1mkd

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[[Image:1mkd.gif|left|200px]]<br /><applet load="1mkd" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1mkd.gif|left|200px]]
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caption="1mkd, resolution 2.90&Aring;" />
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'''crystal structure of PDE4D catalytic domain and zardaverine complex'''<br />
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{{Structure
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|PDB= 1mkd |SIZE=350|CAPTION= <scene name='initialview01'>1mkd</scene>, resolution 2.90&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=ZAR:6-(4-DIFLUOROMETHOXY-3-METHOXY-PHENYL)-2H-PYRIDAZIN-3-ONE'>ZAR</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17]
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|GENE=
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}}
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'''crystal structure of PDE4D catalytic domain and zardaverine complex'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1MKD 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=ZN:'>ZN</scene>, <scene name='pdbligand=MG:'>MG</scene> and <scene name='pdbligand=ZAR:'>ZAR</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MKD OCA].
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1MKD 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=1MKD OCA].
==Reference==
==Reference==
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Crystal structure of phosphodiesterase 4D and inhibitor complex(1)., Lee ME, Markowitz J, Lee JO, Lee H, FEBS Lett. 2002 Oct 23;530(1-3):53-8. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12387865 12387865]
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Crystal structure of phosphodiesterase 4D and inhibitor complex(1)., Lee ME, Markowitz J, Lee JO, Lee H, FEBS Lett. 2002 Oct 23;530(1-3):53-8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12387865 12387865]
[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: zardaverine]]
[[Category: zardaverine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:56:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:44:30 2008''

Revision as of 10:44, 20 March 2008

Image:1mkd.gif


PDB ID 1mkd

Drag the structure with the mouse to rotate
, resolution 2.90Å
Ligands: , and
Activity: 3',5'-cyclic-nucleotide phosphodiesterase, with EC number 3.1.4.17
Coordinates: save as pdb, mmCIF, xml



crystal structure of PDE4D catalytic domain and zardaverine complex


Contents

Overview

Cyclic nucleotide phosphodiesterases (PDEs) regulate physiological processes by degrading intracellular second messengers, adenosine-3',5'-cyclic phosphate or guanosine-3',5'-cyclic phosphate. The first crystal structure of PDE4D catalytic domain and a bound inhibitor, zardaverine, was determined. Zardaverine binds to a highly conserved pocket that includes the catalytic metal binding site. Zardaverine fills only a portion of the active site pocket. More selective PDE4 inhibitors including rolipram, cilomilast and roflumilast have additional functional groups that can utilize the remaining empty space for increased binding energy and selectivity. In the crystal structure, the catalytic domain of PDE4D possesses an extensive dimerization interface containing residues that are highly conserved in PDE1, 3, 4, 8 and 9. Mutations of R358D or D322R among these interface residues prohibit dimerization of the PDE4D catalytic domain in solution.

Disease

Known disease associated with this structure: Stroke, susceptibility to, 1 OMIM:[600129]

About this Structure

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

Reference

Crystal structure of phosphodiesterase 4D and inhibitor complex(1)., Lee ME, Markowitz J, Lee JO, Lee H, FEBS Lett. 2002 Oct 23;530(1-3):53-8. PMID:12387865

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