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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation Panagis Filippakopoulos,1,8Michael Kofler,2,8Oliver Hantschel,3,8Gerald D. Gish,2,8Florian Grebien,3Eidarus Salah,1 Philipp Neudecker,4Lewis E. Kay,4Benjamin E. Turk,5Giulio Superti-Furga,3,*Tony Pawson,2,6,*and Stefan Knapp1,7,* 1Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, UK 2Samuel Lunenfeld Research Institute, Mount Sinai Hospital, 600 University Avenue, Toronto, Ontario M5G 1X5, Canada 3Center for Molecular Medicine of the Austrian Academy of Sciences, Lazarettgasse 19, 1090 Vienna, Austria 4Department of Biochemistry, University of Toronto, Toronto, Ontario M5S 1A8, Canada 5Yale University School of Medicine, Department of Pharmacology, New Haven, CT 06520, USA 6Department of Molecular Genetics, University of Toronto, Toronto, Ontario M5S 1A8, Canada 7Department of Clinical Pharmacology, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, UK 8These authors contributed equally to this work *Correspondence: pawson@mshri.on.ca (T.P.), stefan.knapp@sgc.ox.ac.uk (S.K.), gsuperti@cemm.oeaw.ac.at (G.S.-F.) DOI 10.1016/j.cell.2008.07.047 SUMMARY The SH2 domain of cytoplasmic tyrosine kinases can enhance catalytic activity and substrate recognition, but the molecular mechanisms by which this is achieved are poorly understood. We have solved the structure of the prototypic SH2-kinase unit of the human Fes tyrosine kinase, which appears spe- cialized for positive signaling. In its active conforma- tion, the SH2 domain tightly interacts with the kinase N-terminal lobe and positions the kinase aC helix in an active configuration through essential packing and electrostatic interactions. This interaction is sta- bilized by ligand binding to the SH2 domain. Our data indicate that Fes kinase activation is closely coupled to substrate recognition through cooperative SH2- kinase-substrate interactions. Similarly, we find that the SH2 domain of the active Abl kinase stimulates catalytic activity and substrate phosphorylation through a distinct SH2-kinase interface. Thus, the SH2 and catalytic domains of active Fes and Abl pro-oncogenic kinases form integrated structures essential for effective tyrosine kinase signaling. INTRODUCTION Protein domains are modules that can be joined in new combina- tions during evolution to create novel cellular functions. Once covalently tethered, such domains can acquire specific intramo- lecular interactions that yield selective allosteric regulation ( Kur- iyan and Eisenberg, 2007 ). These processes have been at work in the evolution of multidomain cytoplasmic tyrosine kinases. Most of these enzymes have a core unit comprised of a protein kinase domain and an adjacent Src homology 2 (SH2) domain(Figure S1 available online), an ancient combination that likely emerged at the dawn of phosphotyrosine (pTyr) signaling in organisms such as Dictyostelium discoideum (Eichinger et al., 2005 ). A likely role of this ancestral fusion of SH2 and kinase do- mains was to enhance the phosphorylation of specific substrates (Moniakis et al., 2001 ). In metazoans, the SH2-kinase core is typ- ically flanked by additional regulatory domains, such as SH3. In addition to their positive role in kinase activity and substrate recognition, the interaction domains of tyrosine kinases such as Src, Abl, and ZAP-70 have also acquired an ability to sup- press catalytic activity through intramolecular interactions. The structural basis for these autoinhibitory effects has been ana- lyzed in detail ( Deindl et al., 2007; Nagar et al., 2003; Sicheri et al., 1997; Xu et al., 1997 ). However, we lack a corresponding understanding of the mechanisms by which the SH2 domain synergizes with the tyrosine kinase domain in the active state. The Fps/Fes cytoplasmic tyrosine kinase was identified as a transforming protein encoded by avian ( Fps) and mammalian (Fes) retroviral oncogenes, in which retroviral Gag sequences are fused to the N termini of cell-derived Fps/Fes products ( Grof- fen et al., 1983; Lee et al., 1980; Shibuya et al., 1980 ). We previ- ously used insertion mutagenesis to identify domains required for Fps catalytic and biological activities in the context of the P130gag-fpsviral (v /C0) oncoprotein of Fujinami avian sarcoma virus ( Sadowski et al., 1986; Stone et al., 1984 ). This approach revealed three regions that are important for v-Fps transforming activity: the C-terminal tyrosine kinase domain, an adjacent se- quence designated as the SH2 domain that modifies kinase ac- tivity and substrate recognition, and an N-terminal domain (Nfps) involved in membrane localization ( Brooks-Wilson et al., 1989 ), now annotated as a member of the extended FCH or F-BAR domain family ( Itoh and De Camilli, 2006 ). Fps/Fes proteins do not possess an SH3 domain and, consequently, are not autoinhibited through intramolecular interactions in the fashion of Src and Abl tyrosine kinases (Greer, 2002 ). In contrast, they may be regulated by reversible Cell 134, 793–803, September 5, 2008 ª2008 Elsevier Inc. 793Open access under CC BY license.
