- Interleukin-3-induced phosphorylation of BAD through the protein kinase Akt
L del Peso
Department of Pathology and Comprehensive Cancer Center, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Science 278:687-9. 1997
..Thus, the proapoptotic function of BAD is regulated by the PI 3-kinase-Akt pathway...
- Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation
Developmental Therapeutics Department, Medicine Branch, Division of Clinical Sciences, National Cancer Institute, Bethesda, MD 20889, USA
Cancer Res 61:3986-97. 2001
- Exploring the specificity of the PI3K family inhibitor LY294002
Severine I Gharbi
Ludwig Institute for Cancer Research, Proteomics Unit, Cruciform Building, Gower Street, London WCE1 6BT, UK
Biochem J 404:15-21. 2007
..The present study reveals that LY294002 not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family...
- G1 cell cycle progression and the expression of G1 cyclins are regulated by PI3K/AKT/mTOR/p70S6K1 signaling in human ovarian cancer cells
1820 MBR Cancer Center and Dept of Microbiology, Immunology and Cell Biology, West Virginia University, Morgantown, WV 26506 9300, USA
Am J Physiol Cell Physiol 287:C281-91. 2004
..These results indicate that PI3K mediates G(1) progression and cyclin expression through activation of an AKT/mTOR/p70S6K1 signaling pathway in the ovarian cancer cells...
- Lipopolysaccharide-mediated reactive oxygen species and signal transduction in the regulation of interleukin-1 gene expression
Hsien Yeh Hsu
Faculty of Medical Technology, Institute of Biotechnology in Medicine, National Yang Ming University, 112 Taipei, Taiwan
J Biol Chem 277:22131-9. 2002
- A novel DNA-dependent protein kinase inhibitor, NU7026, potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia
School of Cell and Molecular Biosciences, University of Newcastle upon Tyne Medical School, Newcastle upon Tyne NE2 4HH, United Kingdom
Blood 103:4659-65. 2004
..A concentration-dependent increase in etoposide-induced DSB levels was increased by NU7026. The mechanism of NU7026 potentiation of topo II poisons involves inhibition of NHEJ and a G2/M checkpoint arrest...
- The novel proangiogenic effect of hydrogen sulfide is dependent on Akt phosphorylation
Wen Jie Cai
Department of Physiology and Pathophysiology, Fudan University Shanghai Medical College, Shanghai, China
Cardiovasc Res 76:29-40. 2007
..Hydrogen sulfide (H(2)S) has been reported to be a gasotransmitter which regulates cardiovascular homeostasis. The present study aims to examine the hypothesis that hydrogen sulfide is able to promote angiogenesis...
- Constitutive and inducible Akt activity promotes resistance to chemotherapy, trastuzumab, or tamoxifen in breast cancer cells
Amy S Clark
Cancer Therapeutics Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20889, USA
Mol Cancer Ther 1:707-17. 2002
- Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase
Montreal Centre for Experimental Therapeutics in Cancer Lady Davis Institute for Medical Research, Sir Mortimer B Davis Jewish General Hospital, McGill University, Montreal, Quebec, Canada
J Pharmacol Exp Ther 321:848-55. 2007
- Adiponectin stimulates angiogenesis by promoting cross-talk between AMP-activated protein kinase and Akt signaling in endothelial cells
Molecular Cardiology Whitaker Cardiovascular Institute, Boston University School of Medicine, Boston, Massachusetts 02118, USA
J Biol Chem 279:1304-9. 2004
..These data indicate that adiponectin can function to stimulate the new blood vessel growth by promoting cross-talk between AMP-activated protein kinase and Akt signaling within endothelial cells...
- Loss in oxidative stress tolerance with aging linked to reduced extracellular signal-regulated kinase and Akt kinase activities
Laboratory of Cellular and Molecular Biology, National Institute on Aging IRP, Baltimore, Maryland 21224, USA
FASEB J 16:114-6. 2002
..Strategies aimed at boosting these host responses to acute oxidant injury could have significant anti-aging benefits...
- Mutant PIK3CA promotes cell growth and invasion of human cancer cells
The Sidney Kimmel Comprehensive Cancer Center and The Howard Hughes Medical Institute, The Johns Hopkins University Medical Institutions, Baltimore, MD 21231, USA
Cancer Cell 7:561-73. 2005
..Treatment with the PI3K inhibitor LY294002 abrogated PIK3CA signaling and preferentially inhibited growth of PIK3CA mutant cells. These data have important implications for therapy of cancers harboring PIK3CA alterations...
- Migrating glioma cells activate the PI3-K pathway and display decreased susceptibility to apoptosis
Anna M Joy
The Translational Genomics Research Institute, 400 North 5th Street, Suite 1600, Phoenix, AZ 85004, USA
J Cell Sci 116:4409-17. 2003
..In addition, evidence indicates that treatment with migration inhibitors, while not affecting apoptosis-induction in migration-restricted cells, can sensitize migrating glioma cells to cytotoxic agents...
