Published in J Am Chem Soc on December 24, 2008
Sensitive multiplexed analysis of kinase activities and activity-based kinase identification. Nat Biotechnol (2009) 1.21
Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitors. Cell Rep (2014) 1.01
The genesis of tyrosine phosphorylation. Cold Spring Harb Perspect Biol (2014) 0.97
Phosphorylation-dependent kinase-substrate cross-linking. Angew Chem Int Ed Engl (2010) 0.95
Irreversible inhibitors of c-Src kinase that target a nonconserved cysteine. ACS Chem Biol (2012) 0.90
Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic. Elife (2015) 0.82
The application of modular protein domains in proteomics. FEBS Lett (2012) 0.82
Lignin-derived oak phenolics: a theoretical examination of additional potential health benefits of red wine. J Mol Model (2010) 0.76
Chemical Methods for Encoding and Decoding of Posttranslational Modifications. Cell Chem Biol (2016) 0.75
Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity. ACS Chem Biol (2015) 0.75
A crosslinker based on a tethered electrophile for mapping kinase-substrate networks. Chem Biol (2014) 0.75
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations. Sci Rep (2017) 0.75
The protein kinase complement of the human genome. Science (2002) 35.36
AKT/PKB signaling: navigating downstream. Cell (2007) 31.26
Inhibition of glycogen synthase kinase-3 by insulin mediated by protein kinase B. Nature (1996) 26.30
Scansite 2.0: Proteome-wide prediction of cell signaling interactions using short sequence motifs. Nucleic Acids Res (2003) 15.74
A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74
A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol (2005) 12.22
Large-scale characterization of HeLa cell nuclear phosphoproteins. Proc Natl Acad Sci U S A (2004) 10.78
Assembly of cell regulatory systems through protein interaction domains. Science (2003) 10.59
Global analysis of protein phosphorylation in yeast. Nature (2005) 7.46
Molecular basis for the substrate specificity of protein kinase B; comparison with MAPKAP kinase-1 and p70 S6 kinase. FEBS Lett (1996) 6.16
Large-scale phosphorylation analysis of mouse liver. Proc Natl Acad Sci U S A (2007) 6.08
Use of an oriented peptide library to determine the optimal substrates of protein kinases. Curr Biol (1994) 6.04
Activation of AKT kinases in cancer: implications for therapeutic targeting. Adv Cancer Res (2005) 4.74
A direct linkage between the phosphoinositide 3-kinase-AKT signaling pathway and the mammalian target of rapamycin in mitogen-stimulated and transformed cells. Cancer Res (2000) 4.62
Evidence of insulin-stimulated phosphorylation and activation of the mammalian target of rapamycin mediated by a protein kinase B signaling pathway. Proc Natl Acad Sci U S A (1998) 3.66
Phosphorylation of mammalian target of rapamycin (mTOR) at Ser-2448 is mediated by p70S6 kinase. J Biol Chem (2005) 3.56
Structural basis for control by phosphorylation. Chem Rev (2001) 3.53
Identification of S6 kinase 1 as a novel mammalian target of rapamycin (mTOR)-phosphorylating kinase. J Biol Chem (2005) 2.84
Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates. Proc Natl Acad Sci U S A (2008) 2.53
A semisynthetic epitope for kinase substrates. Nat Methods (2007) 2.40
Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites. EMBO J (2008) 2.12
Suicide substrates, mechanism-based enzyme inactivators: recent developments. Annu Rev Biochem (1984) 1.94
Hitting the target: emerging technologies in the search for kinase substrates. Sci STKE (2002) 1.91
c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty. Structure (2007) 1.87
Identification and characterization of four novel phosphorylation sites (Ser31, Ser325, Thr336 and Thr366) on LKB1/STK11, the protein kinase mutated in Peutz-Jeghers cancer syndrome. Biochem J (2002) 1.80
Reactions of orthophthalaldehyde with nucleophiles. Chem Rev (2004) 1.40
Charging it up: global analysis of protein phosphorylation. Trends Genet (2006) 1.29
Phosphorylation of the kinase homology domain is essential for activation of the A-type natriuretic peptide receptor. Mol Cell Biol (1998) 1.26
A mechanism-based cross-linker for the identification of kinase-substrate pairs. J Am Chem Soc (2004) 1.07
Identification of a novel phosphorylation site, Ser-170, as a regulator of bad pro-apoptotic activity. J Biol Chem (2001) 1.02
p38 map kinase substrate specificity differs greatly for protein and peptide substrates. Arch Biochem Biophys (2000) 0.97
Development of photo-crosslinking reagents for protein kinase-substrate interactions. FEBS Lett (2002) 0.97
Identifying protein kinase substrates: hunting for the organ-grinder's monkeys. Trends Biochem Sci (2004) 0.97
Dialogue between LKB1 and AMPK: a hot topic at the cellular pole. Sci STKE (2007) 0.92
