Conformationally constrained diketopimelic acid analogues as inhibitors of dihydrodipicolinate synthase |
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Authors: | Boughton Berin A Dobson Renwick C J Gerrard Juliet A Hutton Craig A |
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Institution: | School of Chemistry, University of Melbourne, Vic. 3010, Australia. |
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Abstract: | Dihydrodipicolinate synthase (DHDPS) is a key enzyme in lysine biosynthesis and a potential antibiotic target. The enzyme catalyses the condensation of (S)-aspartate semi-aldehyde (ASA) and pyruvate to form dihydrodipicolinate. Constrained diketopimelic acid derivatives have been designed as mimics of the acyclic enzyme-bound condensation product of ASA and pyruvate. Several of the compounds are shown to be active, slow-binding inhibitors with improved inhibition of DHDPS. |
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