Published in Org Biomol Chem on June 14, 2004
Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance. Cancer Res (2009) 3.59
The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther (2005) 1.46
A patient tumor transplant model of squamous cell cancer identifies PI3K inhibitors as candidate therapeutics in defined molecular bins. Mol Oncol (2013) 1.28
Cellular and in vivo activity of a novel PI3K inhibitor, PX-866, against human glioblastoma. Neuro Oncol (2010) 1.27
The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling. Cancer Chemother Pharmacol (2006) 1.03
Slow self-activation enhances the potency of viridin prodrugs. J Med Chem (2008) 0.99
Regulation of morphogenesis and biocontrol properties in Trichoderma virens by a VELVET protein, Vel1. Appl Environ Microbiol (2010) 0.96
Molecular targets and mechanisms of radiosensitization using DNA damage response pathways. Future Oncol (2013) 0.93
Total synthesis of (-)-CP2-disorazole C1. Org Lett (2011) 0.89
A secondary metabolite biosynthesis cluster in Trichoderma virens: evidence from analysis of genes underexpressed in a mutant defective in morphogenesis and antibiotic production. Curr Genet (2006) 0.89
Molecular insights into the membrane-associated phosphatidylinositol 4-kinase IIα. Nat Commun (2014) 0.86
A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer. Oral Oncol (2015) 0.85
A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours. Br J Cancer (2013) 0.84
Somatic mutations in PI3Kalpha: structural basis for enzyme activation and drug design. Biochim Biophys Acta (2009) 0.82
A stabilized demethoxyviridin derivative inhibits PI3 kinase. Bioorg Med Chem Lett (2009) 0.79
Regioselective Palladium-Catalyzed Cross-Coupling Reactions of 2,4,7-Trichloroquinazoline. Synlett (2010) 0.78
Pharmacologic profiling of phosphoinositide 3-kinase inhibitors as mitigators of ionizing radiation-induced cell death. J Pharmacol Exp Ther (2013) 0.76
A multicenter phase 1 study of PX-866 and cetuximab in patients with metastatic colorectal carcinoma or recurrent/metastatic squamous cell carcinoma of the head and neck. Invest New Drugs (2014) 0.76
Rationale-based therapeutic combinations with PI3K inhibitors in cancer treatment. Mol Cell Oncol (2014) 0.76
Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. J Med Chem (2016) 0.75
Improved synthesis of 17β-hydroxy-16α-iodo-wortmannin, 17β-hydroxy-16α-iodoPX866, and the [(131)I] analogue as useful PET tracers for PI3-kinase. Bioorg Med Chem (2013) 0.75
Synthesis of 1,2,4-triazines and the triazinoisoquinolinedione DEF ring system of noelaquinone. Org Biomol Chem (2012) 0.75
Regulation of hypoxia-inducible factor 1alpha expression and function by the mammalian target of rapamycin. Mol Cell Biol (2002) 5.39
Hypoxia: importance in tumor biology, noninvasive measurement by imaging, and value of its measurement in the management of cancer therapy. Int J Radiat Biol (2006) 3.98
Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance. Cancer Res (2009) 3.59
Effect of KRAS oncogene substitutions on protein behavior: implications for signaling and clinical outcome. J Natl Cancer Inst (2012) 2.79
Genotoxic stress targets human Chk1 for degradation by the ubiquitin-proteasome pathway. Mol Cell (2005) 2.75
The absence of mitochondrial thioredoxin 2 causes massive apoptosis, exencephaly, and early embryonic lethality in homozygous mice. Mol Cell Biol (2003) 2.52
HIF-1 regulation: not so easy come, easy go. Trends Biochem Sci (2008) 2.37
Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha. Mol Cancer Ther (2004) 2.32
Stability of phosphoprotein as a biological marker of tumor signaling. Clin Cancer Res (2005) 2.31
Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling. Mol Cancer Ther (2004) 2.25
Comparative metabolic flux profiling of melanoma cell lines: beyond the Warburg effect. J Biol Chem (2011) 2.24
The hypoxia-associated factor switches cells from HIF-1α- to HIF-2α-dependent signaling promoting stem cell characteristics, aggressive tumor growth and invasion. Cancer Res (2011) 2.21
Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res (2010) 2.18
Redox potential of human thioredoxin 1 and identification of a second dithiol/disulfide motif. J Biol Chem (2003) 2.14
Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis. Cancer Res (2009) 1.98
Hypoxia inducible factor-1alpha as a cancer drug target. Mol Cancer Ther (2004) 1.92
Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents. Clin Cancer Res (2012) 1.92
Increased expression of thioredoxin-1 in human colorectal cancer is associated with decreased patient survival. J Lab Clin Med (2003) 1.92
Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorg Med Chem (2004) 1.77
Phosphatidylinositol 3-kinase mediates bronchioalveolar stem cell expansion in mouse models of oncogenic K-ras-induced lung cancer. PLoS One (2008) 1.72
Differential effects of rapamycin on mammalian target of rapamycin signaling functions in mammalian cells. Cancer Res (2003) 1.69
The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol Cancer Ther (2003) 1.65
The promise of patient-derived xenografts: the best laid plans of mice and men. Clin Cancer Res (2012) 1.63
The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures. Mol Cancer Ther (2007) 1.62
Passing the baton: the HIF switch. Trends Biochem Sci (2012) 1.58
Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Mol Cancer Ther (2008) 1.52
Increased expression of mitochondrial peroxiredoxin-3 (thioredoxin peroxidase-2) protects cancer cells against hypoxia and drug-induced hydrogen peroxide-dependent apoptosis. Mol Cancer Res (2003) 1.47
The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther (2005) 1.46
Hypoxia-associated factor, a novel E3-ubiquitin ligase, binds and ubiquitinates hypoxia-inducible factor 1alpha, leading to its oxygen-independent degradation. Mol Cell Biol (2008) 1.46
Dynamic contrast-enhanced and diffusion MRI show rapid and dramatic changes in tumor microenvironment in response to inhibition of HIF-1alpha using PX-478. Neoplasia (2005) 1.45
Thioredoxin-1 binds to the C2 domain of PTEN inhibiting PTEN's lipid phosphatase activity and membrane binding: a mechanism for the functional loss of PTEN's tumor suppressor activity. Arch Biochem Biophys (2004) 1.44
REDD1, an inhibitor of mTOR signalling, is regulated by the CUL4A-DDB1 ubiquitin ligase. EMBO Rep (2009) 1.44
Chemistry and biology of wortmannin. Org Biomol Chem (2005) 1.43
Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy. Mol Cancer Ther (2009) 1.34
Cellular and in vivo activity of a novel PI3K inhibitor, PX-866, against human glioblastoma. Neuro Oncol (2010) 1.27
OSU-03012 promotes caspase-independent but PERK-, cathepsin B-, BID-, and AIF-dependent killing of transformed cells. Mol Pharmacol (2006) 1.26
Cardiac restricted overexpression of kinase-dead mammalian target of rapamycin (mTOR) mutant impairs the mTOR-mediated signaling and cardiac function. J Biol Chem (2008) 1.24
Radiosensitization and stromal imaging response correlates for the HIF-1 inhibitor PX-478 given with or without chemotherapy in pancreatic cancer. Mol Cancer Ther (2010) 1.20
The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Mol Cancer Ther (2009) 1.19
The thioredoxin-1 inhibitor 1-methylpropyl 2-imidazolyl disulfide (PX-12) decreases vascular permeability in tumor xenografts monitored by dynamic contrast enhanced magnetic resonance imaging. Clin Cancer Res (2005) 1.17
In vivo molecular pharmacology and antitumor activity of the targeted Akt inhibitor PX-316. Oncol Res (2004) 1.14
Specific inhibition of the Akt1 pleckstrin homology domain by D-3-deoxy-phosphatidyl-myo-inositol analogues. Mol Cancer Ther (2003) 1.14
Discovery of a novel class of AKT pleckstrin homology domain inhibitors. Mol Cancer Ther (2008) 1.09
Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther (2010) 1.08
Hypoxia triggers hedgehog-mediated tumor-stromal interactions in pancreatic cancer. Cancer Res (2013) 1.08
In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT. Cancer Res (2009) 1.08
Mammalian target of rapamycin activator RHEB is frequently overexpressed in human carcinomas and is critical and sufficient for skin epithelial carcinogenesis. Cancer Res (2010) 1.08
Control of mTORC1 signaling by the Opitz syndrome protein MID1. Proc Natl Acad Sci U S A (2011) 1.05
CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy. Mol Cancer Ther (2012) 1.05
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. Bioorg Med Chem (2009) 1.04
The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling. Cancer Chemother Pharmacol (2006) 1.03
HIF-1alpha and cancer therapy. Recent Results Cancer Res (2010) 1.02