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kinase sh2 domain fes tyrosine domains substrate abl recognition university fps toronto kinases catalytic activity active interactions oxford structural activation
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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
1
membrane association and oligomerization mediated by the F-BAR domain and by recruitment to specific subcellular sites by the SH2 domain ( Brooks-Wilson et al., 1989; Naba et al., 2008; Read et al., 1997; Tsujita et al., 2006 ). The N-terminal Gag sequences of v-Fps/Fes oncoproteins result in more stable membrane localization and, consequently, in constitutive auto- phosphorylation ( Foster et al., 1985; Greer et al., 1994 ). For both v-Fps ( Weinmaster et al., 1984 ) and Fes ( Hjermstad et al., 1993 ), autophosphorylation in the kinase domain stimulates catalytic activity. Dipeptide insertions in the N-terminal region of the v-Fps SH2 domain cause a severe loss of both kinase and transforming functions ( DeClue et al., 1987; Sadowski et al., 1986 ). Taken with the observation that the SH2 and kinase domains forma 45 kDa protease-resistant fragment ( Koch et al., 1989; Wein- master and Pawson, 1982 ), such data have suggested that the v-Fps SH2 domain undergoes an intramolecular interactionwith the kinase domain that stimulates catalytic activity. TheSH2 domains of v-Fps and human Fes also aid in substrate rec- ognition ( DeClue et al., 1987; Jucker et al., 1997; Koch et al., 1989 ), potentially by binding pTyr sites on primed targets. Fps/ Fes proteins, therefore, provide a model to study the cooperative effects of interaction and catalytic domains in promoting the kinase active state. Mammals have two proteins with an F-BAR-SH2-kinase do- main architecture, Fes and Fer. These have a range of functions, including regulation of adherens junction stability, actin dynam-ics, vesicular trafficking, and receptor internalization, mediated by phosphorylation of substrates such as cortactin, Pecam-1, andb-catenin ( Greer, 2002; Sangrar et al., 2007; Udell et al., 2006 ). In vivo, murine Fes and Fer regulate hemostasis and in- nate immunity ( Greer, 2002; Parsons and Greer, 2006; Parsons et al., 2007 ). Here, we identify the molecular mechanisms by which the human Fes SH2 and kinase domains interact with one another and with substrate to promote the active state. We show that the linked SH2 and catalytic domains of the active Abl tyrosinekinase, like Fes, act as a unit in which the SH2 domain stimulates the adjacent kinase domain. These results show how tyrosine kinase activity can be coupled to substrate recognition andidentify a common strategy by which the SH2 domains ofdistinct cytoplasmic tyrosine kinases promote substrate phosphorylation. RESULTS Determination of the Fes SH2-Kinase Structure We investigated the structure of a polypeptide from human Fes comprising a linker region N terminal to the SH2 domain, theSH2 domain, and the C-terminal kinase domain ( Figure 1 A). We obtained high yields for a single Fes construct (containing residues I448 to the C terminus) in E. coli coexpressed with the YopH tyrosine phosphatase ( Seeliger et al., 2005 ). To explore the mechanisms of kinase regulation and substrate recognition, we solved structures of the unphosphorylated Fes SH2-kinase unit both in the presence and absence of a kinase consensussubstrate peptide. In addition, we analyzed Fes