1a7x

From Proteopedia

FKBP12-FK1012 COMPLEX

Structural highlights

1a7x is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2Å
Ligands:	FKA
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

FKB1A_HUMAN Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand. Recruites SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. May modulate the RYR1 calcium channel activity. PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides.^[1] ^[2]

Evolutionary Conservation

Checkto colour the structure by Evolutionary Conservation, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

A ligand that simultaneously binds two proteins must have two high affinity protein binding domains joined in a fashion that facilitates, or at least does not prevent, protein-protein interaction. Designing such ligands is challenging, and a high resolution X-ray structure of FKBP12-FK1012A-FKBP12 illustrates the subtleties of one successful design.

Chemical inducers of dimerization: the atomic structure of FKBP12-FK1012A-FKBP12.,Schultz LW, Clardy J Bioorg Med Chem Lett. 1998 Jan 6;8(1):1-6. PMID:9871618^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations

2 reviews cite this structure

Targeting protein function: the expanding toolkit for conditional disruption.

Campbell et al. (2016)

1 more

5 other articles

No citations found

References

↑ Chen YG, Liu F, Massague J. Mechanism of TGFbeta receptor inhibition by FKBP12. EMBO J. 1997 Jul 1;16(13):3866-76. PMID:9233797 doi:10.1093/emboj/16.13.3866
↑ Yamaguchi T, Kurisaki A, Yamakawa N, Minakuchi K, Sugino H. FKBP12 functions as an adaptor of the Smad7-Smurf1 complex on activin type I receptor. J Mol Endocrinol. 2006 Jun;36(3):569-79. PMID:16720724 doi:10.1677/jme.1.01966
↑ Schultz LW, Clardy J. Chemical inducers of dimerization: the atomic structure of FKBP12-FK1012A-FKBP12. Bioorg Med Chem Lett. 1998 Jan 6;8(1):1-6. PMID:9871618

1 Structural highlights
2 Function
3 Evolutionary Conservation
4 Publication Abstract from PubMed
5 See Also
6 References

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PDB ID 1a7x

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Categories: Homo sapiens | Large Structures | Clardy J | Schultz LW

1a7x

From Proteopedia

FKBP12-FK1012 COMPLEX

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

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