Published in Nat Chem Biol on February 19, 2012
Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol (2012) 1.14
Active site profiling reveals coupling between domains in SRC-family kinases. Nat Chem Biol (2012) 0.91
Selective targeting of distinct active site nucleophiles by irreversible SRC-family kinase inhibitors. J Am Chem Soc (2012) 0.90
Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett (2013) 0.87
Small molecule substrate phosphorylation site inhibitors of protein kinases: approaches and challenges. ACS Chem Biol (2014) 0.82
Identification of potential inhibitors based on compound proposal contest: Tyrosine-protein kinase Yes as a target. Sci Rep (2015) 0.81
Constitutive Activity in an Ancestral Form of Abl Tyrosine Kinase. PLoS One (2015) 0.76
Conformational transition paths harbor structures useful for aiding drug discovery and understanding enzymatic mechanisms in protein kinases. Protein Sci (2015) 0.75
Structural and Biochemical Basis for Intracellular Kinase Inhibition by Src-specific Peptidic Macrocycles. Cell Chem Biol (2016) 0.75
Coot: model-building tools for molecular graphics. Acta Crystallogr D Biol Crystallogr (2004) 227.01
PHENIX: building new software for automated crystallographic structure determination. Acta Crystallogr D Biol Crystallogr (2002) 53.61
The protein kinase complement of the human genome. Science (2002) 35.36
Likelihood-enhanced fast translation functions. Acta Crystallogr D Biol Crystallogr (2005) 29.38
A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
Crystal structure of the Src family tyrosine kinase Hck. Nature (1997) 7.66
Three-dimensional structure of the tyrosine kinase c-Src. Nature (1997) 7.62
Protein kinases--the major drug targets of the twenty-first century? Nat Rev Drug Discov (2002) 7.38
Catalytic specificity of protein-tyrosine kinases is critical for selective signalling. Nature (1995) 6.16
Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nat Rev Drug Discov (2002) 6.13
Crystal structures of c-Src reveal features of its autoinhibitory mechanism. Mol Cell (1999) 5.09
Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog. EMBO J (1997) 4.59
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol (2004) 4.40
Features of selective kinase inhibitors. Chem Biol (2005) 4.07
Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: by the GIMEMA Working Party on Chronic Myeloid Leukemia. Clin Cancer Res (2006) 3.47
A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol (2006) 3.40
Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol (2008) 3.18
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem (1989) 3.02
Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol (2006) 2.96
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. Structure (2005) 2.78
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease. Cancer Cell (2003) 2.70
High yield bacterial expression of active c-Abl and c-Src tyrosine kinases. Protein Sci (2005) 2.32
Recognition and specificity in protein tyrosine kinase-mediated signalling. Trends Biochem Sci (1995) 2.31
Characterization of pp60c-src tyrosine kinase activities using a continuous assay: autoactivation of the enzyme is an intermolecular autophosphorylation process. Biochemistry (1995) 2.13
How does a drug molecule find its target binding site? J Am Chem Soc (2011) 2.13
DNA-templated organic synthesis: nature's strategy for controlling chemical reactivity applied to synthetic molecules. Angew Chem Int Ed Engl (2004) 2.03
DNA-templated organic synthesis and selection of a library of macrocycles. Science (2004) 1.95
The generality of DNA-templated synthesis as a basis for evolving non-natural small molecules. J Am Chem Soc (2001) 1.88
c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty. Structure (2007) 1.87
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem (2008) 1.74
Combinatorial target-guided ligand assembly: identification of potent subtype-selective c-Src inhibitors. Proc Natl Acad Sci U S A (2000) 1.59
Translation of DNA into a library of 13,000 synthetic small-molecule macrocycles suitable for in vitro selection. J Am Chem Soc (2008) 1.23
