1mkd

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[[Image:1mkd.gif|left|200px]]
[[Image:1mkd.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1mkd |SIZE=350|CAPTION= <scene name='initialview01'>1mkd</scene>, resolution 2.90&Aring;
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The line below this paragraph, containing "STRUCTURE_1mkd", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZAR:6-(4-DIFLUOROMETHOXY-3-METHOXY-PHENYL)-2H-PYRIDAZIN-3-ONE'>ZAR</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1mkd| PDB=1mkd | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1mkd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mkd OCA], [http://www.ebi.ac.uk/pdbsum/1mkd PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1mkd RCSB]</span>
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}}
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'''crystal structure of PDE4D catalytic domain and zardaverine complex'''
'''crystal structure of PDE4D catalytic domain and zardaverine complex'''
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[[Category: Lee, M E.]]
[[Category: Lee, M E.]]
[[Category: Markowitz, J.]]
[[Category: Markowitz, J.]]
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[[Category: pde]]
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[[Category: Pde]]
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[[Category: zardaverine]]
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[[Category: Zardaverine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:17:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:17:11 2008''
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Revision as of 22:17, 2 May 2008

Image:1mkd.gif

Template:STRUCTURE 1mkd

crystal structure of PDE4D catalytic domain and zardaverine complex


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.

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 Page seeded by OCA on Sat May 3 01:17:12 2008

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