Published in Bioorg Med Chem Lett on May 14, 2013
Cancer therapy. Ex vivo culture of circulating breast tumor cells for individualized testing of drug susceptibility. Science (2014) 5.25
Targeting Plasmodium PI(4)K to eliminate malaria. Nature (2013) 2.49
PI3'-kinase inhibition forestalls the onset of MEK1/2 inhibitor resistance in BRAF-mutated melanoma. Cancer Discov (2014) 1.58
Oncogenic mutations weaken the interactions that stabilize the p110α-p85α heterodimer in phosphatidylinositol 3-kinase α. FEBS J (2015) 1.38
AXL mediates resistance to PI3Kα inhibition by activating the EGFR/PKC/mTOR axis in head and neck and esophageal squamous cell carcinomas. Cancer Cell (2015) 1.14
Targetable signaling pathway mutations are associated with malignant phenotype in IDH-mutant gliomas. Clin Cancer Res (2014) 1.02
Phosphoinositide 3-Kinase Regulates Glycolysis through Mobilization of Aldolase from the Actin Cytoskeleton. Cell (2016) 0.98
Somatic Activating PIK3CA Mutations Cause Venous Malformation. Am J Hum Genet (2015) 0.98
Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. J Clin Invest (2014) 0.94
Therapeutic targeting of cancers with loss of PTEN function. Curr Drug Targets (2014) 0.93
PI3K isoform dependence of PTEN-deficient tumors can be altered by the genetic context. Proc Natl Acad Sci U S A (2014) 0.93
Combined therapy with RAD001 e BEZ235 overcomes resistance of PET immortalized cell lines to mTOR inhibition. Oncotarget (2014) 0.91
The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther (2014) 0.91
Systematic Screening Identifies Dual PI3K and mTOR Inhibition as a Conserved Therapeutic Vulnerability in Osteosarcoma. Clin Cancer Res (2015) 0.88
Genomic profiling toward precision medicine in non-small cell lung cancer: getting beyond EGFR. Pharmgenomics Pers Med (2015) 0.88
A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer. Clin Cancer Res (2016) 0.88
The PTEN tumor suppressor gene and its role in lymphoma pathogenesis. Aging (Albany NY) (2015) 0.84
Enhanced PI3K p110α signaling confers acquired lapatinib resistance that can be effectively reversed by a p110α-selective PI3K inhibitor. Mol Cancer Ther (2013) 0.83
Discovery and functional characterization of a neomorphic PTEN mutation. Proc Natl Acad Sci U S A (2015) 0.82
Targeting the PI3K/Akt signaling pathway in gastric carcinoma: A reality for personalized medicine? World J Gastroenterol (2015) 0.82
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT). ACS Med Chem Lett (2015) 0.82
Structural basis of nSH2 regulation and lipid binding in PI3Kα. Oncotarget (2014) 0.79
Detection and manipulation of phosphoinositides. Biochim Biophys Acta (2014) 0.79
Population pharmacokinetics and pharmacodynamics of BYL719, a phosphoinositide 3-kinase antagonist, in adult patients with advanced solid malignancies. Br J Clin Pharmacol (2014) 0.79
The pivotal role of mammalian target of rapamycin inhibition in the treatment of patients with neuroendocrine tumors. Cancer Med (2016) 0.78
PIK3CAH1047R Accelerates and Enhances KRASG12D-Driven Lung Tumorigenesis. Cancer Res (2015) 0.78
Preclinical evaluation of PI3K inhibitor BYL719 as a single agent and its synergism in combination with cisplatin or MEK inhibitor in nasopharyngeal carcinoma (NPC). Am J Cancer Res (2015) 0.78
Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11. Protein Sci (2016) 0.78
BYL719, a selective inhibitor of phosphoinositide 3-Kinase α, enhances the effect of selumetinib (AZD6244, ARRY-142886) in KRAS-mutant non-small cell lung cancer. Invest New Drugs (2014) 0.78
Effects of novel isoform-selective phosphoinositide 3-kinase inhibitors on natural killer cell function. PLoS One (2014) 0.78
Dual targeting of acute myeloid leukemia progenitors by catalytic mTOR inhibition and blockade of the p110α subunit of PI3 kinase. Oncotarget (2015) 0.77
Phosphoinositide 3-kinase alpha-dependent regulation of branching morphogenesis in murine embryonic lung: evidence for a role in determining morphogenic properties of FGF7. PLoS One (2014) 0.77
