3odv

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X-ray structure of kaliotoxin by racemic protein crystallographyX-ray structure of kaliotoxin by racemic protein crystallography

Structural highlights

3odv is a 2 chain structure with sequence from Androctonus mauritanicus mauritanicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 0.95Å
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

KAX31_ANDMA Potent inhibitor of large conductance calcium-activated potassium channels (BK-Ca). Also binds to the dendrotoxin sensitive voltage-dependent potassium channel. It appears to block channel activity by a simple bimolecular inhibition process. Induces a transient period of fast flickering in the channel openings, followed by an almost complete blockade of the channel. Its binding affinity to rat brain synaptosomes is 5-fold higher than this of KTX-3. Binding of the toxin to the channel is associated with significant structural rearrangements in both molecules.

Publication Abstract from PubMed

Here we report the total synthesis of kaliotoxin by 'one pot' native chemical ligation of three synthetic peptides. A racemic mixture of d- and l-kaliotoxin synthetic protein molecules gave crystals in the centrosymmetric space group P1[combining macron] that diffracted to atomic-resolution (0.95 A), enabling the X-ray structure of kaliotoxin to be determined by direct methods.

Total chemical synthesis and X-ray structure of kaliotoxin by racemic protein crystallography.,Pentelute BL, Mandal K, Gates ZP, Sawaya MR, Yeates TO, Kent SB Chem Commun (Camb). 2010 Sep 28. PMID:20877851[1]

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

See Also

References

  1. Pentelute BL, Mandal K, Gates ZP, Sawaya MR, Yeates TO, Kent SB. Total chemical synthesis and X-ray structure of kaliotoxin by racemic protein crystallography. Chem Commun (Camb). 2010 Sep 28. PMID:20877851 doi:10.1039/c0cc03148h

3odv, resolution 0.95Å

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