- Radiation sensitization of human cancer cells in vivo by inhibiting the activity of PI3K using LY294002
Anjali K Gupta
Department of Radiation Oncology, University of Pennsylvania, Philadelphia, PA 19104, USA
Int J Radiat Oncol Biol Phys 56:846-53. 2003
..Inhibition of PI3K by LY294002 can synergistically enhance radiation efficacy. This acts as a proof of principle that inhibition of the Ras to PI3K pathway could be useful clinically...
- Salmonella transforms follicle-associated epithelial cells into M cells to promote intestinal invasion
The Roslin Institute and Royal School of Veterinary Studies, University of Edinburgh, Edinburgh EH25 9RG, UK
Cell Host Microbe 12:645-56. 2012
..Thus, via the activity of a single secreted effector, S. Typhimurium transforms primed epithelial cells into M cells to promote host colonization and invasion...
- Activation of Akt/GSK-3beta signaling pathway is involved in intermedin(1-53) protection against myocardial apoptosis induced by ischemia/reperfusion
Jun Qiu Song
Department of Physiology and Pathophysiology, Peking University Health Science Center, Beijing, China
Apoptosis 14:1299-307. 2009
..In conclusion, IMD(1-53) exerts cardioprotective effect against myocardial I/R injury through the activation of the Akt/GSK-3beta signaling pathway to inhibit mitochondria-mediated myocardial apoptosis...
- ER-alpha36, a variant of ER-alpha, promotes tamoxifen agonist action in endometrial cancer cells via the MAPK/ERK and PI3K/Akt pathways
Sheng Li Lin
State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences and Graduate School, Chinese Academy of Sciences, Beijing, China
PLoS ONE 5:e9013. 2010
..ER-alpha36 lacks intrinsic transcription activity and mainly mediates nongenomic estrogen signaling. Here, we studied the role of nongenomic estrogen signaling pathways mediated by ER-alpha36 in tamoxifen resistance and agonist action...
- Phase I pharmacokinetic and pharmacodynamic study of the pan-PI3K/mTORC vascular targeted pro-drug SF1126 in patients with advanced solid tumours and B-cell malignancies
University of Arizona Cancer Center, Tucson, AZ, USA
Eur J Cancer 48:3319-27. 2012
..A first-in-human study evaluated safety, dose limiting toxicities (DLT), maximum tolerated dose (MTD), pharmacokinetics (PK), pharmacodynamics (PD) and efficacy of SF1126, in patients with advanced solid and B-cell malignancies...
- Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination
Northern Institute for Cancer Research, School of Medical Sciences, Newcastle University, Paul O Gorman Building, Framlington Place, NE2 4HH Newcastle upon Tyne, UK
Cancer Chemother Pharmacol 69:155-64. 2012
..One promising target is DNA-PK, a pivotal kinase in double-strand break repair. The purpose of this study was to further characterise the activity of the DNA-PK inhibitor NU7441, giving some new insights into the biology of DNA-PK...
- Involvement of PI3K/Akt signaling in PTTH-stimulated ecdysteroidogenesis by prothoracic glands of the silkworm, Bombyx mori
Shi Hong Gu
Department of Zoology, National Museum of Natural Science, 1 Kuan Chien Road, Taichung 404, Taiwan, ROC
Insect Biochem Mol Biol 41:197-202. 2011
..mori prothoracic glands between insulin and PTTH signaling, which may play a critical role in precisely regulated ecdysteroidogenesis during development...
- Application of response surface methodology to optimise ultrasonic-assisted extraction of four chromones in Radix Saposhnikoviae
College of Chinese Medicinal Materials, Jilin Agricultural University, Changchun, People s Republic of China
Phytochem Anal 22:313-21. 2011
..b>Chromones are considered as one of the effective components...
- Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441
Northern Institute for Cancer Research, Medical School, University of Newcastle upon Tyne, Newcastle upon Tyne, United Kingdom
Cancer Res 66:5354-62. 2006
..In conclusion, NU7441 shows sufficient proof of principle through in vitro and in vivo chemosensitization and radiosensitization to justify further development of DNA-PK inhibitors for clinical use...
- t-DARPP regulates phosphatidylinositol-3-kinase-dependent cell growth in breast cancer
Department of Surgery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
Mol Cancer 9:240. 2010
..In this study, we evaluated expression of t-DARPP in human primary breast tumors, and investigated the role of t-DARPP in regulating growth and proliferation in breast cancer cells...
- LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors
Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117597, Singapore
Cancer Res 69:1941-50. 2009
..Our findings could have implications for the use of LY30 and similar compounds for enhancing the apoptotic sensitivity of neuroblastoma cells that often become refractory to chemotherapy...
- Neuroprotection by brain-derived neurotrophic factor is mediated by extracellular signal-regulated kinase and phosphatidylinositol 3-kinase
Toxicology Program, Department of Environmental Health, the Graduate Program in Neurobiology and Behavior, The Graduate Program in Molecular and Cell Biology, University of Washington, Seattle, Washington 98195 7234, USA
J Biol Chem 274:22569-80. 1999
..Furthermore, the relative contribution of the ERK and PI 3-kinase pathways to neuronal survival may depend on the type of cellular injury...
