Published in Biochem J on January 15, 2008
Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer (2009) 12.92
The emerging mechanisms of isoform-specific PI3K signalling. Nat Rev Mol Cell Biol (2010) 6.28
Helical domain and kinase domain mutations in p110alpha of phosphatidylinositol 3-kinase induce gain of function by different mechanisms. Proc Natl Acad Sci U S A (2008) 3.99
Class I PI3K in oncogenic cellular transformation. Oncogene (2008) 3.90
A frequent kinase domain mutation that changes the interaction between PI3Kalpha and the membrane. Proc Natl Acad Sci U S A (2009) 2.85
Oncogenic mutations mimic and enhance dynamic events in the natural activation of phosphoinositide 3-kinase p110α (PIK3CA). Proc Natl Acad Sci U S A (2012) 2.04
A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J (2011) 1.57
H1047R phosphatidylinositol 3-kinase mutant enhances HER2-mediated transformation by heregulin production and activation of HER3. Oncogene (2010) 1.56
Dynamics of the phosphoinositide 3-kinase p110δ interaction with p85α and membranes reveals aspects of regulation distinct from p110α. Structure (2011) 1.48
Differential enhancement of breast cancer cell motility and metastasis by helical and kinase domain mutations of class IA phosphoinositide 3-kinase. Cancer Res (2009) 1.45
Structural comparisons of class I phosphoinositide 3-kinases. Nat Rev Cancer (2008) 1.42
Oncogenic mutations weaken the interactions that stabilize the p110α-p85α heterodimer in phosphatidylinositol 3-kinase α. FEBS J (2015) 1.38
Insights into the oncogenic effects of PIK3CA mutations from the structure of p110alpha/p85alpha. Cell Cycle (2008) 1.35
Hot-spot mutations in p110alpha of phosphatidylinositol 3-kinase (pI3K): differential interactions with the regulatory subunit p85 and with RAS. Cell Cycle (2010) 1.22
The regulation of class IA PI 3-kinases by inter-subunit interactions. Curr Top Microbiol Immunol (2010) 1.16
Phosphatidylinositol 3-kinase: the oncoprotein. Curr Top Microbiol Immunol (2010) 1.14
Regulation of lipid binding underlies the activation mechanism of class IA PI3-kinases. Oncogene (2011) 1.14
PI3K/Akt/mTOR signaling pathway and targeted therapy for glioblastoma. Oncotarget (2016) 1.02
Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations. Cancer Res (2015) 1.01
The Key Role of Calmodulin in KRAS-Driven Adenocarcinomas. Mol Cancer Res (2015) 0.96
PI3K/PTEN/Akt pathway status affects the sensitivity of high-grade glioma cell cultures to the insulin-like growth factor-1 receptor inhibitor NVP-AEW541. Neuro Oncol (2010) 0.92
Model-based global sensitivity analysis as applied to identification of anti-cancer drug targets and biomarkers of drug resistance in the ErbB2/3 network. Eur J Pharm Sci (2011) 0.91
Structural effects of oncogenic PI3Kα mutations. Curr Top Microbiol Immunol (2010) 0.87
Investigating the structure and dynamics of the PIK3CA wild-type and H1047R oncogenic mutant. PLoS Comput Biol (2014) 0.86
Phosphatidylinositol 3-kinase-dependent activation of mammalian protein kinase B/Akt in Saccharomyces cerevisiae, an in vivo model for the functional study of Akt mutations. J Biol Chem (2009) 0.85
PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control. PLoS Biol (2013) 0.85
Activation of PI3Kα by physiological effectors and by oncogenic mutations: structural and dynamic effects. Biophys Rev (2014) 0.84
Phosphatidylinositol 4,5-bisphosphate-specific AKT1 is oncogenic. Int J Cancer (2010) 0.84
Conditional loss of ErbB3 delays mammary gland hyperplasia induced by mutant PIK3CA without affecting mammary tumor latency, gene expression, or signaling. Cancer Res (2013) 0.83
Kinetic analysis of PI3K reactions with fluorescent PIP2 derivatives. Anal Bioanal Chem (2011) 0.83
Somatic mutations in PI3Kalpha: structural basis for enzyme activation and drug design. Biochim Biophys Acta (2009) 0.82
LYN-activating mutations mediate antiestrogen resistance in estrogen receptor-positive breast cancer. J Clin Invest (2014) 0.81
