1p62

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[[Image:1p62.jpg|left|200px]]<br /><applet load="1p62" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1p62.jpg|left|200px]]
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caption="1p62, resolution 1.90&Aring;" />
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'''Structure of human dCK complexed with gemcitabine and ADP-MG'''<br />
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{{Structure
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|PDB= 1p62 |SIZE=350|CAPTION= <scene name='initialview01'>1p62</scene>, resolution 1.90&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ADP:ADENOSINE-5'-DIPHOSPHATE'>ADP</scene> and <scene name='pdbligand=GEO:GEMCITABINE'>GEO</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Deoxycytidine_kinase Deoxycytidine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.74 2.7.1.74]
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|GENE= DCK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])
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}}
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'''Structure of human dCK complexed with gemcitabine and ADP-MG'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1P62 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=ADP:'>ADP</scene> and <scene name='pdbligand=GEO:'>GEO</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Deoxycytidine_kinase Deoxycytidine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.74 2.7.1.74] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1P62 OCA].
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1P62 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1P62 OCA].
==Reference==
==Reference==
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Structure of human dCK suggests strategies to improve anticancer and antiviral therapy., Sabini E, Ort S, Monnerjahn C, Konrad M, Lavie A, Nat Struct Biol. 2003 Jul;10(7):513-9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12808445 12808445]
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Structure of human dCK suggests strategies to improve anticancer and antiviral therapy., Sabini E, Ort S, Monnerjahn C, Konrad M, Lavie A, Nat Struct Biol. 2003 Jul;10(7):513-9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12808445 12808445]
[[Category: Deoxycytidine kinase]]
[[Category: Deoxycytidine kinase]]
[[Category: Mus musculus]]
[[Category: Mus musculus]]
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[[Category: p-loop]]
[[Category: p-loop]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:25:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:20:20 2008''

Revision as of 11:20, 20 March 2008

Image:1p62.jpg


PDB ID 1p62

Drag the structure with the mouse to rotate
, resolution 1.90Å
Ligands: , and
Gene: DCK (Mus musculus)
Activity: Deoxycytidine kinase, with EC number 2.7.1.74
Coordinates: save as pdb, mmCIF, xml



Structure of human dCK complexed with gemcitabine and ADP-MG


Overview

Human deoxycytidine kinase (dCK) phosphorylates the natural deoxyribonucleosides deoxycytidine (dC), deoxyguanosine (dG) and deoxyadenosine (dA) and is an essential enzyme for the phosphorylation of numerous nucleoside analog prodrugs routinely used in cancer and antiviral chemotherapy. For many of these compounds, the phosphorylation step catalyzed by dCK is the rate-limiting step in their overall activation pathway. To determine the factors that limit the phosphorylation efficiency of the prodrug, we solved the crystal structure of dCK to a resolution of 1.6 A in complex with its physiological substrate deoxycytidine and with the prodrugs AraC and gemcitabine. The structures reveal the determinants of dCK substrate specificity. Especially relevant to new prodrug development is the interaction between Arg128 and the hydrogen-bond acceptor at the sugar 2'-arabinosyl position of AraC and gemcitabine. On the basis of the structures, we designed a catalytically superior dCK variant that could be used in suicide gene-therapy applications.

About this Structure

1P62 is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

Structure of human dCK suggests strategies to improve anticancer and antiviral therapy., Sabini E, Ort S, Monnerjahn C, Konrad M, Lavie A, Nat Struct Biol. 2003 Jul;10(7):513-9. PMID:12808445

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