- Critical role for PI 3-kinase in the control of erythropoietin-induced erythroid progenitor proliferation
Departement d Hematologie, Institut Cochin, Institut National de la Sante et de la Recherche Medicale U567, Centre National de la Recherche Scientifique, UMR 8104, Universite Rene Descartes, Paris, France
Blood 101:3436-43. 2003
- Effect of estradiol on estrogen receptor-alpha gene expression and activity can be modulated by the ErbB2/PI 3-K/Akt pathway
Gerald E Stoica
Department of Oncology, Lombardi Cancer Center, Georgetown University, Washington DC 20057, USA
Oncogene 22:7998-8011. 2003
..This results in the activation of PI 3-K and Akt. Akt, in turn, may interact with nuclear ER-alpha, altering its expression and activity...
- FOXO3a is activated in response to hypoxic stress and inhibits HIF1-induced apoptosis via regulation of CITED2
Walbert J Bakker
Campbell Family Institute for Breast Cancer Research, University Health Network, Ontario Cancer Institute and Princess Margaret Hospital, Toronto, ON M5G 2C1, Canada
Mol Cell 28:941-53. 2007
..Thus, by fine-tuning HIF1 activity, FOXO3a plays an important role in the survival response of normal and cancer cells in response to hypoxic stress...
- Role of phosphatidylinositol 3' kinase and a downstream pleckstrin homology domain-containing protein in controlling chemotaxis in dictyostelium
Section of Cell and Developmental Biology and Center for Molecular Genetics, University of California at San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA
J Cell Biol 153:795-810. 2001
..We suggest that PKB and PhdA lie downstream from PI3K and control different downstream effector pathways that are essential for proper chemotaxis...
- Cytosolic action of thyroid hormone leads to induction of hypoxia-inducible factor-1alpha and glycolytic genes
Lars C Moeller
The University of Chicago, MC3090, 5841 South Maryland Avenue, Chicago, IL 60637, USA
Mol Endocrinol 19:2955-63. 2005
- Cardioprotection induced by hydrogen sulfide preconditioning involves activation of ERK and PI3K/Akt pathways
Cardiovascular Biology Research Group, Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore
Pflugers Arch 455:607-16. 2008
..In conclusion, K(ATP)/PKC/ERK1/2 and PI3K/Akt pathways contributed to SP-induced cardioprotection...
- Role of phosphoinositide 3-kinase in activation of ras and mitogen-activated protein kinase by epidermal growth factor
Imperial Cancer Research Fund, London WC2A 3PX, United Kingdom
Mol Cell Biol 19:4279-88. 1999
- Substituted chromones as highly potent nontoxic inhibitors, specific for the breast cancer resistance protein
Equipe Labellisée Ligue 2011, Institut de Biologie et Chimie des Proteines, BMSSI UMR 5086, CNRS Université Lyon 1, Lyon, France
J Med Chem 55:966-70. 2012
A series of 13 disubstituted chromones was synthesized. Two types of substituents, on each side of the scaffold, contributed to both the potency of ABCG2 inhibition and the cytotoxicity...
- Intrathecal cannabilactone CB(2)R agonist, AM1710, controls pathological pain and restores basal cytokine levels
Jenny L Wilkerson
Department of Neurosciences, University of New Mexico, Albuquerque, NM 87131, USA
Pain 153:1091-106. 2012
..Cannabilactone CB(2)R agonists are emerging as anti-inflammatory agents with pain therapeutic implications...
- PKB/AKT and ERK regulation of caspase-mediated apoptosis by methylseleninic acid in LNCaP prostate cancer cells
The Hormel Institute, University of Minnesota, 801 16th Avenue NE, Austin, MN 55912, USA
Carcinogenesis 26:1374-81. 2005
..These findings support the differential involvement of these protein kinase pathways in regulating apoptosis induction by different forms of selenium...
- The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells
First Department of Pathology, Yamagata University School of Medicine, 2 2 2 Iida nishi, Yamagata 990 9585, Japan
Clin Cancer Res 8:1957-63. 2002
..We postulated that 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a PI3K inhibitor, should inactivate Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis in vitro and in vivo...
- Involvement of estrogen receptor-β in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation
Qun yi Li
The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
Acta Pharmacol Sin 32:433-40. 2011
- LY294002 and LY303511 sensitize tumor cells to drug-induced apoptosis via intracellular hydrogen peroxide production independent of the phosphoinositide 3-kinase-Akt pathway
Tze Wei Poh
Department of Physiology, National University Medical Institute, Faculty of Medicine, National University of Singapore, Singapore, Singapore
Cancer Res 65:6264-74. 2005
- Inhibition of the phosphatidylinositol 3-kinase/p70(S6)-kinase pathway induces B16 melanoma cell differentiation
INSERM U385, Faculte de Medecine, 06107 Nice, Cedex 02, France
J Biol Chem 271:31824-30. 1996
..Furthermore, we provide evidence which suggests that cAMP-induced melanogenesis and dendricity are, at least partially, mediated by the cAMP inhibition of the phosphatidylinositol 3-kinase/p70(S6)-kinase signaling pathway...
