3px9

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^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.