Summary: An indolocarbazole that is a potent PROTEIN KINASE C inhibitor which enhances cAMP-mediated responses in human neuroblastoma cells. (Biochem Biophys Res Commun 1995;214(3):1114-20)

Top Publications

  1. ncbi Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1
    Joachim Manns
    Department of Internal Medicine I, Institute for Medical Virology and Epidemiology of Viral Diseases, University of Tubingen, Tubingen, Germany
    FASEB J 25:3250-61. 2011
  2. pmc Staurosporine induces necroptotic cell death under caspase-compromised conditions in U937 cells
    Zsuzsanna A Dunai
    1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Budapest, Hungary
    PLoS ONE 7:e41945. 2012
  3. ncbi Protein kinase inhibition of clinically important staurosporine analogues
    Osman A B S M Gani
    The Norwegian Structural Biology Center, Institute of Chemistry, University of Tromsø, 9037, Tromsø, Norway
    Nat Prod Rep 27:489-98. 2010
  4. ncbi Staurosporine induces apoptosis of melanoma by both caspase-dependent and -independent apoptotic pathways
    Xu Dong Zhang
    Oncology and Immunology Unit, Newcastle Mater Hospital, Newcastle, New South Wales, Australia
    Mol Cancer Ther 3:187-97. 2004
  5. pmc Modulation of fungal sensitivity to staurosporine by targeting proteins identified by transcriptional profiling
    Andreia S Fernandes
    IBMC Instituto de Biologia Molecular e Celular, Portugal
    Fungal Genet Biol 48:1130-8. 2011
  6. pmc SIRT3 protects from hypoxia and staurosporine-mediated cell death by maintaining mitochondrial membrane potential and intracellular pH
    L Pellegrini
    Department of Experimental Medicine, Sapienza University of Rome, Rome, Italy
    Cell Death Differ 19:1815-25. 2012
  7. pmc Staurosporine induces rapid homotypic intercellular adhesion of U937 cells via multiple kinase activation
    Jae Youl Cho
    Department of Immunology and Molecular Pathology, Windeyer Institute of Medical Sciences, University College London, 46 Cleveland Street, London W1T 4JF
    Br J Pharmacol 140:269-76. 2003
  8. ncbi DIDS attenuates staurosporine-induced cardiomyocyte apoptosis by PI3K/Akt signaling pathway: activation of eNOS/NO and inhibition of Bax translocation
    An Heng Liu
    Department of Geriatrics, Xijing Hospital, Fourth Military Medical University, Xi an, China
    Cell Physiol Biochem 22:177-86. 2008
  9. pmc Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3
    Thomas Fischer
    Dana Farber Cancer Institute, 44 Binney St, Boston, MA 02115, USA
    J Clin Oncol 28:4339-45. 2010
  10. ncbi The Chk1 protein kinase and the Cdc25C regulatory pathways are targets of the anticancer agent UCN-01
    P R Graves
    Department of Cell Biology, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 275:5600-5. 2000

Research Grants

Detail Information

Publications334 found, 100 shown here

  1. ncbi Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1
    Joachim Manns
    Department of Internal Medicine I, Institute for Medical Virology and Epidemiology of Viral Diseases, University of Tubingen, Tubingen, Germany
    FASEB J 25:3250-61. 2011
    The protein kinase inhibitor staurosporine is one of the most potent and frequently used proapoptotic stimuli, although its mechanism of action is poorly understood...
  2. pmc Staurosporine induces necroptotic cell death under caspase-compromised conditions in U937 cells
    Zsuzsanna A Dunai
    1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Budapest, Hungary
    PLoS ONE 7:e41945. 2012
    ..Here we report that staurosporine, the classical inducer of intrinsic apoptotic pathway can induce necroptosis under caspase-compromised ..
  3. ncbi Protein kinase inhibition of clinically important staurosporine analogues
    Osman A B S M Gani
    The Norwegian Structural Biology Center, Institute of Chemistry, University of Tromsø, 9037, Tromsø, Norway
    Nat Prod Rep 27:489-98. 2010
    The isolation in 1977 of the microbial alkaloid staurosporine inaugurated research into several distinct series of related natural and synthetic compounds...
  4. ncbi Staurosporine induces apoptosis of melanoma by both caspase-dependent and -independent apoptotic pathways
    Xu Dong Zhang
    Oncology and Immunology Unit, Newcastle Mater Hospital, Newcastle, New South Wales, Australia
    Mol Cancer Ther 3:187-97. 2004
    b>Staurosporine has long been used in vitro as an initiator of apoptosis in many different cell types, but the mechanism involved remains poorly understood...