- Synthesis and function of 3-phosphorylated inositol lipids
Ludwig Institute for Cancer Research, Riding House Street, London W1W 7BS
Annu Rev Biochem 70:535-602. 2001
..This field is now moving toward a genetic dissection of 3-phosphoinositide action in a variety of model organisms. Such approaches will reveal the true role of the 3-phosphoinositides at the organismal level in health and disease...
- Chromones and coumarins from the dried fructus of Cnidium monnieri
Center for Natural Products Research, Chengdu Institute of Biology of the Chinese Academy of Sciences, P R China
Fitoterapia 82:767-71. 2011
Chemical investigations on the ethanolic extract of the dried fructus of Cnidium monnieri offered three chromones and eight coumarins...
- Long-term safety study of iguratimod in patients with rheumatoid arthritis
Institute of Rheumatology, Tokyo Women s Medical University, Tokyo 162 0054, Japan
Mod Rheumatol 17:10-6. 2007
..The rate was 46.9% at week 28 and 41.0% at week 52. To use iguratimod safely for a long time, patients should be observed closely for adverse reactions such as increased hepatic enzymes...
- Efficacy and safety of iguratimod compared with placebo and salazosulfapyridine in active rheumatoid arthritis: a controlled, multicenter, double-blind, parallel-group study
Institute of Rheumatology, Tokyo Women s Medical University, Tokyo 162 0054, Japan
Mod Rheumatol 17:1-9. 2007
..The study results suggest that iguratimod could become a new option for the treatment of rheumatoid arthritis...
- Luteolin inhibits lipopolysaccharide actions on human gingival fibroblasts
Laboratorio de Bioquímica de la División de Estudios de Posgrado de la Facultad de Odontología, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, 04510 Mexico, D F, Mexico
Eur J Pharmacol 541:95-105. 2006
..We concluded that luteolin interferes with LPS signaling pathways, reducing activation of several mitogen-activated protein kinase family members, and inhibits inflammatory mediator expression...
- Involvement of the phosphoinositide 3-kinase/protein kinase B signaling pathway in insulin/IGF-I-induced chondrogenesis of the mouse embryonal carcinoma-derived cell line ATDC5
Laboratory of Molecular and Cellular Biochemistry, Higashi-ku, 812-8582, Fukuoka, Japan
Int J Biochem Cell Biol 33:1094-103. 2001
..This is the first report that demonstrates the involvement of phosphoinositide signaling in the induction of chondrogenesis from undifferentiated cells...
- Suppression of pro-metastasis phenotypes expression in malignant pleural mesothelioma by the PI3K inhibitor LY294002 or the MEK inhibitor UO126
George W Cole
Section of Thoracic Oncology, Surgery Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anticancer Res 26:809-21. 2006
- Respiratory syncytial virus inhibits apoptosis and induces NF-kappa B activity through a phosphatidylinositol 3-kinase-dependent pathway
Karl W Thomas
Department of Internal Medicine, University of Iowa College of Medicine and Veterans Administration Medical Center, Iowa City, Iowa 52242, USA
J Biol Chem 277:492-501. 2002
..Blockade of PI 3-K activation resulted in rapid, premature apoptosis and inhibition of RSV-stimulated NF-kappaB-dependent gene transcription...
- Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity
Atmaram D Khanolkar
Center for Drug Discovery, Northeastern University, 116 Mugar Hall, 360 Huntington Avenue, Boston, Massachusetts 02115 5000, USA
J Med Chem 50:6493-500. 2007
..In vitro testing revealed that the novel compounds are CB2 agonists, while in vivo testing of cannabilactones 4b and 5 found them to possess potent peripheral analgesic activity...
- TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells
Division of Hematology and Internal Medicine, Mayo Clinic, 200 First Street SW, Rochester, MN 55905, USA
Am J Hematol 85:675-86. 2010
..Our results provide the rationale for clinical evaluation of TG101209 alone or in combination with PI3K/Akt inhibitors in MM...
- LY303511 amplifies TRAIL-induced apoptosis in tumor cells by enhancing DR5 oligomerization, DISC assembly, and mitochondrial permeabilization
T W Poh
Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, 2 Medical Drive, Singapore 117597, Singapore
Cell Death Differ 14:1813-25. 2007
..These data provide a novel mechanism of action of this small molecule with the potential for use in TRAIL-resistant tumors...
- Selective activation of cannabinoid CB2 receptors suppresses neuropathic nociception induced by treatment with the chemotherapeutic agent paclitaxel in rats
Elizabeth J Rahn
Neuroscience and Behavior Program, Department of Psychology, University of Georgia, Athens, GA 30602 3013, USA
J Pharmacol Exp Ther 327:584-91. 2008
..Our data suggest that cannabinoid CB(2) receptors may be important therapeutic targets for the treatment of chemotherapy-evoked neuropathy...
- The phosphatidylinositol 3-kinase/Akt pathway enhances Smad3-stimulated mesangial cell collagen I expression in response to transforming growth factor-beta1
Constance E Runyan
Department of Pediatrics, Northwestern University, Chicago, Illinois 60611, USA
J Biol Chem 279:2632-9. 2004
..This cross-talk between the Smad and PI3K pathways likely contributes to TGF-beta1 induction of glomerular scarring...
