1tco

From Proteopedia

Revision as of 15:00, 5 November 2007

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 CA, ZN, FE, PO4, MYR and FK5 as ligands. Active as Phosphoprotein phosphatase, with EC number 3.1.3.16 Structure known Active Site: 506. 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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