Modzelewska Katarzyna, Elgort Marc G, Huang Jingyu, Jongeward Gregg, Lauritzen Amara, Yoon Charles H, Sternberg Paul W, Moghal Nadeem
Department of Oncological Sciences, Huntsman Cancer Institute, University of Utah, 2000 Circle of Hope, Room 3242, Salt Lake City, UT 84112-5550, USA.
Mol Cell Biol. 2007 May;27(10):3695-707. doi: 10.1128/MCB.01630-06. Epub 2007 Mar 5.
Proper regulation of receptor tyrosine kinase (RTK)-Ras-mitogen-activated protein kinase (MAPK) signaling pathways is critical for normal development and the prevention of cancer. SOS is a dual-function guanine nucleotide exchange factor (GEF) that catalyzes exchange on Ras and Rac. Although the physiologic role of SOS and its CDC25 domain in RTK-mediated Ras activation is well established, the in vivo function of its Dbl Rac GEF domain is less clear. We have identified a novel gain-of-function missense mutation in the Dbl domain of Caenorhabditis elegans SOS-1 that promotes epidermal growth factor receptor (EGFR) signaling in vivo. Our data indicate that a major developmental function of the Dbl domain is to inhibit EGF-dependent MAPK activation. The amount of inhibition conferred by the Dbl domain is equal to that of established trans-acting inhibitors of the EGFR pathway, including c-Cbl and RasGAP, and more than that of MAPK phosphatase. In conjunction with molecular modeling, our data suggest that the C. elegans mutation, as well as an equivalent mutation in human SOS1, activates the MAPK pathway by disrupting an autoinhibitory function of the Dbl domain on Ras activation. Our work suggests that functionally similar point mutations in humans could directly contribute to disease.
受体酪氨酸激酶(RTK)-Ras-丝裂原活化蛋白激酶(MAPK)信号通路的适当调节对于正常发育和癌症预防至关重要。SOS是一种双功能鸟嘌呤核苷酸交换因子(GEF),可催化Ras和Rac上的交换。尽管SOS及其CDC25结构域在RTK介导的Ras激活中的生理作用已得到充分证实,但其Dbl Rac GEF结构域在体内的功能尚不清楚。我们在秀丽隐杆线虫SOS-1的Dbl结构域中鉴定出一种新的功能获得性错义突变,该突变在体内促进表皮生长因子受体(EGFR)信号传导。我们的数据表明,Dbl结构域的主要发育功能是抑制EGF依赖性MAPK激活。Dbl结构域赋予的抑制量与EGFR途径已确定的反式作用抑制剂(包括c-Cbl和RasGAP)的抑制量相等,且大于MAPK磷酸酶的抑制量。结合分子建模,我们的数据表明,秀丽隐杆线虫突变以及人类SOS1中的等效突变通过破坏Dbl结构域对Ras激活的自抑制功能来激活MAPK途径。我们的工作表明,人类中功能相似的点突变可能直接导致疾病。