Published in Curr Opin Struct Biol on November 18, 2009
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The linker between SH2 and kinase domains positively regulates catalysis of the Tec family kinases. Biochemistry (2007) 1.18
Structural characterization of a novel Cbl phosphotyrosine recognition motif in the APS family of adapter proteins. J Biol Chem (2005) 1.14
Conformation of full-length Bruton tyrosine kinase (Btk) from synchrotron X-ray solution scattering. EMBO J (2003) 1.13
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The Jak1 SH2 domain does not fulfill a classical SH2 function in Jak/STAT signaling but plays a structural role for receptor interaction and up-regulation of receptor surface expression. J Biol Chem (2005) 1.10
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Genome wide analysis of pathogenic SH2 domain mutations. Proteins (2008) 1.05
Tyr130 phosphorylation triggers Syk release from antigen receptor by long-distance conformational uncoupling. Proc Natl Acad Sci U S A (2008) 1.04
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Stability and peptide binding specificity of Btk SH2 domain: molecular basis for X-linked agammaglobulinemia. Protein Sci (2000) 1.00
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Large-scale structural analysis of the classical human protein tyrosine phosphatome. Cell (2009) 3.51
Small-molecule inhibition of BRDT for male contraception. Cell (2012) 3.50
Crystal structure of the tetrameric Mad1-Mad2 core complex: implications of a 'safety belt' binding mechanism for the spindle checkpoint. EMBO J (2002) 3.42
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A (2007) 3.21
HMGB1 is an endogenous immune adjuvant released by necrotic cells. EMBO Rep (2004) 3.00
Critical residues for structure and catalysis in short-chain dehydrogenases/reductases. J Biol Chem (2002) 2.95
The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs. Proc Natl Acad Sci U S A (2006) 2.73
Bromodomains as therapeutic targets. Expert Rev Mol Med (2011) 2.52
Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation. Cell (2008) 2.46
The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation. EMBO J (2008) 2.36
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase. J Med Chem (2005) 2.34
Structure of the pseudokinase VRK3 reveals a degraded catalytic site, a highly conserved kinase fold, and a putative regulatory binding site. Structure (2009) 2.33
The (un)targeted cancer kinome. Nat Chem Biol (2010) 2.33
Exogenous high-mobility group box 1 protein induces myocardial regeneration after infarction via enhanced cardiac C-kit+ cell proliferation and differentiation. Circ Res (2005) 2.32
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol (2010) 2.26
Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation. PLoS Biol (2010) 2.22
Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites. EMBO J (2008) 2.12
Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol (2011) 2.06
Structure and substrate specificity of the Pim-1 kinase. J Biol Chem (2005) 1.96
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Specificity profiling of Pak kinases allows identification of novel phosphorylation sites. J Biol Chem (2007) 1.92
The bromodomain interaction module. FEBS Lett (2012) 1.92
The beta-lactam antibiotic, ceftriaxone, dramatically improves survival, increases glutamate uptake and induces neurotrophins in stroke. J Hypertens (2008) 1.91
Hsp70 chaperones as modulators of prion life cycle: novel effects of Ssa and Ssb on the Saccharomyces cerevisiae prion [PSI+]. Genetics (2004) 1.90
Structure and functional characterization of the atypical human kinase haspin. Proc Natl Acad Sci U S A (2009) 1.85
Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res (2013) 1.84
PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers. Haematologica (2010) 1.83
Candesartan but not ramipril pretreatment improves outcome after stroke and stimulates neurotrophin BNDF/TrkB system in rats. J Hypertens (2008) 1.81
Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem (2012) 1.76
Treatment with HMGB1 inhibitors diminishes CTL-induced liver disease in HBV transgenic mice. J Leukoc Biol (2006) 1.73
Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. J Med Chem (2012) 1.64
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. Cancer Res (2007) 1.62
Construction of human activity-based phosphorylation networks. Mol Syst Biol (2013) 1.59
Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. Mol Biosyst (2011) 1.58
Crystal structure of the SOCS2-elongin C-elongin B complex defines a prototypical SOCS box ubiquitin ligase. Proc Natl Acad Sci U S A (2006) 1.57
