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2k4u

From Proteopedia

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Solution structure of the SCORPION TOXIN ADWX-1

Structural highlights

2k4u is a 1 chain structure with sequence from Buthus martensi. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[KAX36_MESMA] Blocks voltage-gated potassium channels. At 2 uM, blocks rat Kv1.1/KCNA1 and Kv1.3/KCNA3, has a strong effect on rat Kv1.2/KCNA2 and Kv1.6/KCNA6 as well as a moderate effect on Shaker IR.^[1] ^[2]

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

The low selectivity of Kv1 peptide inhibitors for specific isoforms makes them poor candidates for the development of theraputics. Using combined approaches, we showed that the Kv1 turret is the critical determinant for ADWX-1 peptide inhibitor selectivity of Kv1.3 over Kv1.1. Mutation of Kv1.1 turret residues to match the sequence of Kv1.3 lead to increased inhibition of Kv1.1 activity. These studies may lead to improvements in peptide inhibitor drug development.

Different Residues in Channel Turret Determining the Selectivity of ADWX-1 Inhibitor Peptide between Kv1.1 and Kv1.3 Channels.,Yin SJ, Jiang L, Yi H, Han S, Yang DW, Liu ML, Liu H, Cao ZJ, Wu YL, Li WX J Proteome Res. 2008 Nov 7;7(11):4890-4897. Epub 2008 Oct 21. PMID:18937510^[3]

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

References

↑ Romi-Lebrun R, Lebrun B, Martin-Eauclaire MF, Ishiguro M, Escoubas P, Wu FQ, Hisada M, Pongs O, Nakajima T. Purification, characterization, and synthesis of three novel toxins from the Chinese scorpion Buthus martensi, which act on K+ channels. Biochemistry. 1997 Nov 4;36(44):13473-82. PMID:9354615 doi:http://dx.doi.org/10.1021/bi971044w
↑ Gao B, Peigneur S, Tytgat J, Zhu S. A potent potassium channel blocker from Mesobuthus eupeus scorpion venom. Biochimie. 2010 Dec;92(12):1847-53. doi: 10.1016/j.biochi.2010.08.003. Epub 2010 , Aug 14. PMID:20713119 doi:http://dx.doi.org/10.1016/j.biochi.2010.08.003
↑ Yin SJ, Jiang L, Yi H, Han S, Yang DW, Liu ML, Liu H, Cao ZJ, Wu YL, Li WX. Different Residues in Channel Turret Determining the Selectivity of ADWX-1 Inhibitor Peptide between Kv1.1 and Kv1.3 Channels. J Proteome Res. 2008 Nov 7;7(11):4890-4897. Epub 2008 Oct 21. PMID:18937510 doi:http://dx.doi.org/10.1021/pr800494a

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2k4u"

@@ Line 3: / Line 3: @@
 <StructureSection load='2k4u' size='340' side='right'caption='[[2k4u]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2k4u]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Buthus_martensi Buthus martensi]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2K4U OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2K4U FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2k4u]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Buthus_martensi Buthus martensi]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2K4U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2K4U FirstGlance]. <br>
-</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2k4u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2k4u OCA], [http://pdbe.org/2k4u PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2k4u RCSB], [http://www.ebi.ac.uk/pdbsum/2k4u PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2k4u ProSAT]</span></td></tr>
+</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2k4u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2k4u OCA], [https://pdbe.org/2k4u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2k4u RCSB], [https://www.ebi.ac.uk/pdbsum/2k4u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2k4u ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://www.uniprot.org/uniprot/KAX36_MESMA KAX36_MESMA]] Blocks voltage-gated potassium channels. At 2 uM, blocks rat Kv1.1/KCNA1 and Kv1.3/KCNA3, has a strong effect on rat Kv1.2/KCNA2 and Kv1.6/KCNA6 as well as a moderate effect on Shaker IR.<ref>PMID:9354615</ref> <ref>PMID:20713119</ref>
+[[https://www.uniprot.org/uniprot/KAX36_MESMA KAX36_MESMA]] Blocks voltage-gated potassium channels. At 2 uM, blocks rat Kv1.1/KCNA1 and Kv1.3/KCNA3, has a strong effect on rat Kv1.2/KCNA2 and Kv1.6/KCNA6 as well as a moderate effect on Shaker IR.<ref>PMID:9354615</ref> <ref>PMID:20713119</ref>
 == Evolutionary Conservation ==
 [[Image:Consurf_key_small.gif|200px|right]]

2k4u

From Proteopedia

Current revision

Solution structure of the SCORPION TOXIN ADWX-1

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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