SH2-kinase that had been autophosphorylated on the kinase activation seg-ment (Y713) in complex with a substrate peptide. The three structures were determined in complex with the ATP mimetic kinase inhibitor staurosporine and were refined to low R factors and acceptable geometry ( Table S1 ). The binding mode of staur- osporine to the ATP pocket is similar to structures reported pre- viously ( Bertrand et al., 2003 ); in addition, two molecules of staurosporine were identified in crystal contacts in Fes-substratecomplexes. The initial structure of unphosphorylated Fes SH2-kinase revealed an active conformation, which was stabilized by two sulphate ions that mimic binding of a pTyr ligand to the SH2 domain, as well as activation segment phosphorylation.This structure was well ordered, showing productive interactions between the SH2 and kinase domains, and we were able to trace the entire chain; we refer to this structure as ‘‘active.’’ In contrast,the other two structures have no ligand bound to the SH2 domain and show disordered loop regions in the SH2 domain and in the upper kinase lobe, indicative of an inactive conformation.Composite analysis of all three structures indicates multiplemechanisms for ordering of the activation segment. Structural Overview of an Active Fes Conformation An overview of unphosphorylated Fes SH2-kinase in its catalyt- ically active conformation is shown in Figure 1 B. In this active configuration, the SH2 domain is stabilized by a sulphate ion,which mimics the phosphate of a pTyr ligand by coordinating a conserved SH2 domain arginine (R483), as well as R467 and S485 (see Figure 5 A). In addition, a sulphate ion is coordinated by Y713 and R706 in the activation segment, thereby mimicking autophosphorylation (see Figure 3 B). The SH2 and kinase do- mains form a stable unit linked by the N-terminal region of theSH2 domain and polar interactions between the SH2 domain he- lixaA and the catalytically important helix aC (Figures 1C,2D, and S2). In Fes/Fer family members, the linker region between the SH2 and kinase domains is about 8 residues shorter whencompared to other cytoplasmic tyrosine kinases, constraining the packing of the SH2 domain. The N terminus of the SH2 do- main ( 462HGAI) intercalates between the central SH2 bsheet and the loop region between strands b4 and b5 in the kinase domain ( Figures 2 D and S3). This tight packing does not leave room for bulky side chains, and the central glycine residue ispresent in all Fes family members, suggesting that this domain packing is conserved. The second major interaction site is formed by a network of acidic residues located in the SH2 helix aA (E469, E472) and R609 in aC of the kinase. This arrangement suggests that the in- teraction between the SH2 and kinase domains positions andstabilizes aC in an active conformation, as indicated by the salt bridge formed between the active site lysine (K590) and the con- served aC glutamate (E607), as well as by low B values in loop regions linking this helix ( Figure 2 D). The structure, therefore, shows the SH2 domain forming an extensive interface with the N lobe of the kinase domain that promotes the organization of a functional kinase active site. A Tight SH2-Kinase Interaction Is Required for Fes ActivityTo pursue the relevance of the observed interdomain inter- actions, we studied the effects of mutating residues in the 794 Cell 134, 793–803, September 5, 2008 ª2008 Elsevier Inc.