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem (2012) 1.55
Ruthenium half-sandwich complexes bound to protein kinase Pim-1. Angew Chem Int Ed Engl (2006) 1.54
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res (2013) 1.53
Dissection of PIM serine/threonine kinases in FLT3-ITD-induced leukemogenesis reveals PIM1 as regulator of CXCL12-CXCR4-mediated homing and migration. J Exp Med (2009) 1.52
Coupling PAF signaling to dynein regulation: structure of LIS1 in complex with PAF-acetylhydrolase. Neuron (2004) 1.51
UnPAKing the class differences among p21-activated kinases. Trends Biochem Sci (2008) 1.51
Girls homozygous for an IL-2-inducible T cell kinase mutation that leads to protein deficiency develop fatal EBV-associated lymphoproliferation. J Clin Invest (2009) 1.49
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J Med Chem (2011) 1.48
Effect of a glucose impulse on the CcpA regulon in Staphylococcus aureus. BMC Microbiol (2009) 1.46
Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases. J Biol Chem (2013) 1.46
Activation segment exchange: a common mechanism of kinase autophosphorylation? Trends Biochem Sci (2007) 1.45
Structure and regulation of the human Nek2 centrosomal kinase. J Biol Chem (2006) 1.45
Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva. J Biol Chem (2012) 1.43
Structural and functional characterization of the human protein kinase ASK1. Structure (2007) 1.42
Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation. Structure (2009) 1.36
Structure of the SOCS4-ElonginB/C complex reveals a distinct SOCS box interface and the molecular basis for SOCS-dependent EGFR degradation. Structure (2007) 1.35
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A (2013) 1.35
Kinase inhibitor selectivity profiling using differential scanning fluorimetry. Methods Mol Biol (2012) 1.35
Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs. Structure (2007) 1.34
Prion variant maintained only at high levels of the Hsp104 disaggregase. Curr Genet (2005) 1.33
Targeting group II PAKs in cancer and metastasis. Cancer Metastasis Rev (2009) 1.30
Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP. Cancer Cell (2013) 1.28
High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem Biol (2011) 1.27
A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B. J Cell Biol (2012) 1.27
DNA damage in oocytes induces a switch of the quality control factor TAp63α from dimer to tetramer. Cell (2011) 1.25
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Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc (2014) 1.23
Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem Biol (2014) 1.23
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. Bioorg Med Chem (2011) 1.23
Clinical relevance of circulating nucleosomes in cancer. Ann N Y Acad Sci (2008) 1.23
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. J Med Chem (2012) 1.23
Doing more than just the structure-structural genomics in kinase drug discovery. Curr Opin Chem Biol (2008) 1.19
Structural determinants of G-protein alpha subunit selectivity by regulator of G-protein signaling 2 (RGS2). J Biol Chem (2009) 1.16
Inhibition of protein-protein interactions: the discovery of druglike beta-catenin inhibitors by combining virtual and biophysical screening. Proteins (2006) 1.15
Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a. Proc Natl Acad Sci U S A (2003) 1.15
Pharmacological inhibition of LIM kinase stabilizes microtubules and inhibits neoplastic growth. Cancer Res (2012) 1.12
HMGB1 interacts differentially with members of the Rel family of transcription factors. Biochem Biophys Res Commun (2003) 1.12
Structurally sophisticated octahedral metal complexes as highly selective protein kinase inhibitors. J Am Chem Soc (2011) 1.11
High-throughput NMR-based screening with competition binding experiments. J Am Chem Soc (2002) 1.10
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. J Med Chem (2013) 1.09
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain. J Med Chem (2013) 1.08
Hot spots in Tcf4 for the interaction with beta-catenin. J Biol Chem (2003) 1.07
The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins. J Struct Funct Genomics (2007) 1.07
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. J Med Chem (2012) 1.04
Structures of Down syndrome kinases, DYRKs, reveal mechanisms of kinase activation and substrate recognition. Structure (2013) 1.03
Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. J Biol Chem (2014) 1.01
Rapid determination of multiple linear kinase substrate motifs by mass spectrometry. Chem Biol (2012) 1.01
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. J Med Chem (2013) 1.01
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