2z3s: Difference between revisions
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==NMR structure of AgTx2-MTX== | |||
<StructureSection load='2z3s' size='340' side='right'caption='[[2z3s]]' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2z3s]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Z3S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Z3S FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</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=2z3s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2z3s OCA], [https://pdbe.org/2z3s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2z3s RCSB], [https://www.ebi.ac.uk/pdbsum/2z3s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2z3s ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Agitoxin 2 (AgTx2) is a 38-residue scorpion toxin, cross-linked by three disulfide bridges, which acts on voltage-gated K(+) (Kv) channels. Maurotoxin (MTX) is a 34-residue scorpion toxin with an uncommon four-disulfide bridge reticulation, acting on both Ca(2+)-activated and Kv channels. A 39-mer chimeric peptide, named AgTx2-MTX, was designed from the sequence of the two toxins and chemically synthesized. It encompasses residues 1-5 of AgTx2, followed by the complete sequence of MTX. As established by enzyme cleavage, the new AgTx2-MTX molecule displays half-cystine pairings of the type C1-C5, C2-C6, C3-C7, and C4-C8, which is different from that of MTX. The 3D structure of AgTx2-MTX solved by (1)H-NMR, revealed both alpha-helical and beta-sheet structures, consistent with a common alpha/beta scaffold of scorpion toxins. Pharmacological assays of AgTx2-MTX revealed that this new molecule is more potent than both original toxins in blocking rat Kv1.2 channel. Docking simulations, performed with the 3D structure of AgTx2-MTX, confirmed this result and demonstrated the participation of the N-terminal domain of AgTx2 in its increased affinity for Kv1.2 through additional molecular contacts. Altogether, the data indicated that replacement of the N-terminal domain of MTX by the one of AgTx2 in the AgTx2-MTX chimera results in a reorganization of the disulfide bridge arrangement and an increase of affinity to the Kv1.2 channel. | |||
Chemical synthesis and 1H-NMR 3D structure determination of AgTx2-MTX chimera, a new potential blocker for Kv1.2 channel, derived from MTX and AgTx2 scorpion toxins.,Pimentel C, M'Barek S, Visan V, Grissmer S, Sampieri F, Sabatier JM, Darbon H, Fajloun Z Protein Sci. 2008 Jan;17(1):107-18. Epub 2007 Nov 27. PMID:18042681<ref>PMID:18042681</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 2z3s" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
== | __TOC__ | ||
< | </StructureSection> | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: Darbon | [[Category: Darbon H]] | ||
[[Category: Fajloun | [[Category: Fajloun Z]] | ||
[[Category: Grissmer | [[Category: Grissmer S]] | ||
[[Category: M'Barrek S]] | |||
[[Category: | [[Category: Pimentel C]] | ||
[[Category: | [[Category: Sabatier JM]] | ||
[[Category: | [[Category: Visan V]] | ||
[[Category: | |||
Latest revision as of 08:41, 30 October 2024
NMR structure of AgTx2-MTX
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