Identification of differential PI3K pathway target dependencies in T-cell acute lymphoblastic leukemia through a large cancer cell panel screen. Oncotarget (2016) 0.77
Rationale-based therapeutic combinations with PI3K inhibitors in cancer treatment. Mol Cell Oncol (2014) 0.76
Coincident signals from GPCRs and receptor tyrosine kinases are uniquely transduced by PI3Kβ in myeloid cells. Sci Signal (2016) 0.75
PIK3CA-mutated melanoma cells rely on cooperative signaling through mTORC1/2 for sustained proliferation. Pigment Cell Melanoma Res (2017) 0.75
PIK3CA mutant tumors depend on oxoglutarate dehydrogenase. Proc Natl Acad Sci U S A (2017) 0.75
Identification of allosteric binding sites for PI3Kα oncogenic mutant specific inhibitor design. Bioorg Med Chem (2017) 0.75
PI3Kα inhibition reduces obesity in mice. Aging (Albany NY) (2016) 0.75
Tumour-specific PI3K inhibition via nanoparticle-targeted delivery in head and neck squamous cell carcinoma. Nat Commun (2017) 0.75
Dysregulations in the PI3K pathway and targeted therapies for head and neck squamous cell carcinoma. Oncotarget (2017) 0.75
Class I phosphatidylinositol 3-kinase inhibitors for cancer therapy. Acta Pharm Sin B (2016) 0.75
PI3K isoform inhibition associated with anti Bcr-Abl drugs shows in vitro increased anti-leukemic activity in Philadelphia chromosome-positive B-acute lymphoblastic leukemia cell lines. Oncotarget (2017) 0.75
The Inositide Signaling Pathway As a Target for Treating Gastric Cancer and Colorectal Cancer. Front Physiol (2016) 0.75
Specific inhibition of p110α subunit of PI3K: putative therapeutic strategy for KRAS mutant colorectal cancers. Oncotarget (2016) 0.75
Dual Inhibition of PI3K/Akt and mTOR by the Dietary Antioxidant, Delphinidin, Ameliorates Psoriatic Features In Vitro and in an Imiquimod-Induced Psoriasis-Like Disease in Mice. Antioxid Redox Signal (2016) 0.75
Combined Inhibition of CDK4/6 and PI3K/AKT/mTOR Pathways Induces a Synergistic Anti-Tumor Effect in Malignant Pleural Mesothelioma Cells. Neoplasia (2017) 0.75
PIK3CA mutations contribute to acquired cetuximab resistance in metastatic colorectal cancer patients. Clin Cancer Res (2017) 0.75
microRNA-143/145 loss induces Ras signaling to promote aggressive Pten-deficient basal-like breast cancer. JCI Insight (2017) 0.75
Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells. Prostate (2017) 0.75
INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC. Mol Cancer Res (2017) 0.75
The selective PI3Kα inhibitor BYL719 as a novel therapeutic option for neuroendocrine tumors: Results from multiple cell line models. PLoS One (2017) 0.75
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
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell (2005) 7.99
A genome-wide association study of psoriasis and psoriatic arthritis identifies new disease loci. PLoS Genet (2008) 5.85
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell (2004) 4.29
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
Large-scale prediction and testing of drug activity on side-effect targets. Nature (2012) 3.88
Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. Proc Natl Acad Sci U S A (2009) 3.26
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412. Cancer Cell (2002) 3.09
Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol (2006) 2.96
Association between the PTPN22 gene and rheumatoid arthritis and juvenile idiopathic arthritis in a UK population: further support that PTPN22 is an autoimmunity gene. Arthritis Rheum (2005) 2.93
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. Structure (2005) 2.78
Essential role for the p110delta phosphoinositide 3-kinase in the allergic response. Nature (2004) 2.73
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther (2011) 2.73
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease. Cancer Cell (2003) 2.70
FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. Cancer Cell (2007) 2.56
Analysis of pharmacology data and the prediction of adverse drug reactions and off-target effects from chemical structure. ChemMedChem (2007) 2.36