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sh2 kinase domain fes active domains substrate fps structure activation terminal region figure structures conformation phosphorylation greer catalytic two tyrosine
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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
2
SH2-kinase interface on human Fes activity. To this end, we monitored Fes autophosphorylation and transphosphorylation activity in transfected cells, using cortactin (residues 382–550)fused to GST as an exogenous substrate ( Figures 2 A and 2B). In an effort to perturb the close interaction between the SH2 and kinase domains, we mutated the conserved glycineresidue (G463) located in the tightly packed interface betweenthe SH2 N terminus and the kinase b4/b5 loop to valine (mutant G/V). Introducing this bulky side chain would be expected to sterically hinder alignment of the SH2 and kinase domains,resulting in an altered domain packing. Wild-type (WT) and G/V mutant full-length human Fes, each with an N-terminal Flag epitope, were expressed in HEK293T cells together withGST-cortactin. The WT protein was active as measured by autophosphorylation and tyrosine phosphorylation of cotrans- fected cortactin, whereas the G/V Fes mutant was completelyinactive ( Figures 2 A and 2B). To extend this approach, we mutated residues involved in the salt bridge network, which appear to position and stabilize the kinase N-terminal lobe helix aC. In particular, we mutated E469 and E472 in the SH2 domain aA helix to lysine either individually or together (mutant EE/KK). The Fes E469K mutant exhibited reduced tyrosine kinase activity, whereas the E472Kmutant was not significantly impaired (data not shown). Consis- tent with this finding, the side chain of E472 was not visible in the electron density and was assumed to be unstructured.However, mutation of both E469 and E472 to lysine strongly re- duced Fes kinase activity, suggesting that both side chains contribute synergistically to this electrostatic interaction ( Fig- ures 2 A and 2B). This is consistent with the observation that the SH2-kinase domain interface shows a charge complemen- tarity such that the surface of the SH2 domain interacting with the kinase is mainly negatively charged, whereas the corre- Figure 1. Structural Overview of Human Fes (A) Domain architecture. The locations of the F-BAR, SH2, and kinase domains are indicated.The F-BAR domain contains the FCH and coiled-coil (CC) sequences. The crystallized construct ishighlighted by arrows.(B) Ribbon diagram representing the overall struc-ture of the SH2-kinase domain unit. The main sec-ondary structure elements are labeled.(C) Surface representation of active Fes. The sur-face is colored by electrostatic potential between/C010 and +10 kcal/mol. sponding kinase domain surface is posi- tively charged ( Figure S2 ). To demon- strate that these mutations did notdisturb the structural integrity of Fes, we sought to rescue the inactive double mutant EE/KK by inverting the polarityof the interface by simultaneously mutat- ing R609 in the aC helix to glutamate. In- deed, the triple mutant (mutant EER/KKE) regained kinase activity to a level approaching wild-type ( Figures 2 A and 2B), providing direct evidence that the electrostatic interactions at the SH2-kinase interface are functionally important. In support of the notion that the G/V and EE/KK mutations have a selective effect on the SH2-kinase interface, they did not alter the affinity of the isolated FesSH2 domain for a pTyr-containing peptide from ezrin (VpYEPVSY). The SH2-kinase polypeptide had a similar affinity for the ezrin phosphopeptide as did the isolated SH2 domain(Figure S4 ). We introduced the same mutations into a Myc-tagged P130 gag-fpsoncoprotein and found that a G823V substitution, analogous to the G/V mutation in Fes, completely inhibited kinase activity ( Figure S5 ). Of interest, the inactivating RX15m v-Fps insertion that was isolated in the earlier muta-genesis screen changes the tyrosine located 2 residues Nterminal to G823 to SRD and, therefore, likely inhibits kinase activity by destabilizing the packing between the N terminus of the SH2 domain and the b4/b5 loop of the kinase domain (Figures 2 C and S5). Single or double mutations of E829 and E832 to lysine or alanine showed similar, albeit less pro- nounced, effects as the corresponding substitutions in Fes(at E469 and E472), and the activity of an EE/KK mutant was restored by further substitution of E for R969 (EER/ KKE), equivalent to R609 in the Fes kinase aC helix (data not shown). Supporting the importance of this interface inv-Fps, the AX9m mutation in v-Fps inserts a LE dipeptide between E832 and L833 in the SH2 aA helix, which likely dis- turbs the electrostatic interface between the SH2 domain andkinase aC helix. Thus, the RX15m and AX9m v-Fps insertion mutations that originally identified the SH2 sequence as a functional module map to the two primary elements thatinteract with the kinase domain. Therefore, the SH2-kinase interface revealed by structural analysis of human Fes is also critical for the transforming activity of the v-Fps oncoprotein. Cell 134, 793–803, September 5, 2008 ª2008 Elsevier Inc. 795