- Phosphatidylinositol 3-kinase/AKT-mediated activation of estrogen receptor alpha: a new model for anti-estrogen resistance
R A Campbell
Department of Surgery, Indiana University School of Medicine, Indianapolis 46202, USA
J Biol Chem 276:9817-24. 2001
..Taken together, these results define a molecular link between activation of the PI 3-kinase/AKT survival pathways, hormone-independent activation of ERalpha, and inhibition of tamoxifen-induced apoptotic regression...
- The PTEN tumor suppressor inhibits telomerase activity in endometrial cancer cells by decreasing hTERT mRNA levels
Department of Obstetrics and Gynecology, Division of Gynecologic Oncology, University of North Carolina at Chapel Hill, CB 7570, Chapel Hill, NC 27599, USA
Gynecol Oncol 101:305-10. 2006
..Given that PTEN is often absent and telomerase is overexpressed by endometrial cancers, we hypothesize that PTEN signaling is important in telomerase regulation...
- Apoptosis of metastatic prostate cancer cells by a combination of cyclin-dependent kinase and AKT inhibitors
Molecular Oncology Program, Moffitt Cancer Center, 12902 Magnolia Drive, Tampa, FL 33612, USA
Int J Biochem Cell Biol 41:595-602. 2009
..Collectively, our data show apoptosis of prostate cancer cells by a drug combination and identify Bax activation as a basis of cooperation...
- Comprehensive analysis of oncogenic effects of PIK3CA mutations in human mammary epithelial cells
Breast Cancer Program, Karmanos Cancer Institute, Detroit, MI 48201, USA
Breast Cancer Res Treat 112:217-27. 2008
- Toll-like receptor 4 mediates lipopolysaccharide-induced collagen secretion by phosphoinositide3-kinase-Akt pathway in fibroblasts during acute lung injury
Department of Anesthesiology, Ninth People s Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China
J Recept Signal Transduct Res 29:119-25. 2009
..Therefore, we infer that besides pulmonary macrophage, lung fibroblasts are also important target cells directly influenced by LPS, which may play an important role in ALI and pulmonary interstitial fibrosis...
- Inhibition of phosphatidylinositol-3-kinase and mitogen-activated protein kinase kinase 1/2 prevents melanoma development and promotes melanoma regression in the transgenic TPRas mouse model
Division of Radiation and Cancer Biology, 269 Campus Drive, CCSR S 1230, Stanford 94305, CA, USA
Mol Cancer Ther 5:3071-7. 2006
- Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026
B P Nutley
Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton SM2 5NG, UK
Br J Cancer 93:1011-8. 2005
..The pharmacokinetic simulations performed predict that NU7026 will have to be administered four times per day at 100 mg kg(-1) i.p. in order to obtain the drug exposure required for radiosensitisation...
- Inhibition of phosphatidylinositol 3'-kinase increases efficacy of paclitaxel in in vitro and in vivo ovarian cancer models
Center for Reproductive Sciences, University of California, San Francisco, San Francisco, California 94143 0556, USA
Cancer Res 62:1087-92. 2002
..Our data suggest that a combination of a PI3k inhibitor and conventional chemotherapy may provide an effective approach to inhibiting tumor growth and ascites production in ovarian cancer with acceptable side effects...
- PI-3K/Akt and NF-kappaB/IkappaBalpha pathways are activated in Jurkat T cells in response to TRAIL treatment
Dipartimento di Morfologia Umana Normale, Universita di Trieste, Via Manzoni, Trieste, Italy
J Cell Physiol 202:900-11. 2005
- Cafestol, a coffee-specific diterpene, induces apoptosis in renal carcinoma Caki cells through down-regulation of anti-apoptotic proteins and Akt phosphorylation
Min Jung Choi
Department of Immunology, School of Medicine, Keimyung University, 2800 Dalgubeoldaero, Dalseo Gu, Daegu 704 701, Republic of Korea
Chem Biol Interact 190:102-8. 2011
..Taken together, our results show the activity of cafestol to modulate multiple components in apoptotic response of human renal Caki cells and a potential as a therapeutic agent for preventing cancers such as renal carcinoma...
- Somatic mutation and gain of copy number of PIK3CA in human breast cancer
Department of Otolaryngology Head and Neck Surgery, Head and Neck Cancer Research Division, Johns Hopkins University School of Medicine, Baltimore, MD, USA
Breast Cancer Res 7:R609-16. 2005
..Even though PIK3CA amplification and somatic mutation have been reported previously in various kinds of human cancers, the genetic change in PIK3CA in human breast cancer has not been clearly identified...
- Inhibition of phosphatidylinositol 3-kinase dephosphorylates BAD and promotes apoptosis in myeloid leukemias
Section of Molecular Hematology and Therapy, Department of Blood and Marrow Transplantation, MD Anderson Cancer Center, The University of Texas, Houston, TX 77030, USA
Leukemia 18:267-75. 2004
..In conclusion, the data suggest that the inhibition of the PI3K/AKT signaling pathway restores apoptosis in AML and may be explored as a novel target for molecular therapeutics in AML...
