3w0l

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The crystal structure of Xenopus Glucokinase and Glucokinase Regulatory Protein complex

Structural highlights

3w0l is a 4 chain structure with sequence from Xenopus laevis. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.92Å
Ligands:F6R, NA, SO4
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

GCKR_XENLA Inhibits glucokinase by forming an inactive complex with this enzyme.

Publication Abstract from PubMed

Glucokinase (GK) is a monomeric allosteric enzyme and plays a pivotal role in blood glucose homeostasis. GK is regulated by GK regulatory protein (GKRP), and indirectly by allosteric effectors of GKRP. Despite the critical roles of GK and GKRP, the molecular basis for the allosteric regulation mechanism of GK by GKRP remains unclear. We determined the crystal structure of Xenopus GK and GKRP complex in the presence of fructose-6-phosphate at 2.9 A. GKRP binds to a super-open conformation of GK mainly through hydrophobic interaction, inhibiting the GK activity by locking a small domain of GK. We demonstrate the molecular mechanism for the modulation of GK activity by allosteric effectors of GKRP. Importantly, GKRP releases GK in a sigmoidal manner in response to glucose concentration by restricting a structural rearrangement of the GK small domain via a single ion pair. We find that GKRP acts as an allosteric switch for GK in blood glucose control by the liver.

Molecular basis for the role of glucokinase regulatory protein as the allosteric switch for glucokinase.,Choi JM, Seo MH, Kyeong HH, Kim E, Kim HS Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):10171-6. doi:, 10.1073/pnas.1300457110. Epub 2013 Jun 3. PMID:23733961[1]

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

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Citations
11 reviews cite this structure
Glucokinase regulatory protein: complexity at the crossroads of triglyceride and glucose metabolism.
Raimondo et al. (2015)
10 more
27 other articles
No citations found

See Also

References

  1. ↑ Choi JM, Seo MH, Kyeong HH, Kim E, Kim HS. Molecular basis for the role of glucokinase regulatory protein as the allosteric switch for glucokinase. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):10171-6. doi:, 10.1073/pnas.1300457110. Epub 2013 Jun 3. PMID:23733961 doi:10.1073/pnas.1300457110

Contents


PDB ID 3w0l

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OCA

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