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kinase sh2 fes domain interface activity mutant helix mutations fps structural domains human figures e472 electrostatic figure cortactin residues mutated
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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
3
In summary, the residues at the SH2-kinase domain interface stabilize an active conformation of the Fes kinase domain, inpart by positioning and stabilizing helix aC to form the active site. Substrate Binding and an Antiparallel bSheet Stabilize the Fes Activation Segment To better understand Fes regulation, we also solved structures ofunphosphorylated Fes in the absence of phosphomimetic salt ions and Fes in which the regulatory activation segment residue (Y713) had been autophosphorylated in vitro ( Table S1 ). In both cases, a substrate peptide (IYESL) was cocrystallized. As ex- pected, in phosphorylated Fes, the phosphorylated Y713 formed a network of salt bridges and hydrogen bonds of the sort typi-cally observed in activation segments of activated kinases(Figure 3 A). This links the conserved catalytic loop arginine (R682) with the activation segment and additionally stabilizes the active conformation through hydrogen bonds to R706 andS716. These polar interactions are mimicked by the sulphate ion present in active Fes ( Figure 3 B). Interestingly, the activation segment of unphosphorylated Fes crystallized in the absence ofsulphate ions assumed a similar conformation, stabilized by hy- drogen bonds to the Y713 hydroxyl group, suggesting that theFes activation segment is quite stable in the absence of tyrosine phosphorylation. Two structural features contribute to this stability. First, the ac- tivation loop forms a short antiparallel bsheet with the loop re- gion linking the helices aEF with aF in the kinase C lobe. Interest- ingly, this bsheet is present in most active (phosphorylated) tyrosine kinases in addition to the constitutively active Ser/Thr kinase MPSK1 ( Eswaran et al., 2008 ) and in all Fes structures presented here ( Figure S6 ). Second, binding of the substrate peptide also induces a bsheet secondary structure between the substrate peptide and a strand in the activation segment(bI), with typical main chain hydrogen bond interactions. The activation segment in active Fes showed significantly higher temperature factors than in either of the Fes-substrate com-plexes, indicating the stabilizing effect of substrate binding(Figure 3 C). A similar antiparallel sheet interaction is also present in insulin receptor-substrate complexes, suggesting that stabili- zation of the activation segment by substrate binding is a morewidespread mechanism of tyrosine kinase activation ( Figure S6 ). Fes is only distantly related to tyrosine kinases of known sub- strate specificity. We used a degenerate peptide library anda peptide array comprising all single substitutions of a known substrate peptide (EAEIYEAIE) to determine the peptide Figure 2. Activation of Fes Kinase Activity by SH2 Domain Interactions (A) The effect of mutations in the SH2 domain on Fes kinase activity: HEK293T cells were cotrans-fected with Flag-tagged Fes and GST-cortactin.Cell lysates were immunoprecipitated with anti-Flag and blotted with anti-pTyr to reveal auto-phosphorylated (p) Flag-Fes (top panel) or withanti-Flag (lower panel) as a control. WT indicateswild-type Fes, and mutants are described in thetext.(B) GST-cortactin was affinity purified from cellscoexpressing WT or mutant Fes proteins and blot-ted either with anti-pTyr antibodies to measureFes-induced phosphorylation (p) (top panel) orwith anti-GST (bottom panel). (C) Comparison of the N-terminal SH2 domain se- quence of Fps/Fes orthologs. Insertions originallyused to identify the SH2 domain in v-Fps are indi-cated (RX15m and AX9m) ( Sadowski et al., 1986; Stone et al., 1984 ). Conserved residues are high- lighted in red and similar residues in yellow.(D) Details of the Fes SH2-kinase interface. Resi-dues important for the SH2 domain-kinase inter-action are conserved in Fps/Fes family membersbut not in other tyrosine kinases. Residues mu-tated in this study are indicated by a green aster-isk. Interactions of interface residues and theinvolved secondary structure elements are shownin the structure of active Fes. The alignment ofhuman sequences is colored as in (C). 796 Cell 134, 793–803, September 5, 2008 ª2008 Elsevier Inc.