  5. pmc Modulation of fungal sensitivity to staurosporine by targeting proteins identified by transcriptional profiling
    Andreia S Fernandes
    IBMC Instituto de Biologia Molecular e Celular, Portugal
    Fungal Genet Biol 48:1130-8. 2011
    An analysis of the time-dependent genetic response to the death-inducer staurosporine was performed in Neurospora crassa by transcriptional profiling...
  6. pmc SIRT3 protects from hypoxia and staurosporine-mediated cell death by maintaining mitochondrial membrane potential and intracellular pH
    L Pellegrini
    Department of Experimental Medicine, Sapienza University of Rome, Rome, Italy
    Cell Death Differ 19:1815-25. 2012
    ..Here, we show that in mammalian cells subjected to hypoxia and staurosporine treatment SIRT3 prevents loss of mitochondrial membrane potential (ΔΨ(mt)), intracellular acidification and ..
  7. pmc Staurosporine induces rapid homotypic intercellular adhesion of U937 cells via multiple kinase activation
    Jae Youl Cho
    Department of Immunology and Molecular Pathology, Windeyer Institute of Medical Sciences, University College London, 46 Cleveland Street, London W1T 4JF
    Br J Pharmacol 140:269-76. 2003
    1. Staurosporine is a broad-specificity kinase inhibitor, which has acted as lead compound for the development of some novel cytotoxic compounds for treatment of cancer...
  8. ncbi DIDS attenuates staurosporine-induced cardiomyocyte apoptosis by PI3K/Akt signaling pathway: activation of eNOS/NO and inhibition of Bax translocation
    An Heng Liu
    Department of Geriatrics, Xijing Hospital, Fourth Military Medical University, Xi an, China
    Cell Physiol Biochem 22:177-86. 2008
  9. pmc Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3
    Thomas Fischer
    Dana Farber Cancer Institute, 44 Binney St, Boston, MA 02115, USA
    J Clin Oncol 28:4339-45. 2010
    ..Midostaurin (PKC412; N-benzoylstaurosporin) is a multitargeted tyrosine kinase inhibitor, with demonstrated activity in patients with AML/myelodysplastic syndrome (MDS) with FLT3 mutations...
  10. ncbi The Chk1 protein kinase and the Cdc25C regulatory pathways are targets of the anticancer agent UCN-01
    P R Graves
    Department of Cell Biology, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 275:5600-5. 2000
    ..Taken together our results identify the Chk1 kinase and the Cdc25C pathway as potential targets of G(2) checkpoint abrogation by UCN-01...
  11. ncbi Staurosporine induces apoptosis through both caspase-dependent and caspase-independent mechanisms
    C A Belmokhtar
    INSERM U496, Centre G Hayem, , avenue Claude Vellefaux, 75010 Paris, France
    Oncogene 20:3354-62. 2001
    ..We report here that staurosporine, a well known inducer of apoptosis in a wide range of cell lines, displays distinct ability to trigger ..
  12. pmc Calcium-independent phospholipase A2 localizes in and protects mitochondria during apoptotic induction by staurosporine
    Konstantin Seleznev
    Division of Experimental Diabetes and Aging, Department of Geriatrics and Adult Development, Mount Sinai School of Medicine, New York, New York 10029, USA
    J Biol Chem 281:22275-88. 2006
    ..of mitochondrial function from damage caused by mitochondrially generated ROS during apoptotic induction by staurosporine (STS). We show that iPLA2-expressing cells were relatively resistant to STS-induced apoptosis...
  13. ncbi Effects of estrone on N-methyl-D-aspartic acid- and staurosporine-induced changes in caspase-3-like protease activity and lactate dehydrogenase-release: time- and tissue-dependent effects in neuronal primary cultures
    M Kajta
    Department of Endocrinology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Neuroscience 123:515-26. 2004
    ..present study we compared effects of estrone (100 and 500 nM) on N-methyl-D-aspartic acid (NMDA) (1 mM)- and staurosporine (1 microM)-induced caspase-3-like activity and lactate dehydrogenase (LDH)-release in primary cultures of rat ..
  14. ncbi Phosphorylation of Ser45 and Ser59 of αB-crystallin and p38/extracellular regulated kinase activity determine αB-crystallin-mediated protection of rat brain astrocytes from C2-ceramide- and staurosporine-induced cell death
    Rongyu Li
    Institut fur Neurobiochemie, Otto von Guericke Universitat Magdeburg, Medizinische Fakultat, Magdeburg, Germany
    J Neurochem 118:354-64. 2011
    ..and protease-activated receptor (PAR) are involved in protection of astrocytes against C2-ceramide- and staurosporine-induced cell death [Li et al. (2009) J. Neurochem.110, 1433-1444]...
  15. ncbi Reactive oxygen species participate in the p38-mediated apoptosis induced by potassium deprivation and staurosporine in cerebellar granule neurons
    Yazmín Ramiro-Cortés
    Division of Neuroscience, Institute of Cell Physiology, National University of Mexico, Mexico City, Mexico
    Int J Biochem Cell Biol 43:1373-82. 2011
    Apoptosis induced by low potassium (K5) or staurosporine in cerebellar granule neurons triggers an increase in reactive oxygen species (ROS) levels...