- Nanoparticle-mediated targeting of phosphatidylinositol-3-kinase signaling inhibits angiogenesis
Harvard MIT Division of Health Sciences and Technology, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
Angiogenesis 12:325-38. 2009
..The objective of this study was to engineer a PI3K inhibitor-loaded biodegradable nanoparticle and to evaluate its efficacy...
- Neurite growth promotion by nerve growth factor and insulin-like growth factor-1 in cultured adult sensory neurons: role of phosphoinositide 3-kinase and mitogen activated protein kinase
Division of Basic Medical Sciences, Memorial University of Newfoundland, St. John's, Newfoundland, Canada
J Neurosci Res 63:486-99. 2001
..Activation of PI 3-kinase and SNT by both NGF and IGF-1 correlated with their effects on neurite growth. These results support the hypothesis that the PI 3-kinase pathway plays an important role in neuritogenesis...
- ErbB2-overexpressing human mammary carcinoma cells display an increased requirement for the phosphatidylinositol 3-kinase signaling pathway in anchorage-independent growth
Department of Microbiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA
Oncogene 20:7551-62. 2001
- Cisplatin and PI3kinase inhibition decrease invasion and migration of human ovarian carcinoma cells and regulate matrix-metalloproteinase expression
Amer K Karam
Division of Gynecologic Oncology, Department of Obstetrics and Gynecology, The David Geffen School of Medicine at UCLA, Los Angeles, California 90095, USA
Cytoskeleton (Hoboken) 67:535-44. 2010
..Our data suggests that inhibition of ovarian cancer cell motility is mediated via down-regulation of activated MMP2, TIMP1 and TIMP2 expression under these treatment conditions...
- Activation of phosphatidylinositol 3-kinase is important for erythropoietin-induced erythropoiesis from CD34(+) hematopoietic progenitor cells
June Helen Myklebust
Department of Immunology, Institute for Cancer Research, The Norwegian Radium Hospital, Oslo, Norway
Exp Hematol 30:990-1000. 2002
..The aim of this was to examine the relative involvement of PI3K in the development of glycophorin A (GPA)(+) erythroid cells from normal hematopoietic progenitor cells...
- 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK)
Jonathan J Hollick
Northern Institute for Cancer Research, School of Natural Sciences Chemistry, Bedson Building, University of Newcastle, Newcastle upon Tyne NE1 7RU, UK
Bioorg Med Chem Lett 13:3083-6. 2003
..2-0.4 microM range...
- Phosphorylation and regulation of Raf by Akt (protein kinase B)
Institute of Medical Virology, University of Zurich, Gloriastrasse 30 32, CH 8028 Zurich, Switzerland
Science 286:1741-4. 1999
..These observations provide a molecular basis for cross talk between two signaling pathways at the level of Raf and Akt...
- Synthesis, crystal structure and DNA-binding studies of the Ln(III) complex with 6-hydroxychromone-3-carbaldehyde benzoyl hydrazone
Bao Dui Wang
College of Chemistry and Chemical Engineering and State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China
J Inorg Biochem 101:1492-504. 2007
..The intrinsic binding constants of complexes 1 and 2, and L were (7.62+/-0.56)x10(6), (3.70+/-0.47)x10(6) and (2.41+/-0.46)x10(6)M(-1), respectively...
- 1alpha,25-dihydroxyvitamin D(3)-induced myeloid cell differentiation is regulated by a vitamin D receptor-phosphatidylinositol 3-kinase signaling complex
Department of Medicine, The University of British Columbia, Faculties of Medicine and Science, The Research Institute of the Vancouver Hospital and Health Sciences Center, Vancouver, British Columbia, Canada
J Exp Med 190:1583-94. 1999
..These findings suggest that PI 3-kinase selectively regulates D(3)-induced monocyte differentiation, independent of any effects on p21...
- Phosphatidylinositol-3-kinase as a therapeutic target in melanoma
Saadia A Aziz
Department of Pathology, Yale University School of Medicine, New Haven, Connecticut, USA
Clin Cancer Res 15:3029-36. 2009
..We assessed expression of PI3K in melanomas and nevi, and studied associations between PI3K pathway members and in vitro response to a PI3K inhibitor, LY294002...
- Selective regulation of interleukin-10 production via Janus kinase pathway in murine conventional dendritic cells
Division of Immunobiology, Institute for Genetic Medicine, Hokkaido University, Kita ku, Sapporo, Japan
Cell Immunol 258:9-17. 2009
..LY294002, a specific inhibitor of PI3K, markedly inhibited the DC production of IL-10. Thus, JAK-PI3K axis appeared to be responsible for the IL-10 production by DCs...
- Role of the phosphatidylinositol 3'-kinase-Akt signal pathway in the proliferation of human pancreatic ductal carcinoma cell lines
Division of Organ Pathology, Department of Microbiology and Pathology, Graduate School of Medicine, Tottori University, Yonago, Japan
Pancreas 28:353-8. 2004
- Activation of telomerase by ionizing radiation: differential response to the inhibition of DNA double-strand break repair by abrogation of poly (ADP-ribosyl)ation, by LY294002, or by Wortmannin
Laboratory of Radiation Biology, Department of Radiation Oncology, University of Heidelberg, Heidelberg, Germany
Int J Radiat Oncol Biol Phys 69:887-94. 2007
..In addition, the role of trans-dominant inhibition of poly(ADP-ribosyl)ation, which strongly reduces DSB rejoining, was assessed in comparison with 3-aminobenzamide...
