ATP-citrate-lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-. beta.-lactam containing analogs of citric acid as potential tight-binding …

RE Dolle, D McNair, MJ Hughes, LI Kruse…

Index: Dolle; McNair; Hughes; Kruse; Eggelston; Saxty; Wells; Groot Journal of Medicinal Chemistry, 1992 , vol. 35, # 26 p. 4875 - 4884

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Citation Number: 13

Abstract

Citric acid analogues (&)-12a, b and (&)-17a, b, where one of the primary carboxylates has been replaced by a sulfoximinoyl and a 3-(3-hydroxy-fl-lactamyl) moiety, respectively, have been synthesized and evaluated as inhibitors of ATP-citrate lyase. The design of these inhibitors was based on methionine sulfoximine and tabtoxinine &lactam, potent, tight- binding inhibitors of glutamine synthetase. Both ATP-citrate lyase and glutamine ...