Docking studies on isoform-specific inhibition of phosphoinositide-3-kinases. J Chem Inf Model (2010) 0.81
Capitalizing on tumor genotyping: towards the design of mutation specific inhibitors of phosphoinsitide-3-kinase. Adv Enzyme Regul (2010) 0.81
New and emerging factors in tumorigenesis: an overview. Cancer Manag Res (2015) 0.80
Structural basis of nSH2 regulation and lipid binding in PI3Kα. Oncotarget (2014) 0.79
Autophosphorylation of serine 608 in the p85 regulatory subunit of wild type or cancer-associated mutants of phosphoinositide 3-kinase does not affect its lipid kinase activity. BMC Biochem (2012) 0.79
Preclinical Efficacy of Ron Kinase Inhibitors Alone and in Combination with PI3K Inhibitors for Treatment of sfRon-Expressing Breast Cancer Patient-Derived Xenografts. Clin Cancer Res (2015) 0.78
The tumor suppressor PTEN and the PDK1 kinase regulate formation of the columnar neural epithelium. Elife (2016) 0.77
p110α Hot Spot Mutations E545K and H1047R Exert Metabolic Reprogramming Independently of p110α Kinase Activity. Mol Cell Biol (2015) 0.75
Insights into the pathological mechanisms of p85α mutations using a yeast-based phosphatidylinositol 3-kinase model. Biosci Rep (2017) 0.75
Calmodulin and PI3K Signaling in KRAS Cancers. Trends Cancer (2017) 0.75
PI3K Signaling in Tissue Hyper-Proliferation: From Overgrowth Syndromes to Kidney Cysts. Cancers (Basel) (2017) 0.75
Assessing the subcellular distribution of oncogenic phosphoinositide 3-kinase using microinjection into live cells. Biosci Rep (2014) 0.75
Identification of allosteric binding sites for PI3Kα oncogenic mutant specific inhibitor design. Bioorg Med Chem (2017) 0.75
Definition of the binding mode of phosphoinositide 3-kinase α-selective inhibitor A-66S through molecular dynamics simulation. J Mol Model (2014) 0.75
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature (2011) 8.29
ATP citrate lyase inhibition can suppress tumor cell growth. Cancer Cell (2005) 7.65
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature (2012) 7.01
Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists. Methods Biochem Anal (2005) 5.37
Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell (2011) 4.90
Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas. Proc Natl Acad Sci U S A (2010) 4.52
Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res (2006) 4.20
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol (2012) 3.89
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27). Proc Natl Acad Sci U S A (2012) 3.22
Chromatin proteins and modifications as drug targets. Nature (2013) 2.60
Residence time of receptor-ligand complexes and its effect on biological function. Biochemistry (2008) 2.47
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood (2013) 2.28
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A (2013) 2.26
Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res (2008) 2.15
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem (2002) 1.94
Aggrecan protects cartilage collagen from proteolytic cleavage. J Biol Chem (2003) 1.93
Interleukin-1F7B (IL-1H4/IL-1F7) is processed by caspase-1 and mature IL-1F7B binds to the IL-18 receptor but does not induce IFN-gamma production. Cytokine (2002) 1.92
Chemogenetic analysis of human protein methyltransferases. Chem Biol Drug Des (2011) 1.77
Yersiniabactin synthetase: a four-protein assembly line producing the nonribosomal peptide/polyketide hybrid siderophore of Yersinia pestis. Chem Biol (2002) 1.75
Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A (2010) 1.72
Induced-fit tightens pleuromutilins binding to ribosomes and remote interactions enable their selectivity. Proc Natl Acad Sci U S A (2007) 1.46
The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states. FEBS Lett (2011) 1.42
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem (2008) 1.41
ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism. Nat Chem Biol (2007) 1.39
A biochemical rationale for the anticancer effects of Hsp90 inhibitors: slow, tight binding inhibition by geldanamycin and its analogues. Proc Natl Acad Sci U S A (2006) 1.38
Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther (2014) 1.37
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens. J Biomol Screen (2012) 1.30
GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther (2009) 1.27
GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther (2009) 1.25
Biochemical characterization of the interactions of the novel pleuromutilin derivative retapamulin with bacterial ribosomes. Antimicrob Agents Chemother (2006) 1.22
Mechanism of inhibition of human KSP by ispinesib. Biochemistry (2008) 1.21
Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity. Mol Cancer Ther (2005) 1.20
Cancer epigenetics drug discovery and development: the challenge of hitting the mark. J Clin Invest (2014) 1.20
Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem Biol (2011) 1.20
Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation. Epigenetics (2012) 1.19
BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One (2013) 1.19
Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem (2007) 1.18
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. J Am Chem Soc (2002) 1.18
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. Oncotarget (2013) 1.17
Arresting initiation of hepatitis C virus RNA synthesis using heterocyclic derivatives. J Biol Chem (2003) 1.15
Evidence for allosteric interactions of antagonist binding to the smoothened receptor. J Pharmacol Exp Ther (2009) 1.13
Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis. Cancer Res (2009) 1.13
A second p53 binding site in the central domain of Mdm2 is essential for p53 ubiquitination. Biochemistry (2006) 1.13
Phylogenomics of phosphoinositide lipid kinases: perspectives on the evolution of second messenger signaling and drug discovery. BMC Evol Biol (2011) 1.12
Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L. Chem Biol Drug Des (2012) 1.12
Binding of TPX2 to Aurora A alters substrate and inhibitor interactions. Biochemistry (2007) 1.12
Crystal structure of the kinase domain of serum and glucocorticoid-regulated kinase 1 in complex with AMP PNP. Protein Sci (2007) 1.11
From 'gills to pills': urotensin-II as a regulator of mammalian cardiorenal function. Trends Pharmacol Sci (2004) 1.09
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase. J Med Chem (2006) 1.09
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. J Med Chem (2007) 1.06
A687V EZH2 is a gain-of-function mutation found in lymphoma patients. FEBS Lett (2012) 1.06
Enzymatic characterization of the pancreatic islet-specific glucose-6-phosphatase-related protein (IGRP). J Biol Chem (2004) 1.06
Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br J Pharmacol (2005) 1.05
Mechanism of inhibition of human KSP by monastrol: insights from kinetic analysis and the effect of ionic strength on KSP inhibition. Biochemistry (2004) 1.04
Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors. Proc Natl Acad Sci U S A (2002) 1.03
ALDH1A1 is a novel EZH2 target gene in epithelial ovarian cancer identified by genome-wide approaches. Cancer Prev Res (Phila) (2011) 1.03
Modulation of kinase-inhibitor interactions by auxiliary protein binding: crystallography studies on Aurora A interactions with VX-680 and with TPX2. Protein Sci (2008) 1.02
Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLoS One (2013) 1.02
Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor. Biochem Biophys Res Commun (2011) 1.01
An assay for Fe(II)/2-oxoglutarate-dependent dioxygenases by enzyme-coupled detection of succinate formation. Anal Biochem (2006) 1.00
Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1. Biochem J (2009) 0.98
Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem (2007) 0.96
Targeting epigenetic regulators for cancer therapy. Ann N Y Acad Sci (2014) 0.95
Fluorescence polarization method to characterize macrolide-ribosome interactions. Antimicrob Agents Chemother (2005) 0.95
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem (2010) 0.92