- p27Kip1 is required for PTEN-induced G1 growth arrest
A R Gottschalk
Department of Radiation Oncology, University of California at San Francisco, 94143, USA
Cancer Res 61:2105-11. 2001
..These results implicate p27Kip1 as a critical mediator of PTEN-induced G1 arrest...
- HB-EGF-induced VEGF production and eNOS activation depend on both PI3 kinase and MAP kinase in HaCaT cells
Department of Dermatology, Kagawa University, Japan
J Dermatol Sci 55:170-8. 2009
- Therapeutic targeting of multiple signaling pathways in malignant pleural mesothelioma
Lowe Center for Thoracic Oncology, Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
Oncology 68:500-10. 2005
..Furthermore, combinations of growth factor and signal transduction inhibitors may be needed to inhibit the growth of the majority of MPM cell lines, and therefore patients with MPM...
- Pressurized liquid extraction followed by LC-ESI/MS for analysis of four chromones in Radix Saposhnikoviae
College of Chinese Medicinal Materials, Jilin Agricultural University, Changchun, P R China
J Sep Sci 33:2881-7. 2010
An efficient pressurized liquid extraction (PLE) technique was employed in extracting chromones from the roots of Saposhnikovia divaricata (Radix Saposhnikoviae). Chromones were quantified and analyzed by LC-ESI/MS...
- Two chromones from Peperomia vulcanica
James A Mbah
Department of Chemistry, Faculty of Science, University of Dschang, Box 67 Dschang, Cameroon
Phytochemistry 60:799-801. 2002
TWO CHROMONES: 5-hydroxy-2-(14'-(E)-nonadecenyl) chromone (1) and 5-hydroxy-2-[12'-(3",4"-methylenedioxyphenyl)dodecanyl] chromone (2), together with six known compounds have been isolated from Peperomia vulcanica Baker & C...
- Xanthones and oxepino[2, 3-b]chromones from three endophytic fungi
Department Chemie, Universität Paderborn, Warburger Strasse 100, 33098 Paderborn, Germany
Chemistry 15:12121-32. 2009
..Preliminary studies indicated that 1, 2, and enone 7 showed antibacterial, fungicidal, and algicidal properties...
- Phosphatidylinositol 3-kinase inhibition by LY294002 radiosensitizes human cervical cancer cell lines
Christopher M Lee
Department of Radiation Oncology, University of Utah School of Medicine and Huntsman Cancer Hospital, Salt Lake City, Utah, USA
Clin Cancer Res 12:250-6. 2006
..We evaluated the radiosensitizing effect of PI3K inhibition by LY294002 on clonogenic survival, growth characteristics, and gene expression in cervical cancer cell lines (HeLa and CaSki)...
- Synthesis of 3-aminomethyl-2-aryl- 8-bromo-6-chlorochromones
Erik A A Wallen
Department of Chemistry, Medicinal Chemistry, Goteborg University, SE 412 96 Goteborg, Sweden
Org Lett 9:389-91. 2007
..The Cbz-protected 3-aminomethyl-2-aryl-8-bromo-6-chlorochromones can, e.g., be used in the synthesis of chromone-based beta-turn peptidomimetics...
- Synthesis of a novel series of diphenolic chromone derivatives as inhibitors of NO production in LPS-activated RAW264.7 macrophages
Guo Biao Liu
Key Lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093, China
Bioorg Med Chem 18:2864-71. 2010
..Furthermore, a computational analysis of physicochemical parameters revealed that the most of the compounds possessed drug-like properties...
- Synthesis of 2-alkyl-substituted chromone derivatives using microwave irradiation
Department of Chemistry, Medicinal Chemistry, University of Gothenburg, SE 41296 Goteborg, Sweden
J Org Chem 74:2755-9. 2009
..The 4-chromanones could be further converted into highly functionalized 2,3,6,8-tetrasubstituted chromones in which a 3-substituent (acetate, amine, or bromine) was introduced via straightforward chemical transformations...
- Phosphatidylinositol 3-kinase in cumulus cells is responsible for both suppression of spontaneous maturation and induction of gonadotropin-stimulated maturation of porcine oocytes
Laboratory of Animal Reproduction, Graduate School of Biosphere Science, Hiroshima University, Higashi Hiroshima, Hiroshima, 739 8528, Japan
J Endocrinol 179:25-34. 2003
..Judging from these results, it is estimated that PI 3-kinase in cumulus cells is required for both the suppression of spontaneous meiotic resumption and the induction of gonadotropin-stimulated meiotic resumption...
- P2X7 nucleotide receptor is coupled to GSK-3 inhibition and neuroprotection in cerebellar granule neurons
Departamento de Bioquimica y Biologia Molecular IV, Facultad de Veterinaria, Universidad Complutense de Madrid, Avda Puerta de Hierro s n, Madrid 28040, Spain
Neurotox Res 15:193-204. 2009
..These results reveal that P2X(7) receptor activation could provide a relevant survival route alternative to classical neurotrophic factors...