  16. ncbi Cleavage at the caspase-6 site is required for neuronal dysfunction and degeneration due to mutant huntingtin
    Rona K Graham
    Department of Medical Genetics, Centre for Molecular Medicine and Therapeutics, University of British Columbia, Vancouver, BC V5Z 4H4, Canada
    Cell 125:1179-91. 2006
    ..are protected against neurotoxicity induced by multiple stressors including NMDA, quinolinic acid (QA), and staurosporine. These results are consistent with proteolysis of htt at the caspase-6 cleavage site being an important event ..
  17. ncbi Silencing the constitutive active transcription factor CREB by the LKB1-SIK signaling cascade
    Yoshiko Katoh
    Molecular Physiological Chemistry, Osaka University Medical School, Japan
    FEBS J 273:2730-48. 2006
    ..The inactivation of kinase cascades by 10 nm staurosporine in LKB1-positive HEK293 cells also induced unregulated, constitutively activated, CRE activity...
  18. pmc Noncovalent wild-type-sparing inhibitors of EGFR T790M
    Ho June Lee
    Department of Discovery Oncology, Genentech, Inc, South San Francisco, California 94080, USA
    Cancer Discov 3:168-81. 2013
  19. pmc Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia
    R M Stone
    Medical Oncology, Dana Farber Cancer Institute, Boston, MA, USA
    Leukemia 26:2061-8. 2012
    ..A phase III prospective trial is ongoing (CALGB 10603, NCT00651261)...
  20. pmc Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors
    E Weisberg
    Department of Medical Oncology, Dana Farber Cancer Institute, Harvard Medical School, Boston, MA, USA
    Leukemia 26:2233-44. 2012
    ..These results hint at a novel concept of using combination therapy to override drug resistance in mutant FLT3-positive AML in the bone marrow niche and suppress or eradicate residual disease...
  21. ncbi MAGI2 enhances the sensitivity of BEL-7404 human hepatocellular carcinoma cells to staurosporine-induced apoptosis by increasing PTEN stability
    Xin Li
    Department of Biochemistry and Molecular Biology, School of Basic Medical Science, Fudan University, Shanghai 200032, P R China
    Int J Mol Med 32:439-47. 2013
    ..The cells were then treated with various doses of staurosporine (STS) for different periods of time...
  22. ncbi Down-regulation of DNA methyltransferase 3B in staurosporine-induced apoptosis and its mechanism in human hepatocarcinoma cell lines
    Chao Zhao
    Department of Biochemistry and Molecular Biology, Shanghai Medical College, Fudan University, Shanghai, China
    Mol Cell Biochem 376:111-9. 2013
    ..We concluded here that STS-regulated DNMT3B gene expression via p-JNK and down-regulation of DNMT3B-mediated STS-induced apoptosis through the up-regulation p16 expression...
  23. pmc Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models
    Cynthia X Ma
    Section of Breast Oncology, Division of Oncology, Washington University School of Medicine, St Louis, Missouri 63110 1093, USA
    J Clin Invest 122:1541-52. 2012
    ..In addition, knockdown of p53 sensitized WU-BC3 tumors to the combination therapy. These results demonstrate that p53 is a major determinant of how TNBCs respond to therapies that combine DNA damage with Chk1 inhibition...
  24. ncbi Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412
    Richard M Stone
    Dana Farber Cancer Institute, Boston, MA 02115, USA
    Blood 105:54-60. 2005
    ..PKC412 is an oral tyrosine kinase inhibitor with clinical activity in patients with AML whose blasts have an activating mutation of FLT3, suggesting potential use in combination with active agents, such as chemotherapy...
  25. ncbi Human alphaA- and alphaB-crystallins bind to Bax and Bcl-X(S) to sequester their translocation during staurosporine-induced apoptosis
    Y W Mao
    Department of Molecular Biology, University of Medicine and Dentistry of New Jersey, Stratford, NJ, USA
    Cell Death Differ 11:512-26. 2004
    ..Here, we demonstrate that human alphaA- and alphaB-crystallins prevent staurosporine-induced apoptosis through interactions with members of the Bcl-2 family...
  26. pmc beta-Adrenoceptor blockers protect against staurosporine-induced apoptosis in SH-SY5Y neuroblastoma cells
    Maya Mikami
    Department of Anesthesiology, Columbia University P and S, New York, NY 10032, USA
    Eur J Pharmacol 589:14-21. 2008
    ..and ICI 118551 (1-[2,3-(dihydro-7-methyl-1H-iden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol), against staurosporine-induced apoptosis in SH-SY5Y human neuroblastoma cells...