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fes activation kinase substrate sh2 active segment domain peptide figure residues tyrosine binding bsheet phosphorylated kinases interactions flag anti panel
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Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
4
sequence preferentially recognized by the Fes active site (Figure S7 ). The two screens revealed that Fes prefers substrates with bulky aliphatic residues at the position N terminal to the sub- strate tyrosine (position /C01), an acidic or phosphorylated residue at position +1, and hydrophobic residues at position +3. Thestructure of Fes in complex with its consensus peptide IYESL supports the peptide library results ( Figures 4 andS7). Selectivity for hydrophobic interactions in substrate positions /C01 and +3 can be explained by binding of the corresponding substrate res- idues isoleucine and leucine to hydrophobic pockets on the Fes kinase, and selectivity for acidic residues in position +1 is due toformation of a hydrogen bond with N766 located in helix aG. The determined substrate specificity corresponds well to known exogenous Fes-substrate sites ( Greer, 2002 ). Fes Is Stabilized by Ligand Binding to Its SH2 DomainIn the latter two structures, crystallized in the absence of phos-phomimetic salt ions, there was no ligand bound to the SH2 do- main. A striking feature of both structures was the large degree of disorder in SH2 domain loop regions as well as in the loop con-necting the sheet b3 with aC. In addition, helix aC showed very high temperature factors, indicating a high degree of mobility of this regulatory element (Figures 3C and 5B). In contrast, the sulphate ion occupying the pTyr-binding site of the SH2 domain in the active Fes structure formed a network of salt bridges Figure 3. Conformation of the Fes Activa- tion Segment (A) Superimposition of the activation segment in active Fes (gray) and the phosphorylatedFes-substrate complex. Hydrophilic interactionsformed by the phosphate moiety and the substratetyrosine are indicated by yellow dots. The antipar-allelbsheet formed at the tip of the activation seg- ment is labeled as b-A-loop, and the substrate peptide is shown as a red ribbon. The inducedbsheet present in the substrate complex ( bI) is also shown.(B) Interactions of the activation segment Y713 inunphosphorylated (left), active (ligating a sulphateion; middle), and phosphorylated (right) Fes.A2 F o–Fcelectron density map around the inter- acting residues is also shown contoured at 2 s. (C) Schematic drawing of the Fes main chain. Re-gions with high temperature factors are shown byan increasing radius of the backbone. The activa-tion segment is highlighted in purple; aC, in pink; the SH2 domain, in green; and the substrate pep-tide (in the phosphorylated Fes structure), inorange. Note the absence of ordered loop regionsin the SH2 domain and kinase N lobe of phosphor-ylated Fes. typically observed in SH2 domain phos- phopeptide complexes, correlating withstabilization and ordering of the SH2 do-main and aC(Figures 5 A and 5B). The high flexibility of residues in the SH2-ki- nase domain interface in the absence of an SH2 ligand suggested that Fes activity and SH2 domain li- gand binding are coupled. To pursue this model, we substituted R483 in the SH2 pTyr-binding pocket with methionine (mutant R/M), which abolishes pTyr recognition ( Figure S4 A). The R/M mutant failed to autophosphorylate in transfected cells and had a significantly reduced ability to transphosphorylate cortac- tin (Figures 2 A and 2B). We used NMR spectroscopy to assess whether this substitution might affect SH2 residues at the inter- face with the kinase domain. An HSQC NMR spectrum of an 15N-labeled sample of the isolated R/M mutant Fes SH2 domain revealed chemical shift changes of amide resonances of the critical interface residues G463 and E469 and nearby residues, as compared