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[[ | ==RTA in complex with N-(furanylmethyl)-7-carbamoyl-pterin== | ||
<StructureSection load='3px9' size='340' side='right' caption='[[3px9]], [[Resolution|resolution]] 1.89Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3px9]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Ricinus_communis Ricinus communis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PX9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PX9 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=JP3:2-AMINO-N-(FURAN-2-YLMETHYL)-4-OXO-3,4-DIHYDROPTERIDINE-7-CARBOXAMIDE'>JP3</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3px8|3px8]]</td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3px9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3px9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3px9 RCSB], [http://www.ebi.ac.uk/pdbsum/3px9 PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Ricin is a potent toxin found in castor seeds. The A chain, RTA, enzymaticlly depurinates a specific adenosine in ribosomal RNA, inhibiting protein synthesis. Ricin is a known chemical weapons threat having no effective antidote. This makes the discovery of new inhibitors of great importance. We have previously used 6-substituted pterins, such as pteroic acid, as an inhibitor platform with moderate success. We now report the success of 7-carboxy pterin (7CP) as an RTA inhibitor; its binding has been monitored using both kinetic and temperature shift assays and by X-ray crystallography. We also discuss the synthesis of various derivatives of 7CP, and their binding affinity and inhibitory effects, as part of a program to make effective RTA inhibitors. | |||
7-Substituted pterins provide a new direction for ricin A chain inhibitors.,Pruet JM, Jasheway KR, Manzano LA, Bai Y, Anslyn EV, Robertus JD Eur J Med Chem. 2011 May 20. PMID:21641093<ref>PMID:21641093</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
==See Also== | ==See Also== | ||
*[[Ricin|Ricin]] | *[[Ricin|Ricin]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
</StructureSection> | |||
[[Category: Ricinus communis]] | [[Category: Ricinus communis]] | ||
[[Category: Jasheway, K R | [[Category: Jasheway, K R]] | ||
[[Category: Robertus, J D | [[Category: Robertus, J D]] | ||
[[Category: Hydrolase]] | [[Category: Hydrolase]] | ||
[[Category: Hydrolase-inhibitor complex]] | [[Category: Hydrolase-inhibitor complex]] | ||
Revision as of 14:16, 9 December 2014
RTA in complex with N-(furanylmethyl)-7-carbamoyl-pterinRTA in complex with N-(furanylmethyl)-7-carbamoyl-pterin
Structural highlights
Publication Abstract from PubMedRicin is a potent toxin found in castor seeds. The A chain, RTA, enzymaticlly depurinates a specific adenosine in ribosomal RNA, inhibiting protein synthesis. Ricin is a known chemical weapons threat having no effective antidote. This makes the discovery of new inhibitors of great importance. We have previously used 6-substituted pterins, such as pteroic acid, as an inhibitor platform with moderate success. We now report the success of 7-carboxy pterin (7CP) as an RTA inhibitor; its binding has been monitored using both kinetic and temperature shift assays and by X-ray crystallography. We also discuss the synthesis of various derivatives of 7CP, and their binding affinity and inhibitory effects, as part of a program to make effective RTA inhibitors. 7-Substituted pterins provide a new direction for ricin A chain inhibitors.,Pruet JM, Jasheway KR, Manzano LA, Bai Y, Anslyn EV, Robertus JD Eur J Med Chem. 2011 May 20. PMID:21641093[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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