1rd9: Difference between revisions

Revision as of 07:21, 3 May 2008

Cholera Toxin B-Pentamer Complexed With Bivalent Nitrophenol-Galactoside Ligand BV2

OverviewOverview

A series of bivalent ligands of varying length were synthesized to inhibit the receptor-binding process of cholera toxin. Competitive surface receptor binding assays showed that significant potency gains relative to the constituent monovalent ligands were achieved independently from the ability of the extended bivalent ligands to span binding sites within the toxin pentamer. Several models that could account for the unexpected improvement in IC(50) values are examined, taking into account crystallographic analysis of each ligand in complex with the toxin pentamer. Evidence is presented that steric blocking at the receptor binding surface may play a role. The results of our study suggest that the use of relatively short, "nonspanning" bivalent ligands, or monovalent ligands of similar topology and bulk may be an effective way of blocking the interaction of multimeric proteins with their cell surface receptors.

About this StructureAbout this Structure

1RD9 is a Single protein structure of sequence from Vibrio cholerae. Full crystallographic information is available from OCA.

ReferenceReference

Nonspanning bivalent ligands as improved surface receptor binding inhibitors of the cholera toxin B pentamer., Pickens JC, Mitchell DD, Liu J, Tan X, Zhang Z, Verlinde CL, Hol WG, Fan E, Chem Biol. 2004 Sep;11(9):1205-15. PMID:15380181 Page seeded by OCA on Sat May 3 07:21:25 2008

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OCA

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 [[Image:1rd9.jpg|left|200px]]
- {{Structure
+<!--
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+The line below this paragraph, containing "STRUCTURE_1rd9", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=BV2:1,3-BIS-([3-(4-{3-[3-NITRO-5-(GALACTOPYRANOSYLOXY)-BENZOYLAMINO]-PROPYL}-PIPERAZIN-1-YL)-PROPYL-AMINO]-CARBONYLOXY)-2-AMINO-PROPANE'>BV2</scene>, <scene name='pdbligand=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</scene>
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-|GENE= ctxB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=666 Vibrio cholerae])
+-->
-|DOMAIN=
+{{STRUCTURE_1rd9|  PDB=1rd9  |  SCENE=  }}
-|RELATEDENTRY=[[1rcv|1RCV]], [[1rdp|1RDP]], [[1rf2|1RF2]]
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1rd9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1rd9 OCA], [http://www.ebi.ac.uk/pdbsum/1rd9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1rd9 RCSB]</span>
-}}
 '''Cholera Toxin B-Pentamer Complexed With Bivalent Nitrophenol-Galactoside Ligand BV2'''
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 [[Category: Verlinde, C L.]]
 [[Category: Zhang, Z.]]
-[[Category: bivalent]]
+[[Category: Bivalent]]
-[[Category: cholera]]
+[[Category: Cholera]]
-[[Category: complex]]
+[[Category: Complex]]
-[[Category: pentamer]]
+[[Category: Pentamer]]
-[[Category: toxin]]
+[[Category: Toxin]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 07:21:25 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:26:29 2008''