector., Martin RF, Broadhurst S, Reum ME, Squire CJ, Clark GR, Lobachevsky PN, White JM, Clark C, Sy D, Spotheim-Maurizot M, Kelly DP, Cancer Res. 2004 Feb 1;64(3):1067-70. PMID:14871839
Page seeded by OCA on Thu Feb 21 14:44:01 2008
