Published in Nat Chem Biol on January 15, 2006
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
Quantitative analysis of HSP90-client interactions reveals principles of substrate recognition. Cell (2012) 3.44
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature (2010) 3.39
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27
Pushing the limits of targeted therapy in chronic myeloid leukaemia. Nat Rev Cancer (2012) 2.35
The (un)targeted cancer kinome. Nat Chem Biol (2010) 2.33
Role of ABL family kinases in cancer: from leukaemia to solid tumours. Nat Rev Cancer (2013) 1.92
ABL tyrosine kinases: evolution of function, regulation, and specificity. Sci Signal (2010) 1.91
Src activates Abl to augment Robo1 expression in order to promote tumor cell migration. Oncotarget (2010) 1.52
Aurora kinase inhibitors as anticancer molecules. Biochim Biophys Acta (2010) 1.33
Myristoylation and membrane binding regulate c-Src stability and kinase activity. Mol Cell Biol (2010) 1.33
Mechanisms of drug resistance in kinases. Expert Opin Investig Drugs (2011) 1.29
A new screening assay for allosteric inhibitors of cSrc. Nat Chem Biol (2009) 1.16
Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol (2012) 1.14
Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One (2011) 1.12
Ten things you should know about protein kinases: IUPHAR Review 14. Br J Pharmacol (2015) 1.06
Computational modeling of allosteric communication reveals organizing principles of mutation-induced signaling in ABL and EGFR kinases. PLoS Comput Biol (2011) 1.06
Imaging the intracellular distribution of tyrosine kinase inhibitors in living cells with quantitative hyperspectral stimulated Raman scattering. Nat Chem (2014) 1.05
Targeting cancer with kinase inhibitors. J Clin Invest (2015) 1.05
N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem (2009) 1.04
NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors. Proc Natl Acad Sci U S A (2013) 1.03
c-Abl phosphorylates α-synuclein and regulates its degradation: implication for α-synuclein clearance and contribution to the pathogenesis of Parkinson's disease. Hum Mol Genet (2014) 1.03
The Abl SH2-kinase linker naturally adopts a conformation competent for SH3 domain binding. Protein Sci (2007) 1.01
Structure and dynamic regulation of Abl kinases. J Biol Chem (2013) 1.01
p63 the guardian of human reproduction. Cell Cycle (2012) 0.98
Current concepts in pediatric Philadelphia chromosome-positive acute lymphoblastic leukemia. Front Oncol (2014) 0.97
Reply to: Cisplatin-induced primordial follicle oocyte killing and loss of fertility are not prevented by imatinib. Nat Med (2012) 0.97
Allosteric inhibition of the nonMyristoylated c-Abl tyrosine kinase by phosphopeptides derived from Abi1/Hssh3bp1. Biochim Biophys Acta (2008) 0.96
A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem (2010) 0.96
The growing arsenal of ATP-competitive and allosteric inhibitors of BCR-ABL. Cancer Res (2012) 0.95
Insights into protein kinase regulation and inhibition by large scale structural comparison. Biochim Biophys Acta (2009) 0.95
Biochemical mechanisms of resistance to small-molecule protein kinase inhibitors. ACS Chem Biol (2010) 0.94
Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML. Leukemia (2010) 0.93
Small molecule probes of cellular pathways and networks. ACS Chem Biol (2010) 0.92
Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions. Chem Biol (2015) 0.91
Structure, regulation, signaling, and targeting of abl kinases in cancer. Genes Cancer (2012) 0.90
Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles. Nat Chem Biol (2012) 0.90
Enhanced SH3/linker interaction overcomes Abl kinase activation by gatekeeper and myristic acid binding pocket mutations and increases sensitivity to small molecule inhibitors. J Biol Chem (2013) 0.90
Molecular mechanisms for survival regulation of chronic myeloid leukemia stem cells. Protein Cell (2013) 0.90
Development of an effective therapy for chronic myelogenous leukemia. Cancer J (2011) 0.87
Development of an online p38α mitogen-activated protein kinase binding assay and integration of LC-HR-MS. Anal Bioanal Chem (2010) 0.87
The energy landscape analysis of cancer mutations in protein kinases. PLoS One (2011) 0.86
Crk and ABI1: binary molecular switches that regulate abl tyrosine kinase and signaling to the cytoskeleton. Genes Cancer (2012) 0.86
Innovation in academic chemical screening: filling the gaps in chemical biology. Curr Opin Chem Biol (2013) 0.85
A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer (2010) 0.85
Curcumin derivative C817 inhibits proliferation of imatinib-resistant chronic myeloid leukemia cells with wild-type or mutant Bcr-Abl in vitro. Acta Pharmacol Sin (2014) 0.85
p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia. Haematologica (2011) 0.85
Detection of secondary binding sites in proteins using fragment screening. Proc Natl Acad Sci U S A (2015) 0.83
Activation state-selective kinase inhibitor assay based on ion mobility-mass spectrometry. Anal Chem (2013) 0.83
Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I. BMC Cancer (2012) 0.83
Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. J Med Chem (2011) 0.83
Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem (2010) 0.83
SPLINTS: small-molecule protein ligand interface stabilizers. Curr Opin Struct Biol (2016) 0.82