SRC family kinases as potential therapeutic targets for malignancies and immunological disorders. Curr Med Chem (2008) 0.92
Toward a pharmacophore for kinase frequent hitters. J Med Chem (2004) 0.91
Conversion of a tyrosine kinase protein substrate to a high affinity ligand by ATP linkage. J Am Chem Soc (2003) 0.86
An improved mechanism-based cross-linker for multiplexed kinase detection and inhibition in a complex proteome. Chembiochem (2008) 0.84
Rational design and evaluation of improved o-phthalaldehyde-like fluorogenic reagents. Anal Biochem (1985) 0.83
Evidence for proximal cysteine and lysine residues present at the nucleotide domain of rabbit muscle creatine kinase. Biochim Biophys Acta (1993) 0.79
Inactivation of yeast hexokinase by o-phthalaldehyde: evidence for the presence of a cysteine and a lysine at or near the active site. Biochim Biophys Acta (1988) 0.78
RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature (2010) 17.31
A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74
Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell (2002) 13.03
A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol (2005) 12.22
The conformational plasticity of protein kinases. Cell (2002) 11.21
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell (2006) 10.28
A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell (2006) 10.06
Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol (2009) 9.63
IRE1 signaling affects cell fate during the unfolded protein response. Science (2007) 9.01
Targets of the cyclin-dependent kinase Cdk1. Nature (2003) 8.05
Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature (2007) 6.56
A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell (2006) 6.15
T cell receptor signaling controls Foxp3 expression via PI3K, Akt, and mTOR. Proc Natl Acad Sci U S A (2008) 5.97
Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol (2011) 5.65
The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature (2012) 5.61
The forkhead transcription factor Foxo1 regulates adipocyte differentiation. Dev Cell (2003) 5.59
Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science (2005) 5.53
Structural basis for the autoinhibition of c-Abl tyrosine kinase. Cell (2003) 5.44
Inhibitor hijacking of Akt activation. Nat Chem Biol (2009) 4.91
Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segment. Cell (2009) 4.78
Regulation of insulin action and pancreatic beta-cell function by mutated alleles of the gene encoding forkhead transcription factor Foxo1. Nat Genet (2002) 4.76
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A (2005) 4.70
Elevated gene expression levels distinguish human from non-human primate brains. Proc Natl Acad Sci U S A (2003) 4.69
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature (2013) 4.43
Structural analysis of a eukaryotic sliding DNA clamp-clamp loader complex. Nature (2004) 4.37
Disruption of forkhead transcription factor (FOXO) family members in mice reveals their functional diversification. Proc Natl Acad Sci U S A (2004) 4.25
The site-specific installation of methyl-lysine analogs into recombinant histones. Cell (2007) 4.22
Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res (2002) 4.19
Features of selective kinase inhibitors. Chem Biol (2005) 4.07
The forkhead transcription factor Foxo1 links insulin signaling to Pdx1 regulation of pancreatic beta cell growth. J Clin Invest (2002) 4.05
Rewiring of genetic networks in response to DNA damage. Science (2010) 4.03
Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia. Nature (2012) 4.01
The unfolded protein response signals through high-order assembly of Ire1. Nature (2008) 3.87
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol (2008) 3.84
Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E. Cancer Cell (2010) 3.79
Targeting the cancer kinome through polypharmacology. Nat Rev Cancer (2010) 3.74
Structural evidence for feedback activation by Ras.GTP of the Ras-specific nucleotide exchange factor SOS. Cell (2003) 3.66
The Ipl1-Aurora protein kinase activates the spindle checkpoint by creating unattached kinetochores. Nat Cell Biol (2005) 3.61
A myristoyl/phosphotyrosine switch regulates c-Abl. Cell (2003) 3.48
A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol (2006) 3.40
Akt and autophagy cooperate to promote survival of drug-resistant glioma. Sci Signal (2010) 3.35
A chemical-genetic strategy implicates myosin-1c in adaptation by hair cells. Cell (2002) 3.34
Chemical genetic analysis of the time course of signal transduction by JNK. Mol Cell (2006) 3.32
Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34. Science (2010) 3.20
Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol (2008) 3.18
