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ID: ALA1821685
Journal: Eur J Med Chem
Title: 7-Substituted pterins provide a new direction for ricin A chain inhibitors.
Authors: Pruet JM, Jasheway KR, Manzano LA, Bai Y, Anslyn EV, Robertus JD.
Abstract: 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.
CiteXplore: 21641093