Despite extensive study of the EGF receptor (EGFR) signaling network, the immediate posttranslational changes that occur in response to growth factor stimulation remain poorly characterized; as a result, the biological mechanisms underlying signaling initiation remain obscured. To address this deficiency, we have used a mass spectrometry-based approach to measure system-wide phosphorylation changes throughout the network with 10-s resolution in the 80 s after stimulation in response to a range of eight growth factor concentrations. Significant changes were observed on proteins far downstream in the network as early as 10 s after stimulation, indicating a system capable of transmitting information quickly. Meanwhile, canonical members of the EGFR signaling network fall into clusters with distinct activation patterns. Src homology 2 domain containing transforming protein (Shc) and phosphoinositol 3-kinase (PI3K) phosphorylation levels increase rapidly, but equilibrate within 20 s, whereas proteins such as Grb2-associated binder-1 (Gab1) and SH2-containing tyrosine phosphatase (SHP2) show slower, sustained increases. Proximity ligation assays reveal that Shc and Gab1 phosphorylation patterns are representative of separate timescales for physical association with the receptor. Inhibition of phosphatases with vanadate reveals site-specific regulatory mechanisms and also uncovers primed activating components in the network, including Src family kinases, whose inhibition affects only a subset of proteins within the network. The results presented highlight the complexity of signaling initiation and provide a window into exploring mechanistic hypotheses about receptor tyrosine kinase (RTK) biology.signal transduction | tyrosine phosphorylation | epidermal growth factor receptor | mass spectrometry T he EGF receptor (EGFR) sits atop a complex signaling network that controls cell behavior in response to environmental cues. Cascades of posttranslational modifications initiated from EGFR, notably phosphorylation on tyrosine, serine, and threonine, influence protein-protein interactions and enzymatic activity to activate transcriptional programs that regulate proliferation, differentiation, and apoptosis (1). Mutation or overexpression of EGFR has been identified as an oncogenic driver for many tumor types, making it an attractive target for anticancer therapies (2).Building on decades of specific characterization using traditional biochemistry techniques, platforms such as protein microarrays and mass spectrometry have allowed systems biology to provide a comprehensive picture of intact and aberrant network behavior, which can be used to establish design criteria for therapeutic interventions (3). Manipulating components within the network experimentally and computationally has uncovered many features of the system that influence behaviors such as proliferation and survival (4-6). With many phenotypic responses occurring on the order of hours to days, most phosphorylation measurements have been on the timescale of minutes to...
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