Functional organization of the S. cerevisiae phosphorylation network. Cell (2009) 3.15
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat Chem Biol (2010) 3.15
Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition. Cancer Res (2009) 3.14
Structure of the autoinhibited kinase domain of CaMKII and SAXS analysis of the holoenzyme. Cell (2005) 3.08
Chemical genetic screen for AMPKα2 substrates uncovers a network of proteins involved in mitosis. Mol Cell (2011) 2.99
A chemical-genetic approach to studying neurotrophin signaling. Neuron (2005) 2.93
Arterial-venous segregation by selective cell sprouting: an alternative mode of blood vessel formation. Science (2009) 2.82
Membrane-dependent signal integration by the Ras activator Son of sevenless. Nat Struct Mol Biol (2008) 2.82
Control of landmark events in meiosis by the CDK Cdc28 and the meiosis-specific kinase Ime2. Genes Dev (2003) 2.79
Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface. Nature (2007) 2.78
Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proc Natl Acad Sci U S A (2009) 2.77
The F box protein Dsg1/Mdm30 is a transcriptional coactivator that stimulates Gal4 turnover and cotranscriptional mRNA processing. Cell (2005) 2.75
Chemical genetic analysis of Apg1 reveals a non-kinase role in the induction of autophagy. Mol Biol Cell (2003) 2.72
Structural basis for the inhibition of tyrosine kinase activity of ZAP-70. Cell (2007) 2.68
Evolution of phosphoregulation: comparison of phosphorylation patterns across yeast species. PLoS Biol (2009) 2.67
Oncogenic mutations counteract intrinsic disorder in the EGFR kinase and promote receptor dimerization. Cell (2012) 2.67
A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma. Cancer Res (2007) 2.62
The mechanism of linkage-specific ubiquitin chain elongation by a single-subunit E2. Cell (2011) 2.58
Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3. Proc Natl Acad Sci U S A (2009) 2.55
Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates. Proc Natl Acad Sci U S A (2008) 2.53
Conformational coupling across the plasma membrane in activation of the EGF receptor. Cell (2013) 2.49
A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases. Nat Methods (2005) 2.47
Adult mouse brain gene expression patterns bear an embryologic imprint. Proc Natl Acad Sci U S A (2005) 2.46
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol (2007) 2.43
Structure of a sliding clamp on DNA. Cell (2008) 2.42
Resiliency and vulnerability in the HER2-HER3 tumorigenic driver. Sci Transl Med (2010) 2.42
Crystal structure of an oxygen-binding heme domain related to soluble guanylate cyclases. Proc Natl Acad Sci U S A (2004) 2.41
A semisynthetic epitope for kinase substrates. Nat Methods (2007) 2.40
Structural analysis of autoinhibition in the Ras activator Son of sevenless. Cell (2004) 2.38
Chemical genetics reveals the requirement for Polo-like kinase 1 activity in positioning RhoA and triggering cytokinesis in human cells. Proc Natl Acad Sci U S A (2007) 2.37
Phosphoproteomic analysis reveals interconnected system-wide responses to perturbations of kinases and phosphatases in yeast. Sci Signal (2010) 2.36
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms. Mol Cell (2011) 2.35
Toxoplasma gondii calcium-dependent protein kinase 1 is a target for selective kinase inhibitors. Nat Struct Mol Biol (2010) 2.34
Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature (2012) 2.33
Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha. Cancer Cell (2008) 2.32
JNK2 is a positive regulator of the cJun transcription factor. Mol Cell (2006) 2.32
High yield bacterial expression of active c-Abl and c-Src tyrosine kinases. Protein Sci (2005) 2.32
Recognizing and exploiting differences between RNAi and small-molecule inhibitors. Nat Chem Biol (2007) 2.31
Architecture and membrane interactions of the EGF receptor. Cell (2013) 2.29
Glyoxalase 1 and glutathione reductase 1 regulate anxiety in mice. Nature (2005) 2.29
Organization of the SH3-SH2 unit in active and inactive forms of the c-Abl tyrosine kinase. Mol Cell (2006) 2.28
EGFR phosphorylates tumor-derived EGFRvIII driving STAT3/5 and progression in glioblastoma. Cancer Cell (2013) 2.28
Two cyclin-dependent kinases promote RNA polymerase II transcription and formation of the scaffold complex. Mol Cell Biol (2004) 2.26
Calcium-dependent protein kinase 1 is an essential regulator of exocytosis in Toxoplasma. Nature (2010) 2.25
Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell (2007) 2.22
An integrated platform of genomic assays reveals small-molecule bioactivities. Nat Chem Biol (2008) 2.21
PIK3CA cooperates with other phosphatidylinositol 3'-kinase pathway mutations to effect oncogenic transformation. Cancer Res (2008) 2.20