Small-molecule discovery from DNA-encoded chemical libraries. Chem Soc Rev (2011) 1.20
Optimized selective N-methylation of peptides on solid support. J Pept Sci (2006) 1.18
Protein tyrosine kinase inhibitors as novel therapeutic agents. Pharmacol Ther (1999) 1.17
Highly sensitive in vitro selections for DNA-linked synthetic small molecules with protein binding affinity and specificity. J Am Chem Soc (2003) 1.15
In vitro selection of a DNA-templated small-molecule library reveals a class of macrocyclic kinase inhibitors. J Am Chem Soc (2010) 1.06
Restriction of Src activity by Cullin-5. Curr Biol (2009) 1.04
Kinase domain mutations in cancer: implications for small molecule drug design strategies. J Med Chem (2009) 0.98
A conserved salt bridge in the G loop of multiple protein kinases is important for catalysis and for in vivo Lyn function. Mol Cell (2009) 0.96
Biochemical mechanisms of resistance to small-molecule protein kinase inhibitors. ACS Chem Biol (2010) 0.94
Discovery of thienopyridines as Src-family selective Lck inhibitors. Bioorg Med Chem Lett (2006) 0.80
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight. Bioorg Med Chem Lett (2002) 0.78
Conversion of 5-methylcytosine to 5-hydroxymethylcytosine in mammalian DNA by MLL partner TET1. Science (2009) 32.97
High-throughput profiling of off-target DNA cleavage reveals RNA-programmed Cas9 nuclease specificity. Nat Biotechnol (2013) 8.40
The behaviour of 5-hydroxymethylcytosine in bisulfite sequencing. PLoS One (2010) 8.10
Revealing off-target cleavage specificities of zinc-finger nucleases by in vitro selection. Nat Methods (2011) 6.90
A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell (2009) 4.64
Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol (2008) 3.18
A system for the continuous directed evolution of biomolecules. Nature (2011) 2.77
The pathogen-associated iroA gene cluster mediates bacterial evasion of lipocalin 2. Proc Natl Acad Sci U S A (2006) 2.63
Supercharging proteins can impart unusual resilience. J Am Chem Soc (2007) 2.52
How pathogenic bacteria evade mammalian sabotage in the battle for iron. Nat Chem Biol (2006) 2.45
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms. Mol Cell (2011) 2.35
A conserved protonation-dependent switch controls drug binding in the Abl kinase. Proc Natl Acad Sci U S A (2008) 2.18
Directed evolution and substrate specificity profile of homing endonuclease I-SceI. J Am Chem Soc (2006) 2.18
Opposing effects of Tcf3 and Tcf1 control Wnt stimulation of embryonic stem cell self-renewal. Nat Cell Biol (2011) 2.13
How does a drug molecule find its target binding site? J Am Chem Soc (2011) 2.13
DNA-templated organic synthesis: nature's strategy for controlling chemical reactivity applied to synthetic molecules. Angew Chem Int Ed Engl (2004) 2.03
Reaction discovery enabled by DNA-templated synthesis and in vitro selection. Nature (2004) 1.99
Mammalian cell penetration, siRNA transfection, and DNA transfection by supercharged proteins. Proc Natl Acad Sci U S A (2009) 1.95
DNA-templated organic synthesis and selection of a library of macrocycles. Science (2004) 1.95
Engineering a ligand-dependent RNA transcriptional activator. Chem Biol (2004) 1.94
Photoswitching mechanism of cyanine dyes. J Am Chem Soc (2009) 1.86
A general strategy for the evolution of bond-forming enzymes using yeast display. Proc Natl Acad Sci U S A (2011) 1.85
Autonomous multistep organic synthesis in a single isothermal solution mediated by a DNA walker. Nat Nanotechnol (2010) 1.84
A conserved mechanism of DEAD-box ATPase activation by nucleoporins and InsP6 in mRNA export. Nature (2011) 1.70
Discovery and biological characterization of geranylated RNA in bacteria. Nat Chem Biol (2012) 1.70
In vivo evolution of an RNA-based transcriptional activator. Chem Biol (2003) 1.69
Structural basis for the recognition of c-Src by its inactivator Csk. Cell (2008) 1.66
A de novo protein binding pair by computational design and directed evolution. Mol Cell (2011) 1.65
In vivo evolution of an RNA-based transcriptional silencing domain in S. cerevisiae. Chem Biol (2007) 1.56