- Preparative separation of chromones in plant extract of Saposhnikovia divaricata by high-performance counter-current chromatography
The Central Laboratory, Changchun Normal University, China, Changchun, PR China
J Sep Sci 34:520-6. 2011
Four chromones, prim-O-glucosylcimifugin, 4'-O-β-D-glucosyl-5-O-methylvisamminol, cimifugin and sec-O-glucosylhamaudol, were isolated and purified from Saposhnikovia divaricata for the first time by high-performance counter-current ..
- Enhancement of the dissolution rate and gastrointestinal absorption of pranlukast as a model poorly water-soluble drug by grinding with gelatin
Department of Pharmaceutics, Hokkaido Pharmaceutical University, 7 1 Katsuraoka cho, Otaru city 047 0264, Japan
Int J Pharm 347:71-8. 2008
..Grinding a poorly water-soluble drug with gelatin is a useful method of enhancing its gastrointestinal absorption...
- Subinhibitory concentrations of farrerol reduce α-toxin expression in Staphylococcus aureus
Institute of Zoonoses, College of Animal Sciences and Veterinary Medicine, Jilin University, Changchun, China
FEMS Microbiol Lett 315:129-33. 2011
..aureus. The results show that farrerol significantly decreased, in a dose-dependent manner, the production of α-toxin by both methicillin-sensitive S. aureus and methicillin-resistant S. aureus...
- The effect of an oral leukotriene antagonist, ONO-1078, on allergen-induced immediate bronchoconstriction in asthmatic subjects
First Department of Internal Medicine, Tohoku University School of Medicine, Sendai, Japan
J Allergy Clin Immunol 92:507-12. 1993
..0 10 minutes after the exposure. CONCLUSIONS: Therefore, we conclude that cysteinyl leukotrienes primarily mediate a later part of immediate airway obstruction after allergen exposure...
- Overexpression of interferon-gamma-inducible GTPase inhibits coxsackievirus B3-induced apoptosis through the activation of the phosphatidylinositol 3-kinase/Akt pathway and inhibition of viral replication
Huifang M Zhang
Department of Pathology and Laboratory Medicine, University of British Columbia MRL The iCAPTUR4E Centre, St Paul s Hospital, Vancouver, British Columbia V6Z 1Y6, Canada
J Biol Chem 278:33011-9. 2003
- Synthesis of 2,3,6,8-tetrasubstituted chromone scaffolds
Department of Chemistry, Medicinal Chemistry, Goteborg University, SE 412 96 Goteborg, Sweden
J Org Chem 71:6863-71. 2006
..The chromones are also interesting structural scaffolds, and they have for example been designed to be used as mimetics of ..
- New sesquiterpenes from Ferula ferulaeoides (Steud.) Korovin. VI. Isolation and identification of three new dihydrofuro[2,3-b]chromones
Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan
Chem Pharm Bull (Tokyo) 50:675-7. 2002
..The structures were established by comprehensive spectral analysis. The biosynthetic pathway leading to these 2-prenyl-dihydrofurochromone-type sesquiterpenoids is proposed based on their structures...
- In vivo pharmacologic profile of ONO-1078: a potent, selective and orally active peptide leukotriene (LT) antagonist
Minase Research Institute, Ono Pharmaceutical Co, Ltd, Osaka, Japan
Jpn J Pharmacol 60:217-25. 1992
- Pharmacological characterization of AM1710, a putative cannabinoid CB2 agonist from the cannabilactone class: antinociception without central nervous system side-effects
Elizabeth J Rahn
Program in Neuroscience, Biomedical and Health Sciences Institute, University of Georgia, Athens, GA, United States
Pharmacol Biochem Behav 98:493-502. 2011
..The observed pattern of pharmacological specificity produced by AM1710 is consistent with limited blood brain barrier penetration of this compound and absence of CNS side-effects...
- Antitubercular chromones and flavonoids from Pisonia aculeata
Ming Chun Wu
Graduate Institute of Natural Products, Department of Biomedical Laboratory Science and Biotechnology, School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan 807, Republic of China
J Nat Prod 74:976-82. 2011
Three new chromones, pisonins A (1), B (2), and D (4), two new flavonoids, pisonivanone [(2S)-5,7,2'-trihydroxy-8-methylflavanone] (7) and pisonivanol [(2R,3R)-3,7-dihydroxy-5,6-dimethoxyflavanone] (8), one new isoflavonoid, pisonianone (..
- Pigment epithelium-derived factor inhibits advanced glycation end-product-induced angiogenesis and stimulates apoptosis in retinal endothelial cells
Department of Biotechnology, Division of Molecular and Cellular Biology, Kalasalingam University, Anand Nagar, Krishnankoil, 626190, Tamil Nadu, India
Life Sci 85:719-31. 2009
- A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity
JOSEPH R GARLICH
Semafore Pharmaceuticals, Indianapolis, Indiana, USA
Cancer Res 68:206-15. 2008
..The results support SF1126 as a viable pan PI3K inhibitor for phase I clinical trials in cancer and provide support for a new paradigm, the application of pan PI3K inhibitory prodrugs for the treatment of cancer...