Levin L R, Kuret J, Johnson K E, Powers S, Cameron S, Michaeli T, Wigler M, Zoller M J
Cold Spring Harbor Laboratory, NY 11724.
Science. 1988 Apr 1;240(4848):68-70. doi: 10.1126/science.2832943.
A mutant catalytic subunit of adenosine 3',5'-monophosphate (cAMP)-dependent protein kinase has been isolated from Saccharomyces cerevisiae that is no longer subject to regulation yet retains its catalytic activity. Biochemical analysis of the mutant subunit indicates a 100-fold decreased affinity for the regulatory subunit. The mutant catalytic subunit exhibits approximately a threefold increase in Michaelis constant for adenosine triphosphate and peptide cosubstrates, and is essentially unchanged in its catalytic rate. The nucleotide sequence of the mutant gene contains a single nucleotide change resulting in a threonine-to-alanine substitution at amino acid 241. This residue is conserved in other serine-threonine protein kinases. These results identify this threonine as an important contact between catalytic and regulatory subunits but only a minor contact in substrate recognition.
已从酿酒酵母中分离出一种3',5'-环磷酸腺苷(cAMP)依赖性蛋白激酶的突变催化亚基,该亚基不再受调控,但仍保留其催化活性。对突变亚基的生化分析表明,它与调节亚基的亲和力降低了100倍。突变催化亚基对三磷酸腺苷和肽共底物的米氏常数增加了约三倍,其催化速率基本不变。突变基因的核苷酸序列包含一个单核苷酸变化,导致第241位氨基酸由苏氨酸替换为丙氨酸。该残基在其他丝氨酸-苏氨酸蛋白激酶中保守。这些结果表明,该苏氨酸是催化亚基和调节亚基之间的重要接触位点,但在底物识别中只是次要接触位点。