Acetylphosphinate is the most potent mechanism-based substrate-like inhibitor of both the human and Escherichia coli pyruvate dehydrogenase components of the pyruvate dehydrogenase complex

Formation of LThDP and its phosphonate and phosphinate analogues. Two analogues of pyruvate, acetylphosphinate and acetylmethylphosphinate were tested as inhibitors of the E1 (pyruvate dehydrogenase) component of the human and Escherichia coli pyruvate dehydrogenase complexes. This is the first inst...

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Veröffentlicht in:	Bioorganic chemistry 2006-12, Vol.34 (6), p.362-379
Hauptverfasser:	Nemeria, Natalia S., Korotchkina, Lioubov G., Chakraborty, Sumit, Patel, Mulchand S., Jordan, Frank
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetoin Acetylmethylphosphinate Acetylphosphinate Acetylphosphonate methyl ester Circular Dichroism Enzyme Inhibitors Escherichia coli Escherichia coli Proteins - antagonists & inhibitors Escherichia coli pyruvate dehydrogenase complex Human pyruvate dehydrogenase complex Humans Ketone Oxidoreductases - antagonists & inhibitors Ketone Oxidoreductases - metabolism Kinetics Mechanism-based inhibition Multienzyme Complexes Phosphinic Acids - pharmacology Thiamin 2-thiothia zolone diphosphate Thiamin diphosphate Titrimetry
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