1tco

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[[Image:1tco.gif|left|200px]]<br /><applet load="1tco" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1tco.gif|left|200px]]
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caption="1tco, resolution 2.5&Aring;" />
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'''TERNARY COMPLEX OF A CALCINEURIN A FRAGMENT, CALCINEURIN B, FKBP12 AND THE IMMUNOSUPPRESSANT DRUG FK506 (TACROLIMUS)'''<br />
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{{Structure
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|PDB= 1tco |SIZE=350|CAPTION= <scene name='initialview01'>1tco</scene>, resolution 2.5&Aring;
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|SITE= <scene name='pdbsite=506:The+Fk506+Binding+Site+On+Fkbp12+(Subunit+C)+As+Well+As+...'>506</scene>
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|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=FE:FE+(III)+ION'>FE</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=MYR:MYRISTIC+ACID'>MYR</scene> and <scene name='pdbligand=FK5:8-DEETHYL-8-[BUT-3-ENYL]-ASCOMYCIN'>FK5</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Phosphoprotein_phosphatase Phosphoprotein phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.16 3.1.3.16]
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|GENE=
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}}
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'''TERNARY COMPLEX OF A CALCINEURIN A FRAGMENT, CALCINEURIN B, FKBP12 AND THE IMMUNOSUPPRESSANT DRUG FK506 (TACROLIMUS)'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1TCO is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=CA:'>CA</scene>, <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=FE:'>FE</scene>, <scene name='pdbligand=PO4:'>PO4</scene>, <scene name='pdbligand=MYR:'>MYR</scene> and <scene name='pdbligand=FK5:'>FK5</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phosphoprotein_phosphatase Phosphoprotein phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.16 3.1.3.16] Known structural/functional Site: <scene name='pdbsite=506:The+Fk506+Binding+Site+On+Fkbp12+(Subunit+C)+As+Well+As+...'>506</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TCO OCA].
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1TCO is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TCO OCA].
==Reference==
==Reference==
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X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex., Griffith JP, Kim JL, Kim EE, Sintchak MD, Thomson JA, Fitzgibbon MJ, Fleming MA, Caron PR, Hsiao K, Navia MA, Cell. 1995 Aug 11;82(3):507-22. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=7543369 7543369]
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X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex., Griffith JP, Kim JL, Kim EE, Sintchak MD, Thomson JA, Fitzgibbon MJ, Fleming MA, Caron PR, Hsiao K, Navia MA, Cell. 1995 Aug 11;82(3):507-22. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/7543369 7543369]
[[Category: Bos taurus]]
[[Category: Bos taurus]]
[[Category: Phosphoprotein phosphatase]]
[[Category: Phosphoprotein phosphatase]]
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[[Category: immunosuppressant]]
[[Category: immunosuppressant]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:12:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:16:39 2008''

Revision as of 12:16, 20 March 2008


PDB ID 1tco

Drag the structure with the mouse to rotate
, resolution 2.5Å
Sites:
Ligands: , , , , and
Activity: Phosphoprotein phosphatase, with EC number 3.1.3.16
Coordinates: save as pdb, mmCIF, xml



TERNARY COMPLEX OF A CALCINEURIN A FRAGMENT, CALCINEURIN B, FKBP12 AND THE IMMUNOSUPPRESSANT DRUG FK506 (TACROLIMUS)


Overview

The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. In the structure, the FKBP12-FK506 binary complex does not contact the phosphatase active site on calcineurin A that is more than 10 A removed. Instead, FKBP12-FK506 is so positioned that it can inhibit the dephosphorylation of its macromolecular substrates by physically hindering their approach to the active site. The ternary complex described here represents the three-dimensional structure of a Ser/Thr protein phosphatase and provides a structural basis for understanding calcineurin inhibition by FKBP12-FK506.

About this Structure

1TCO is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex., Griffith JP, Kim JL, Kim EE, Sintchak MD, Thomson JA, Fitzgibbon MJ, Fleming MA, Caron PR, Hsiao K, Navia MA, Cell. 1995 Aug 11;82(3):507-22. PMID:7543369

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