Small molecule substrate phosphorylation site inhibitors of protein kinases: approaches and challenges. ACS Chem Biol (2014) 0.82
The human kinome and kinase inhibition. Curr Protoc Pharmacol (2013) 0.80
Oxidative Stress, DNA Damage, and c-Abl Signaling: At the Crossroad in Neurodegenerative Diseases? Int J Cell Biol (2012) 0.80
GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Cell Chem Biol (2016) 0.80
Misfolding, Aggregation, and Disordered Segments in c-Abl and p53 in Human Cancer. Front Oncol (2015) 0.79
Allosteric BCR-ABL inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia: novel opportunities for drug combinations to overcome resistance. Haematologica (2012) 0.79
Defying c-Abl signaling circuits through small allosteric compounds. Front Genet (2014) 0.79
Targeting GTPases in Parkinson's disease: comparison to the historic path of kinase drug discovery and perspectives. Front Mol Neurosci (2014) 0.79
The functional interplay between the t(9;22)-associated fusion proteins BCR/ABL and ABL/BCR in Philadelphia chromosome-positive acute lymphatic leukemia. PLoS Genet (2015) 0.78
Enhanced interrogation: emerging strategies for cell signaling inhibition. Nat Struct Mol Biol (2010) 0.78
Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions. Bioorg Med Chem (2011) 0.77
Abl Kinases Regulate HGF/Met Signaling Required for Epithelial Cell Scattering, Tubulogenesis and Motility. PLoS One (2015) 0.77
Molecular diagnostics, targeted therapy, and the indication for allogeneic stem cell transplantation in acute lymphoblastic leukemia. Adv Hematol (2011) 0.77
Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism. BMC Cancer (2012) 0.76
Allosteric Inhibition of Bcr-Abl Kinase by High Affinity Monobody Inhibitors Directed to the Src Homology 2 (SH2)-Kinase Interface. J Biol Chem (2016) 0.76
Fluorescence Polarization Screening Assays for Small Molecule Allosteric Modulators of ABL Kinase Function. PLoS One (2015) 0.76
Simultaneous protein expression and modification: an efficient approach for production of unphosphorylated and biotinylated receptor tyrosine kinases by triple infection in the baculovirus expression system. J Biomol Tech (2010) 0.76
Dynamics of protein kinases: insights from nuclear magnetic resonance. Acc Chem Res (2015) 0.76
The function of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) explored using a specific inhibitor that targets the PI5P-binding site. Biochem J (2015) 0.76
Opposing roles of KIT and ABL1 in the therapeutic response of gastrointestinal stromal tumor (GIST) cells to imatinib mesylate. Oncotarget (2016) 0.75
BCR: a new target in resistance mediated by BCR/ABL-315I? Genes Cancer (2016) 0.75
Overcoming resistance to HER2 inhibitors through state-specific kinase binding. Nat Chem Biol (2016) 0.75
Inhibitors of Bcr-abl... breaking new ground again. Nat Chem Biol (2006) 0.75
Identification of small molecules that disrupt signaling between ABL and its positive regulator RIN1. PLoS One (2015) 0.75
Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK. PLoS One (2017) 0.75
Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature (2012) 15.91
An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem (2009) 12.73
Generation of induced pluripotent stem cells using recombinant proteins. Cell Stem Cell (2009) 11.65
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther (2008) 10.35
EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res (2008) 9.29
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Engl J Med (2006) 8.26
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A (2007) 8.23
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell (2005) 7.99
Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell (2008) 7.79
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature (2009) 7.05
Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature (2008) 6.80
The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science (2011) 6.75
Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res (2008) 6.71
KCNQ1 gain-of-function mutation in familial atrial fibrillation. Science (2003) 6.60
MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A (2009) 6.58
A unifying model for mTORC1-mediated regulation of mRNA translation. Nature (2012) 6.44
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res (2005) 5.98
DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell (2009) 5.97
A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell Stem Cell (2008) 5.90
The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature (2012) 5.61
The TEAD/TEF family protein Scalloped mediates transcriptional output of the Hippo growth-regulatory pathway. Dev Cell (2008) 5.58
Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol (2006) 5.03
mTORC1-mediated cell proliferation, but not cell growth, controlled by the 4E-BPs. Science (2010) 4.81
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl Acad Sci U S A (2008) 4.80
Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov (2011) 4.80
Attenuated cold sensitivity in TRPM8 null mice. Neuron (2007) 4.73
miR-21 mediates fibrogenic activation of pulmonary fibroblasts and lung fibrosis. J Exp Med (2010) 4.71
Conversion of mouse fibroblasts into cardiomyocytes using a direct reprogramming strategy. Nat Cell Biol (2011) 4.64
Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell (2008) 4.63
Mitogenic influence of human R-spondin1 on the intestinal epithelium. Science (2005) 4.58
