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

…, LG Korotchkina, S Chakraborty, MS Patel, F Jordan

文献索引：Nemeria, Natalia S.; Korotchkina, Lioubov G.; Chakraborty, Sumit; Patel, Mulchand S.; Jordan, Frank Bioorganic Chemistry, 2006 , vol. 34, # 6 p. 362 - 379

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被引用次数: 25

摘要

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 instance of such studies on the human enzyme. The acetylphosphinate is a stronger inhibitor of both enzymes (Ki< 1μM) than acetylmethylphosphinate. Both inhibitors are found to be reversible tight-binding inhibitors ...