The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. Blood (2005) 2.14
Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol (2011) 2.06
Extended kinase profile and properties of the protein kinase inhibitor nilotinib. Biochim Biophys Acta (2009) 2.04
A public-private partnership to unlock the untargeted kinome. Nat Chem Biol (2013) 1.83
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood (2006) 1.83
AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res (2004) 1.82
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder. Proc Natl Acad Sci U S A (2004) 1.81
Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia. Cancer Res (2004) 1.79
Mapping adverse drug reactions in chemical space. J Med Chem (2009) 1.77
The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res (2007) 1.65
Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia. Acta Crystallogr D Biol Crystallogr (2006) 1.61
Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412. Blood (2005) 1.58
Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther (2014) 1.56
Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development. Drug Discov Today (2005) 1.55
Alkylamides from Echinacea are a new class of cannabinomimetics. Cannabinoid type 2 receptor-dependent and -independent immunomodulatory effects. J Biol Chem (2006) 1.54
Reducing safety-related drug attrition: the use of in vitro pharmacological profiling. Nat Rev Drug Discov (2012) 1.47
In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol Exp Ther (2006) 1.42
Gaining insight into off-target mediated effects of drug candidates with a comprehensive systems chemical biology analysis. J Chem Inf Model (2009) 1.40
Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth. Cancer Discov (2012) 1.37
PI3K and mTOR inhibitors: a new generation of targeted anticancer agents. Curr Opin Cell Biol (2009) 1.34
FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies. Oncogene (2005) 1.32
Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking. J Med Chem (2003) 1.30
RET/PTC-induced cell growth is mediated in part by epidermal growth factor receptor (EGFR) activation: evidence for molecular and functional interactions between RET and EGFR. Cancer Res (2008) 1.30
Classical PKC isoforms in cancer. Pharmacol Res (2007) 1.29
Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations. Mol Cancer Ther (2012) 1.26
Inhibition of protein kinase c-Src reduces the incidence of breast cancer metastases and increases survival in mice: implications for therapy. J Pharmacol Exp Ther (2006) 1.26
Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. Mini Rev Med Chem (2004) 1.26
Multicenter randomized phase II study of weekly or twice-weekly bortezomib plus rituximab in patients with relapsed or refractory follicular or marginal-zone B-cell lymphoma. J Clin Oncol (2009) 1.24
Crystalline histiocytosis in hereditary cysinosis. Arch Pathol Lab Med (2002) 1.23
Protein kinases as targets for anticancer agents: from inhibitors to useful drugs. Pharmacol Ther (2002) 1.22
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther (2010) 1.22
Therapeutic potential of phosphoinositide 3-kinase inhibitors. Chem Biol (2003) 1.21
Modeling promiscuity based on in vitro safety pharmacology profiling data. ChemMedChem (2007) 1.21
Phosphorylation regulates transcriptional activity of PAX3/FKHR and reveals novel therapeutic possibilities. Cancer Res (2008) 1.17
Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers. Clin Cancer Res (2014) 1.13
Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay. J Am Chem Soc (2010) 1.11
Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases. Blood (2002) 1.10
Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity. Gastroenterology (2006) 1.09
Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res (2013) 1.08
Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis. Sci Transl Med (2013) 1.08
Crystal structure of Clostridium botulinum neurotoxin protease in a product-bound state: Evidence for noncanonical zinc protease activity. Proc Natl Acad Sci U S A (2004) 1.08