Expanding the reaction scope of DNA-templated synthesis. Angew Chem Int Ed Engl (2002) 1.56
A biomolecule-compatible visible-light-induced azide reduction from a DNA-encoded reaction-discovery system. Nat Chem (2011) 1.54
In vitro characterization of IroB, a pathogen-associated C-glycosyltransferase. Proc Natl Acad Sci U S A (2004) 1.52
Sequence-controlled polymers. Science (2013) 1.50
In vitro characterization of salmochelin and enterobactin trilactone hydrolases IroD, IroE, and Fes. J Am Chem Soc (2005) 1.47
In silico abstraction of zinc finger nuclease cleavage profiles reveals an expanded landscape of off-target sites. Nucleic Acids Res (2013) 1.46
Directed evolution of ligand dependence: small-molecule-activated protein splicing. Proc Natl Acad Sci U S A (2004) 1.46
Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol (2012) 1.46
Potent delivery of functional proteins into Mammalian cells in vitro and in vivo using a supercharged protein. ACS Chem Biol (2010) 1.42
Multistep small-molecule synthesis programmed by DNA templates. J Am Chem Soc (2002) 1.42
Enzyme-free translation of DNA into sequence-defined synthetic polymers structurally unrelated to nucleic acids. Nat Chem (2013) 1.41
Efficient and sequence-specific DNA-templated polymerization of peptide nucleic acid aldehydes. J Am Chem Soc (2003) 1.41
LC/MS analysis of cellular RNA reveals NAD-linked RNA. Nat Chem Biol (2009) 1.29
A protein interaction surface in nonribosomal peptide synthesis mapped by combinatorial mutagenesis and selection. Proc Natl Acad Sci U S A (2006) 1.28
Development and initial application of a hybridization-independent, DNA-encoded reaction discovery system compatible with organic solvents. J Am Chem Soc (2007) 1.25
Translation of DNA into a library of 13,000 synthetic small-molecule macrocycles suitable for in vitro selection. J Am Chem Soc (2008) 1.23
Three different binding sites of Cks1 are required for p27-ubiquitin ligation. J Biol Chem (2002) 1.20
Nucleic acid evolution and minimization by nonhomologous random recombination. Nat Biotechnol (2002) 1.20
Small-molecule discovery from DNA-encoded chemical libraries. Chem Soc Rev (2011) 1.20
DNA-templated polymerization of side-chain-functionalized peptide nucleic acid aldehydes. J Am Chem Soc (2008) 1.18
A class of human proteins that deliver functional proteins into mammalian cells in vitro and in vivo. Chem Biol (2011) 1.16
Highly sensitive in vitro selections for DNA-linked synthetic small molecules with protein binding affinity and specificity. J Am Chem Soc (2003) 1.15
Directed evolution can rapidly improve the activity of chimeric assembly-line enzymes. Proc Natl Acad Sci U S A (2007) 1.15
Creating small-molecule-dependent switches to modulate biological functions. Chem Biol (2005) 1.14
A chemical screen for biological small molecule-RNA conjugates reveals CoA-linked RNA. Proc Natl Acad Sci U S A (2009) 1.12
Mechanism of CDK5/p25 binding by CDK inhibitors. J Med Chem (2005) 1.11
Localized protein interaction surfaces on the EntB carrier protein revealed by combinatorial mutagenesis and selection. J Am Chem Soc (2006) 1.10
Experimental interrogation of the path dependence and stochasticity of protein evolution using phage-assisted continuous evolution. Proc Natl Acad Sci U S A (2013) 1.09
Enzymatic tailoring of enterobactin alters membrane partitioning and iron acquisition. ACS Chem Biol (2006) 1.09
Directing otherwise incompatible reactions in a single solution by using DNA-templated organic synthesis. Angew Chem Int Ed Engl (2002) 1.08
Control of transcription factor activity and osteoblast differentiation in mammalian cells using an evolved small-molecule-dependent intein. J Am Chem Soc (2006) 1.07
In vitro selection of a DNA-templated small-molecule library reveals a class of macrocyclic kinase inhibitors. J Am Chem Soc (2010) 1.06
Two enabling architectures for DNA-templated organic synthesis. Angew Chem Int Ed Engl (2003) 1.06
Directed evolution of protein enzymes using nonhomologous random recombination. Proc Natl Acad Sci U S A (2004) 1.05
