Dehan Elinor, Bassermann Florian, Guardavaccaro Daniele, Vasiliver-Shamis Gaia, Cohen Michael, Lowes Kym N, Dustin Michael, Huang David C S, Taunton Jack, Pagano Michele
Department of Pathology, NYU Cancer Institute, Smilow Research Center, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA.
Mol Cell. 2009 Jan 16;33(1):109-16. doi: 10.1016/j.molcel.2008.12.020.
The BimEL tumor suppressor is a potent proapoptotic BH3-only protein. We found that, in response to survival signals, BimEL was rapidly phosphorylated on three serine residues in a conserved degron, facilitating binding and degradation via the F box protein betaTrCP. Phosphorylation of the BimEL degron was executed by Rsk1/2 and promoted by the Erk1/2-mediated phosphorylation of BimEL on Ser69. Compared to wild-type BimEL, a BimEL phosphorylation mutant unable to bind betaTrCP was stabilized and consequently potent at inducing apoptosis by the intrinsic mitochondrial pathway. Moreover, although non-small cell lung cancer (NSCLC) cells often become resistant to gefitinib (a clinically relevant tyrosine kinase inhibitor that induces apoptosis through BimEL), silencing of either betaTrCP or Rsk1/2 resulted in BimEL-mediated apoptosis of both gefitinib-sensitive and gefitinib-insensitive NSCLC cells. Our findings reveal that betaTrCP promotes cell survival in cooperation with the ERK-RSK pathway by targeting BimEL for degradation.
BimEL肿瘤抑制因子是一种强效的仅含BH3结构域的促凋亡蛋白。我们发现,在生存信号的作用下,BimEL保守降解结构域中的三个丝氨酸残基会迅速发生磷酸化,从而促进其与F盒蛋白βTrCP的结合及降解。BimEL降解结构域的磷酸化由Rsk1/2执行,并由Erk1/2介导的BimEL第69位丝氨酸的磷酸化所促进。与野生型BimEL相比,一种无法结合βTrCP的BimEL磷酸化突变体得以稳定,因此通过内在线粒体途径诱导凋亡的能力很强。此外,尽管非小细胞肺癌(NSCLC)细胞通常会对吉非替尼(一种临床上相关的酪氨酸激酶抑制剂,通过BimEL诱导凋亡)产生耐药性,但沉默βTrCP或Rsk1/2会导致吉非替尼敏感和吉非替尼不敏感的NSCLC细胞均发生BimEL介导的凋亡。我们的研究结果表明,βTrCP通过靶向BimEL进行降解,与ERK-RSK途径协同促进细胞存活。