3px8

RTA in complex with 7-carboxy-pterin

spinqualitylabelsall models 3px8, resolution 1.29Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3px8 is a 1 chain structure with sequence from Castor bean. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: JP2 Related: 3px9 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Ricin

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