Directed evolution of a small-molecule-triggered intein with improved splicing properties in mammalian cells. Chem Biol (2011) 1.05
Ordered multistep synthesis in a single solution directed by DNA templates. Angew Chem Int Ed Engl (2005) 1.04
N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem (2009) 1.04
Recent advances in the in vitro evolution of nucleic acids. Curr Opin Chem Biol (2002) 1.03
Interaction-dependent PCR: identification of ligand-target pairs from libraries of ligands and libraries of targets in a single solution-phase experiment. J Am Chem Soc (2010) 1.03
An in vitro translation, selection and amplification system for peptide nucleic acids. Nat Chem Biol (2009) 1.02
Inhibition of bacterial conjugation by phage M13 and its protein g3p: quantitative analysis and model. PLoS One (2011) 1.00
A sequential strand-displacement strategy enables efficient six-step DNA-templated synthesis. J Am Chem Soc (2011) 0.98
Engineering and identifying supercharged proteins for macromolecule delivery into mammalian cells. Methods Enzymol (2012) 0.97
A population-based experimental model for protein evolution: effects of mutation rate and selection stringency on evolutionary outcomes. Biochemistry (2013) 0.97
Tuning a three-component reaction for trapping kinase substrate complexes. J Am Chem Soc (2008) 0.96
Recent progress toward the templated synthesis and directed evolution of sequence-defined synthetic polymers. Chem Biol (2009) 0.96
A novel activating, germline JAK2 mutation, JAK2R564Q, causes familial essential thrombocytosis. Blood (2013) 0.96
Cellular uptake mechanisms and endosomal trafficking of supercharged proteins. Chem Biol (2012) 0.95
An in vivo selection system for homing endonuclease activity. Nucleic Acids Res (2002) 0.94
An intein-based genetic selection allows the construction of a high-quality library of binary patterned de novo protein sequences. Protein Eng Des Sel (2005) 0.93
DNA-enabled self-assembly of plasmonic nanoclusters. Nano Lett (2011) 0.92
DNA-templated functional group transformations enable sequence-programmed synthesis using small-molecule reagents. J Am Chem Soc (2005) 0.92
Dissecting protein structure and function using directed evolution. Nat Methods (2007) 0.91
Enhanced functional potential of nucleic acid aptamer libraries patterned to increase secondary structure. J Am Chem Soc (2010) 0.90
Templated synthesis of peptide nucleic acids via sequence-selective base-filling reactions. J Am Chem Soc (2009) 0.90
Comparative analysis of mutant tyrosine kinase chemical rescue. Biochemistry (2009) 0.89
Effects of template sequence and secondary structure on DNA-templated reactivity. J Am Chem Soc (2008) 0.89
DNA ligase-mediated translation of DNA into densely functionalized nucleic acid polymers. J Am Chem Soc (2012) 0.89
Folding and fibril formation of the cell cycle protein Cks1. J Biol Chem (2006) 0.89
Synthesis of acyclic alpha,beta-unsaturated ketones via Pd(II)-catalyzed intermolecular reaction of alkynamides and alkenes. J Am Chem Soc (2007) 0.87
Translation of DNA into synthetic N-acyloxazolidines. J Am Chem Soc (2004) 0.86
Activation of ubiquitin ligase SCF(Skp2) by Cks1: insights from hydrogen exchange mass spectrometry. J Mol Biol (2006) 0.86
Solving chemical problems through the application of evolutionary principles. Curr Opin Chem Biol (2007) 0.84
Small-molecule diversification from iterated branching reaction pathways enabled by DNA-templated synthesis. Angew Chem Int Ed Engl (2005) 0.84
Stereoselectivity in DNA-templated organic synthesis and its origins. J Am Chem Soc (2003) 0.84
Identification of ligand-target pairs from combined libraries of small molecules and unpurified protein targets in cell lysates. J Am Chem Soc (2014) 0.82
Reactivity-dependent PCR: direct, solution-phase in vitro selection for bond formation. J Am Chem Soc (2009) 0.82
DNA-templated synthesis in organic solvents. Chembiochem (2006) 0.82
Bromoenterobactins as potent inhibitors of a pathogen-associated, siderophore-modifying C-glycosyltransferase. J Am Chem Soc (2006) 0.82
Targeting conformational plasticity of protein kinases. ACS Chem Biol (2014) 0.82