1e9c

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[[Image:1e9c.jpg|left|200px]]<br /><applet load="1e9c" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1e9c.jpg|left|200px]]
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caption="1e9c, resolution 1.6&Aring;" />
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'''MUTANT HUMAN THYMIDYLATE KINASE COMPLEXED WITH TMP AND APPNP'''<br />
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{{Structure
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|PDB= 1e9c |SIZE=350|CAPTION= <scene name='initialview01'>1e9c</scene>, resolution 1.6&Aring;
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|SITE= <scene name='pdbsite=TMP:Anp+Binding+Site'>TMP</scene>
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=TMP:THYMIDINE-5'-PHOSPHATE'>TMP</scene> and <scene name='pdbligand=ADP:ADENOSINE-5'-DIPHOSPHATE'>ADP</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/dTMP_kinase dTMP kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.4.9 2.7.4.9]
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|GENE=
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}}
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'''MUTANT HUMAN THYMIDYLATE KINASE COMPLEXED WITH TMP AND APPNP'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1E9C is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=TMP:'>TMP</scene> and <scene name='pdbligand=ADP:'>ADP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/dTMP_kinase dTMP kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.4.9 2.7.4.9] Known structural/functional Site: <scene name='pdbsite=TMP:Anp+Binding+Site'>TMP</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1E9C OCA].
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1E9C is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1E9C OCA].
==Reference==
==Reference==
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Potentiating AZT activation: structures of wild-type and mutant human thymidylate kinase suggest reasons for the mutants' improved kinetics with the HIV prodrug metabolite AZTMP., Ostermann N, Lavie A, Padiyar S, Brundiers R, Veit T, Reinstein J, Goody RS, Konrad M, Schlichting I, J Mol Biol. 2000 Nov 17;304(1):43-53. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11071809 11071809]
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Potentiating AZT activation: structures of wild-type and mutant human thymidylate kinase suggest reasons for the mutants' improved kinetics with the HIV prodrug metabolite AZTMP., Ostermann N, Lavie A, Padiyar S, Brundiers R, Veit T, Reinstein J, Goody RS, Konrad M, Schlichting I, J Mol Biol. 2000 Nov 17;304(1):43-53. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11071809 11071809]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: thymidylate kinase]]
[[Category: thymidylate kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:25:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 10:52:02 2008''

Revision as of 08:52, 20 March 2008

Image:1e9c.jpg


PDB ID 1e9c

Drag the structure with the mouse to rotate
, resolution 1.6Å
Sites:
Ligands: , and
Activity: dTMP kinase, with EC number 2.7.4.9
Coordinates: save as pdb, mmCIF, xml



MUTANT HUMAN THYMIDYLATE KINASE COMPLEXED WITH TMP AND APPNP


Overview

The 60-fold reduced phosphorylation rate of azidothymidine (AZT) monophosphate (AZTMP), the partially activated AZT metabolite, by human thymidylate kinase (TMPK) severely limits the efficacy of this anti-HIV prodrug. Crystal structures of different TMPK nucleotide complexes indicate that steric hindrance by the azido group of AZTMP prevents formation of the catalytically active closed conformation of the P-loop of TMPK. The F105Y mutant and a chimeric mutant that contains sequences of the human and Escherichia coli enzyme phosphorylate AZTMP 20-fold faster than the wild-type enzyme. The structural basis of the increased activity is assigned to stabilization of the closed P-loop conformation.

About this Structure

1E9C is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potentiating AZT activation: structures of wild-type and mutant human thymidylate kinase suggest reasons for the mutants' improved kinetics with the HIV prodrug metabolite AZTMP., Ostermann N, Lavie A, Padiyar S, Brundiers R, Veit T, Reinstein J, Goody RS, Konrad M, Schlichting I, J Mol Biol. 2000 Nov 17;304(1):43-53. PMID:11071809

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