with the wild-type SH2 domain ( Figure 5 C). While these changes are ligand independent, the low activity of theR/M mutation, together with the structural data, suggests a cou- pling between SH2 domain pTyr binding and the catalytically active Fes conformation. In the active Fes structure, the pTyr-binding site of the Fes SH2 domain is only about 30 A ˚distant from the active site of the ki- nase domain. Since peptides bound to the activation segmentand the SH2 domain should be in the same N- to C-terminal ori- entation, the Fes phosphorylation site and the pTyr that recog- nize the Fes SH2 domain could, in principle, be connected withinthe same polypeptide chain by a short intervening sequence (seeFigure 7 ). To test this model, we synthesized primed substrate peptides, each containing a C-terminal phosphorylated SH2 Cell 134, 793–803, September 5, 2008 ª2008 Elsevier Inc. 797
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sh2 fes domain substrate residues active binding ptyr kinase activation site position figure phosphorylated figures ligand loop high segment shown
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"Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activa(...TRUNCATED)
5
"domain-binding site, linked by a polyglycine spacer of variable\nlength to an unphosphorylated tyro(...TRUNCATED)
pdf_pagechunk
[-0.06775268912315369,-0.44722098112106323,-0.09322696924209595,-0.19570235908031464,0.1372824609279(...TRUNCATED)
"kinase sh2 abl domain activity substrate lobe fes figure nagar tyrosine phosphorylation peptide res(...TRUNCATED)
[0.11022280156612396,-0.5681320428848267,-0.19959218800067902,-0.04248280078172684,0.143803149461746(...TRUNCATED)
"Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activa(...TRUNCATED)
6
"S9D and S9E). HA-tagged Abl proteins were precipitated from\nHEK293 cells and assayed for phosphory(...TRUNCATED)
pdf_pagechunk
[-0.06674288958311081,-0.443125456571579,-0.09188003838062286,-0.18679212033748627,0.139508008956909(...TRUNCATED)
"sh2 domain kinase fes active activation helix substrate abl interactions binding effect figure acti(...TRUNCATED)
[0.028668534010648727,-0.7448766231536865,-0.1550757735967636,-0.23680339753627777,0.101315610110759(...TRUNCATED)
"Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activa(...TRUNCATED)
7
"through a series of linked devices. For one, clustering induces\nintermolecular autophosphorylation(...TRUNCATED)
pdf_pagechunk
[-0.06940232217311859,-0.4536266326904297,-0.09464538097381592,-0.19815759360790253,0.11981225013732(...TRUNCATED)
"kinase abl domain sh2 fes activation substrate activity active domains stabilizes state membrane pt(...TRUNCATED)
[0.1557217836380005,-0.842115581035614,-0.14626534283161163,-0.010230571031570435,0.2113016843795776(...TRUNCATED)
"Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activa(...TRUNCATED)
8
"SH2 domain can direct subcellular localization and substrate re-\ncruitment and promote an active c(...TRUNCATED)
pdf_pagechunk
[-0.08142413944005966,-0.4328019917011261,-0.09554870426654816,-0.183843195438385,0.1405455172061920(...TRUNCATED)
"sh2 kinase domain fes active abl using domains data anti catalytic protein substrate conformation s(...TRUNCATED)
[0.16253094375133514,-0.8001930713653564,-0.19065743684768677,0.050327323377132416,0.216953471302986(...TRUNCATED)
"Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activa(...TRUNCATED)
9
"Data Processing, Molecular Replacement, and Refinement\nData were indexed and integrated using MOS(...TRUNCATED)
pdf_pagechunk
[-0.07736387848854065,-0.4417183995246887,-0.09811335802078247,-0.1873847097158432,0.133638203144073(...TRUNCATED)
"fes cell kinase protein using structure domain 2008 fps 2007 biol tyrosine structural mol src data (...TRUNCATED)
[0.10716253519058228,-0.3093935549259186,-0.20897433161735535,0.03832915797829628,0.1606442034244537(...TRUNCATED)
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