Insulin modulates gluconeogenesis by inhibition of the coactivator TORC2. Nature (2007) 4.54
A chemical platform for improved induction of human iPSCs. Nat Methods (2009) 4.54
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell (2004) 4.29
A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res (2011) 4.22
Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia. Nat Genet (2004) 3.96
Direct reprogramming of mouse fibroblasts to neural progenitors. Proc Natl Acad Sci U S A (2011) 3.93
Mesenchymal stem cell-mediated functional tooth regeneration in swine. PLoS One (2006) 3.91
Long-term self-renewal and directed differentiation of human embryonic stem cells in chemically defined conditions. Proc Natl Acad Sci U S A (2006) 3.90
White Collar-1, a circadian blue light photoreceptor, binding to the frequency promoter. Science (2002) 3.85
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A (2006) 3.83
Association between adverse clinical outcome in human disease caused by novel influenza A H7N9 virus and sustained viral shedding and emergence of antiviral resistance. Lancet (2013) 3.83
Reprogramming of human primary somatic cells by OCT4 and chemical compounds. Cell Stem Cell (2010) 3.82
Direct reprogramming of adult human fibroblasts to functional neurons under defined conditions. Cell Stem Cell (2011) 3.62
The renewal and differentiation of Isl1+ cardiovascular progenitors are controlled by a Wnt/beta-catenin pathway. Cell Stem Cell (2007) 3.54
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature (2010) 3.39
The role of YAP transcription coactivator in regulating stem cell self-renewal and differentiation. Genes Dev (2010) 3.37
Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med (2010) 3.26
R-Spondin1 regulates Wnt signaling by inhibiting internalization of LRP6. Proc Natl Acad Sci U S A (2007) 3.24
Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One (2011) 3.23
Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol (2008) 3.18
The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res (2010) 3.16
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat Chem Biol (2010) 3.15
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412. Cancer Cell (2002) 3.09
Metabolic oxidation regulates embryonic stem cell differentiation. Nat Chem Biol (2010) 3.06
Expansion of Bcr-Abl-positive leukemic stem cells is dependent on Hedgehog pathway activation. Cancer Cell (2008) 3.01
Revealing a core signaling regulatory mechanism for pluripotent stem cell survival and self-renewal by small molecules. Proc Natl Acad Sci U S A (2010) 3.01
White collar-1, a DNA binding transcription factor and a light sensor. Science (2002) 2.97
Characterization of the apical papilla and its residing stem cells from human immature permanent teeth: a pilot study. J Endod (2008) 2.95
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol (2011) 2.91
Practical reconstruction method for bioluminescence tomography. Opt Express (2005) 2.83
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. Structure (2005) 2.78
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther (2011) 2.73
mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science (2013) 2.71
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease. Cancer Cell (2003) 2.70
In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol (2011) 2.69
Identification of a KCNE2 gain-of-function mutation in patients with familial atrial fibrillation. Am J Hum Genet (2004) 2.66
Cryptochrome mediates circadian regulation of cAMP signaling and hepatic gluconeogenesis. Nat Med (2010) 2.65
Self-renewal of embryonic stem cells by a small molecule. Proc Natl Acad Sci U S A (2006) 2.65
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A (2007) 2.60
FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. Cancer Cell (2007) 2.56
A Kir2.1 gain-of-function mutation underlies familial atrial fibrillation. Biochem Biophys Res Commun (2005) 2.55
An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A (2006) 2.51
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov (2012) 2.47
CCL2/CCR2 pathway mediates recruitment of myeloid suppressor cells to cancers. Cancer Lett (2007) 2.43
Rapid induction and long-term self-renewal of primitive neural precursors from human embryonic stem cells by small molecule inhibitors. Proc Natl Acad Sci U S A (2011) 2.39
Pure spinal epidural cavernous hemangioma. Acta Neurochir (Wien) (2012) 2.38
Mesenchymal stem cells derived from human gingiva are capable of immunomodulatory functions and ameliorate inflammation-related tissue destruction in experimental colitis. J Immunol (2009) 2.37
Variable fitness impact of HIV-1 escape mutations to cytotoxic T lymphocyte (CTL) response. PLoS Pathog (2009) 2.36
Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nat Med (2011) 2.34
Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells (2009) 2.29
A general strategy for creating "inactive-conformation" abl inhibitors. Chem Biol (2006) 2.27
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol (2010) 2.26
A chemical approach to stem-cell biology and regenerative medicine. Nature (2008) 2.25
Diverse pathways generate microRNA-like RNAs and Dicer-independent small interfering RNAs in fungi. Mol Cell (2010) 2.23
Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res (2010) 2.20
Phosphoproteomic analysis of human embryonic stem cells. Cell Stem Cell (2009) 2.19