Synthesis and target identification of hymenialdisine analogs. Chem Biol (2004) 1.05
FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model. Oncogene (2005) 1.05
SRC family kinases: potential targets for the treatment of human cancer and leukemia. Curr Pharm Des (2003) 1.05
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). Biochem J (2003) 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
The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death. Br J Pharmacol (2014) 1.01
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. J Med Chem (2007) 1.01
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors. Bioorg Med Chem Lett (2005) 1.00
Identification of the C3a receptor (C3AR1) as the target of the VGF-derived peptide TLQP-21 in rodent cells. J Biol Chem (2013) 1.00
Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach. Anal Biochem (2003) 1.00
Clustering and rule-based classifications of chemical structures evaluated in the biological activity space. J Chem Inf Model (2007) 0.99
A spiking neuron model of cortical correlates of sensorineural hearing loss: Spontaneous firing, synchrony, and tinnitus. Neural Comput (2006) 0.99
Nitric oxide induces degradation of the neutral ceramidase in rat renal mesangial cells and is counterregulated by protein kinase C. J Biol Chem (2002) 0.98
Functional redundancy of class I phosphoinositide 3-kinase (PI3K) isoforms in signaling growth factor-mediated human neutrophil survival. PLoS One (2012) 0.97
Targeted intestinal overexpression of the immediate early gene tis7 in transgenic mice increases triglyceride absorption and adiposity. J Biol Chem (2005) 0.96
Ceramide induces translocation of protein kinase C-alpha to the Golgi compartment of human embryonic kidney cells by interacting with the C2 domain. Biochim Biophys Acta (2003) 0.96
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit. Eur J Med Chem (2009) 0.94
Structural insights into the conformational selectivity of STI-571 and related kinase inhibitors. Curr Opin Drug Discov Devel (2004) 0.94
Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. J Clin Invest (2014) 0.94
Tracing pathway activities with kinase inhibitors and reverse phase protein arrays. Proteomics Clin Appl (2008) 0.92
Preliminary characterization and crystal structure of a thermostable cytochrome P450 from Thermus thermophilus. J Biol Chem (2002) 0.92
Randomized phase II adjuvant trial of dose-dense docetaxel before or after doxorubicin plus cyclophosphamide in axillary node-positive breast cancer. J Clin Oncol (2008) 0.92
Identification of apolipoprotein A-I as a "STOP" signal for myopia. Mol Cell Proteomics (2006) 0.91
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT. Haematologica (2007) 0.91
Structural biology contributions to tyrosine kinase drug discovery. Curr Opin Cell Biol (2009) 0.91
Stable expression of small interfering RNA sensitizes TEL-PDGFbetaR to inhibition with imatinib or rapamycin. J Clin Invest (2004) 0.90
7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem (2012) 0.90
Patupilone acts as radiosensitizing agent in multidrug-resistant cancer cells in vitro and in vivo. Clin Cancer Res (2005) 0.89
Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists. Naunyn Schmiedebergs Arch Pharmacol (2010) 0.88
Differential activation of the phosphatidylinositol 3'-kinase/Akt survival pathway by ionizing radiation in tumor and primary endothelial cells. Cancer Res (2004) 0.87
Effects of intravitreally and intraperitoneally injected atropine on two types of experimental myopia in chicken. Exp Eye Res (2006) 0.87
High-throughput in vitro profiling assays: lessons learnt from experiences at Novartis. Expert Opin Drug Metab Toxicol (2006) 0.86
Dipeptide nitrile inhibitors of cathepsin K. Bioorg Med Chem Lett (2006) 0.86
The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. Bioorg Med Chem (2013) 0.86
Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors. PLoS One (2013) 0.86