1y4l

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[[Image:1y4l.gif|left|200px]]<br /><applet load="1y4l" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1y4l.gif|left|200px]]
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caption="1y4l, resolution 1.70&Aring;" />
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'''Crystal structure of Bothrops asper myotoxin II complexed with the anti-trypanosomal drug suramin'''<br />
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{{Structure
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|PDB= 1y4l |SIZE=350|CAPTION= <scene name='initialview01'>1y4l</scene>, resolution 1.70&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=SVR:8,8'-[CARBONYLBIS[IMINO-3,1-PHENYLENECARBONYLIMINO(4-METHYL-3,1-PHENYLENE)CARBONYLIMINO]]BIS-1,3,5-NAPHTHALENETRISULFONIC+ACID'>SVR</scene>, <scene name='pdbligand=P33:3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL'>P33</scene> and <scene name='pdbligand=IPA:ISOPROPYL ALCOHOL'>IPA</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Phospholipase_A(2) Phospholipase A(2)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.4 3.1.1.4]
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|GENE=
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}}
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'''Crystal structure of Bothrops asper myotoxin II complexed with the anti-trypanosomal drug suramin'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1Y4L is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bothrops_asper Bothrops asper] with <scene name='pdbligand=SVR:'>SVR</scene>, <scene name='pdbligand=P33:'>P33</scene> and <scene name='pdbligand=IPA:'>IPA</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phospholipase_A(2) Phospholipase A(2)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.4 3.1.1.4] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y4L OCA].
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1Y4L is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Bothrops_asper Bothrops asper]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y4L OCA].
==Reference==
==Reference==
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Inhibition of myotoxic activity of Bothrops asper myotoxin II by the anti-trypanosomal drug suramin., Murakami MT, Arruda EZ, Melo PA, Martinez AB, Calil-Elias S, Tomaz MA, Lomonte B, Gutierrez JM, Arni RK, J Mol Biol. 2005 Jul 15;350(3):416-26. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15961104 15961104]
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Inhibition of myotoxic activity of Bothrops asper myotoxin II by the anti-trypanosomal drug suramin., Murakami MT, Arruda EZ, Melo PA, Martinez AB, Calil-Elias S, Tomaz MA, Lomonte B, Gutierrez JM, Arni RK, J Mol Biol. 2005 Jul 15;350(3):416-26. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15961104 15961104]
[[Category: Bothrops asper]]
[[Category: Bothrops asper]]
[[Category: Phospholipase A(2)]]
[[Category: Phospholipase A(2)]]
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[[Category: bothrops asper myotoxin ii]]
[[Category: bothrops asper myotoxin ii]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:01:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:18:20 2008''

Revision as of 13:18, 20 March 2008


PDB ID 1y4l

Drag the structure with the mouse to rotate
, resolution 1.70Å
Ligands: , and
Activity: Phospholipase A(2), with EC number 3.1.1.4
Coordinates: save as pdb, mmCIF, xml



Crystal structure of Bothrops asper myotoxin II complexed with the anti-trypanosomal drug suramin


Overview

Suramin, a synthetic polysulfonated compound, developed initially for the treatment of African trypanosomiasis and onchocerciasis, is currently used for the treatment of several medically relevant disorders. Suramin, heparin, and other polyanions inhibit the myotoxic activity of Lys49 phospholipase A2 analogues both in vitro and in vivo, and are thus of potential importance as therapeutic agents in the treatment of viperid snake bites. Due to its conformational flexibility around the single bonds that link the central phenyl rings to the secondary amide backbone, the symmetrical suramin molecule binds by an induced-fit mechanism complementing the hydrophobic surfaces of the dimer and adopts a novel conformation that lacks C2 symmetry in the dimeric crystal structure of the suramin-Bothrops asper myotoxin II complex. The simultaneous binding of suramin at the surfaces of the two monomers partially restricts access to the nominal active sites and significantly changes the overall charge of the interfacial recognition face of the protein, resulting in the inhibition of myotoxicity.

About this Structure

1Y4L is a Single protein structure of sequence from Bothrops asper. Full crystallographic information is available from OCA.

Reference

Inhibition of myotoxic activity of Bothrops asper myotoxin II by the anti-trypanosomal drug suramin., Murakami MT, Arruda EZ, Melo PA, Martinez AB, Calil-Elias S, Tomaz MA, Lomonte B, Gutierrez JM, Arni RK, J Mol Biol. 2005 Jul 15;350(3):416-26. PMID:15961104

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