Hypoxia-induced assembly of prolyl hydroxylase PHD3 into complexes: implications for its activity and susceptibility for degradation by the E3 ligase Siah2. Biochem J (2007) 1.01
Hypoxia inducible factor as a cancer drug target. Curr Cancer Drug Targets (2003) 1.01
The role of Dbf4/Drf1-dependent kinase Cdc7 in DNA-damage checkpoint control. Mol Cell (2008) 1.01
Treatment with HIF-1alpha antagonist PX-478 inhibits progression and spread of orthotopic human small cell lung cancer and lung adenocarcinoma in mice. J Thorac Oncol (2010) 1.00
Identification of thioredoxin-interacting protein 1 as a hypoxia-inducible factor 1alpha-induced gene in pancreatic cancer. Pancreas (2008) 0.99
Metabolite changes in HT-29 xenograft tumors following HIF-1alpha inhibition with PX-478 as studied by MR spectroscopy in vivo and ex vivo. NMR Biomed (2005) 0.97
Clonidine for the treatment of supine hypertension and pressure natriuresis in autonomic failure. Hypertension (2006) 0.97
A randomized phase II study of PX-12, an inhibitor of thioredoxin in patients with advanced cancer of the pancreas following progression after a gemcitabine-containing combination. Cancer Chemother Pharmacol (2010) 0.96
Recombinase-mediated cassette exchange to rapidly and efficiently generate mice with human cardiac sodium channels. Genesis (2006) 0.93
The antitumor thioredoxin-1 inhibitor PX-12 (1-methylpropyl 2-imidazolyl disulfide) decreases thioredoxin-1 and VEGF levels in cancer patient plasma. J Lab Clin Med (2006) 0.93
Vascular endothelial growth factor receptor-1 and receptor-2 initiate a phosphatidylinositide 3-kinase-dependent clonogenic response in acute myeloid leukemia cells. Exp Hematol (2004) 0.91
Natural product based inhibitors of the thioredoxin-thioredoxin reductase system. Org Biomol Chem (2004) 0.91
The hypoxic inducible stress response as a target for cancer drug discovery. Semin Oncol (2006) 0.91
Antitumor agent PX-12 inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase in spermidine/spermine acetyl transferase. Cancer Chemother Pharmacol (2010) 0.91
In Vivo Therapeutic Silencing of Hypoxia-Inducible Factor 1 Alpha (HIF-1α) Using Single-Walled Carbon Nanotubes Noncovalently Coated with siRNA. Nano Res (2009) 0.90
The FRB domain of mTOR: NMR solution structure and inhibitor design. Biochemistry (2006) 0.90
HAF : the new player in oxygen-independent HIF-1alpha degradation. Cell Cycle (2009) 0.90
Protein kinase CK2 modulates IL-6 expression in inflammatory breast cancer. Biochem Biophys Res Commun (2011) 0.90
IL-24 is expressed during wound repair and inhibits TGFalpha-induced migration and proliferation of keratinocytes. Exp Dermatol (2010) 0.90
Cyclodextrin-derived diorganyl tellurides as glutathione peroxidase mimics and inhibitors of thioredoxin reductase and cancer cell growth. J Med Chem (2004) 0.90
IkappaBalpha kinase inhibitor IKI-1 conferred tumor necrosis factor alpha sensitivity to pancreatic cancer cells and a xenograft tumor model. Cancer Res (2008) 0.88
Effective inhibition of melanoma by BI-69A11 is mediated by dual targeting of the AKT and NF-κB pathways. Pigment Cell Melanoma Res (2011) 0.87
Laparoscopic accessory splenectomy: the value of perioperative localization studies. Surg Endosc (2009) 0.87
Inhibiting the hypoxia response for cancer therapy: the new kid on the block. Clin Cancer Res (2009) 0.87
Peroxisome proliferator-activated receptor gamma agonist pioglitazone prevents the hyperglycemia caused by phosphatidylinositol 3-kinase pathway inhibition by PX-866 without affecting antitumor activity. Mol Cancer Ther (2009) 0.86
HIF-1-dependent stromal adaptation to ischemia mediates in vivo tumor radiation resistance. Mol Cancer Res (2011) 0.86
Development of sulfonamide AKT PH domain inhibitors. Bioorg Med Chem (2011) 0.85
Synthesis of (+/-)-thiohalenaquinone by iterative metalations of thiophene. Org Lett (2007) 0.85
A phase I trial of PX-12, a small-molecule inhibitor of thioredoxin-1, administered as a 72-hour infusion every 21 days in patients with advanced cancers refractory to standard therapy. Invest New Drugs (2011) 0.84
Identification of novel synergistic targets for rational drug combinations with PI3 kinase inhibitors using siRNA synthetic lethality screening against GBM. Neuro Oncol (2011) 0.84
The antitumor agent imexon activates antioxidant gene expression: evidence for an oxidative stress response. Clin Cancer Res (2007) 0.84