1337912-77-2Relevant articles and documents
7-Substituted pterins provide a new direction for ricin A chain inhibitors
Pruet, Jeff M.,Jasheway, Karl R.,Manzano, Lawrence A.,Bai, Yan,Anslyn, Eric V.,Robertus, Jon D.
, p. 3608 - 3615 (2011)
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.
