Progress in the discovery of inhibitors of LTA ₄ hydrolase

This Monthly Update summarizes current research In the development of inhibitors of the enzyme LTA 4 hydrolase. LTA 4 hydrolase (EC 3.3.2.6) converts the reactive epoxide LTA 4 into the proinflam-matory dihydroxyeicosanoid, LTB 4 , by a stereoselective addition of a water molecule. Inhibition of LTA 4 hydrolase may offer benefit to diseases Involving a predominant LTB4 pathological component. The interesting inhibitors reported by researchers at Scripps Research Institute, Karolinska Institute, and Rhfine-Poulenc Rorer provide the basis for further advances to maximize potency, oral bioavailability and duration of action of this class of leukotriene inhibitors.