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1,3-Phenylene bis(ketoacid) derivatives as inhibitors of Escherichia coli dihydrodipicolinate synthase
Journal article   Peer reviewed

1,3-Phenylene bis(ketoacid) derivatives as inhibitors of Escherichia coli dihydrodipicolinate synthase

B.A. Boughton, L. Hor, J.A. Gerrard and C.A. Hutton
Bioorganic & Medicinal Chemistry, Vol.20(7), pp.2419-2426
2012
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Abstract

Dihydrodipicolinate synthase is a key enzyme in the lysine biosynthesis pathway that catalyzes the condensation of pyruvate and aspartate semi-aldehyde. A series of phenolic ketoacid derivatives that mimic the proposed enzymatic intermediate were designed as potential inhibitors of this enzyme and were synthesized from simple precursors. The ketoacid derivatives were shown to act as slow and slow-tight binding inhibitors. Mass spectrometric experiments provided further evidence to support the proposed model of inhibition, demonstrating either an encounter complex or a condensation product for the slow and slow-tight binding inhibitors, respectively.

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Collaboration types
Domestic collaboration
International collaboration
Citation topics
3 Agriculture, Environment & Ecology
3.180 Microbial Biotechnology
3.180.1184 Amino Acid Biosynthesis
Web Of Science research areas
Biochemistry & Molecular Biology
Chemistry, Medicinal
Chemistry, Organic
ESI research areas
Chemistry
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