Habelhah H, Shah K, Huang L, Burlingame A L, Shokat K M, Ronai Z
Ruttenberg Cancer Center, Mount Sinai School of Medicine, New York, New York 10029, USA.
J Biol Chem. 2001 May 25;276(21):18090-5. doi: 10.1074/jbc.M011396200. Epub 2001 Mar 19.
Modification of the ATP pocket on protein kinases allows selective use of an ATP analogue that exhibits high affinity for the altered kinases. Using this approach, we altered the ATP-binding site on JNK and identified N(6)-(2-phenythyl)-ATP, a modified form of ATP that exhibits high specificity and affinity for the modified, but not the wild type form, of JNK. Using modified JNK and its ATP analogue enables the detection of novel JNK substrates. Among substrates identified using this approach is heterogeneous nuclear ribonucleoprotein K, which is involved in transcription and post-transcriptional mRNA metabolism. The newly identified substrate can be phosphorylated by JNK on amino acids 216 and 353, which contribute to heterogeneous nuclear ribonucleoprotein K mediated transcriptional activities.
对蛋白激酶上的ATP口袋进行修饰,可以选择性地使用对改变后的激酶具有高亲和力的ATP类似物。采用这种方法,我们改变了JNK上的ATP结合位点,并鉴定出N(6)-(2-苯乙基)-ATP,这是一种ATP的修饰形式,对修饰后的JNK(而非野生型JNK)具有高特异性和亲和力。使用修饰后的JNK及其ATP类似物能够检测新的JNK底物。通过这种方法鉴定出的底物包括参与转录和转录后mRNA代谢的不均一核核糖核蛋白K。新鉴定出的底物可被JNK在氨基酸216和353处磷酸化,这有助于不均一核核糖核蛋白K介导的转录活性。