1tco
From Proteopedia
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==Overview== | ==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 | + | 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== | ==About this Structure== | ||
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[[Category: Phosphoprotein phosphatase]] | [[Category: Phosphoprotein phosphatase]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Caron, P | + | [[Category: Caron, P R.]] |
| - | [[Category: Fitzgibbon, M | + | [[Category: Fitzgibbon, M J.]] |
| - | [[Category: Fleming, M | + | [[Category: Fleming, M A.]] |
| - | [[Category: Griffith, J | + | [[Category: Griffith, J P.]] |
[[Category: Hsiao, K.]] | [[Category: Hsiao, K.]] | ||
| - | [[Category: Kim, E | + | [[Category: Kim, E E.]] |
| - | [[Category: Kim, J | + | [[Category: Kim, J L.]] |
| - | [[Category: Navia, M | + | [[Category: Navia, M A.]] |
| - | [[Category: Sintchak, M | + | [[Category: Sintchak, M D.]] |
| - | [[Category: Thomson, J | + | [[Category: Thomson, J A.]] |
[[Category: CA]] | [[Category: CA]] | ||
[[Category: FE]] | [[Category: FE]] | ||
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[[Category: immunosuppressant]] | [[Category: immunosuppressant]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:12:13 2008'' |
Revision as of 13:12, 21 February 2008
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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 with , , , , and as ligands. Active as Phosphoprotein phosphatase, with EC number 3.1.3.16 Known structural/functional Site: . 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
Page seeded by OCA on Thu Feb 21 15:12:13 2008
Categories: Bos taurus | Phosphoprotein phosphatase | Protein complex | Caron, P R. | Fitzgibbon, M J. | Fleming, M A. | Griffith, J P. | Hsiao, K. | Kim, E E. | Kim, J L. | Navia, M A. | Sintchak, M D. | Thomson, J A. | CA | FE | FK5 | MYR | PO4 | ZN | Complex (hydrolase/isomerase) | Immunosuppressant