  27. ncbi Abrogation of the Chk1-mediated G(2) checkpoint pathway potentiates temozolomide-induced toxicity in a p53-independent manner in human glioblastoma cells
    Y Hirose
    Brain Tumor Research Center, Department of Neurological Surgery, University of California-San Francisco, 2340 Sutter Street, San Francisco, CA 94143-0875, USA
    Cancer Res 61:5843-9. 2001
    ..Furthermore, inhibition of the cytoprotective G(2) arrest pathway sensitizes cells to TMZ-induced cytotoxicity and may represent a novel, mechanism-based means of increasing TMZ efficacy in both p53 wild-type and p53 mutant glioma cells...
  28. ncbi Defective p53 signaling in p53 wild-type tumors attenuates p21waf1 induction and cyclin B repression rendering them sensitive to Chk1 inhibitors that abrogate DNA damage-induced S and G2 arrest
    Aime A Levesque
    Department of Pharmacology and Toxicology and Norris Cotton Cancer Center, Dartmouth Medical School, Lebanon, NH 03756, USA
    Mol Cancer Ther 7:252-62. 2008
  29. ncbi Dose- and time-dependent pharmacokinetics of midostaurin in patients with diabetes mellitus
    Yanfeng Wang
    Oncology Clinical Pharmacology, Novartis Pharmaceuticals Corporation, 180 Park Ave, Florham Park, NJ 07932 0675, USA
    J Clin Pharmacol 48:763-75. 2008
    ..The most common treatment-related adverse events (eg, loose stools, nausea, vomiting, and headache) were found to be dose related, and the frequency increased markedly above the 150-mg/day dose level...
  30. pmc The serine/threonine kinase Pim-2 is a transcriptionally regulated apoptotic inhibitor
    Casey J Fox
    Abramson Family Cancer Research Institute, Philadelphia, Pennsylvania 19104, USA
    Genes Dev 17:1841-54. 2003
    ..These results establish Pim-2 as a direct link between growth factor-induced transcription and a novel, kinase-dependent pathway that promotes cell-autonomous survival...
  31. ncbi Prevention of apoptosis by Bcl-2: release of cytochrome c from mitochondria blocked
    J Yang
    Department of Biochemistry, Emory University School of Medicine, Atlanta, GA 30322, USA
    Science 275:1129-32. 1997
    ..Overexpression of Bcl-2 prevented the efflux of cytochrome c from the mitochondria and the initiation of apoptosis. Thus, one possible role of Bcl-2 in prevention of apoptosis is to block cytochrome c release from mitochondria...
  32. ncbi Induction of the mitochondrial permeability transition mediates the killing of HeLa cells by staurosporine
    M Tafani
    Department of Pathology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    Cancer Res 61:2459-66. 2001
    The role of the mitochondrial permeability transition (MPT) in the killing of HeLa cells by staurosporine (STR) was assessed with the use of bongkrekic acid (BK), an inhibitor of the MPT...
  33. ncbi Estrogen receptor alpha inhibits p53-mediated transcriptional repression: implications for the regulation of apoptosis
    Aejaz Sayeed
    Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Cancer Res 67:7746-55. 2007 reduced Survivin expression and enhanced the propensity of MCF-7 cells to undergo apoptosis in response to staurosporine treatment, an effect that was blocked by exogenous expression of Survivin...
  34. ncbi Spatiotemporal activation of caspase-dependent and -independent pathways in staurosporine-induced apoptosis of p53wt and p53mt human cervical carcinoma cells
    Magali Nicolier
    CHU Jean Minjoz, EA 3181, IFR 133, Universite de Franche Comte, UFR Médecine et Pharmacie, Besancon, France
    Biol Cell 101:455-67. 2009
    ..has reported that p53 is a key contributor of mitochondrial apoptosis in cervical carcinoma cells after staurosporine exposure...
  35. pmc Staurosporine induces endothelial cell apoptosis via focal adhesion kinase dephosphorylation and focal adhesion disassembly independent of focal adhesion kinase proteolysis
    Jahangir Kabir
    Department of Medicine, BHF Laboratories, University College London, 5 University Street, London WC1E 6JJ, U K
    Biochem J 367:145-55. 2002
    ..phosphorylation and proteolysis during apoptosis of primary porcine aortic endothelial cells (PAEC) induced by staurosporine, a widely used apoptogenic agent in diverse cell types...
  36. pmc PUMA induction by FoxO3a mediates the anticancer activities of the broad-range kinase inhibitor UCN-01
    Crissy Dudgeon
    Department of Pharmacology and Chemical Biology, University of Pittsburgh Cancer Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA
    Mol Cancer Ther 9:2893-902. 2010
    ..In this study, we found that UCN-01, a staurosporine analogue and broad-range kinase inhibitor used in clinical trials, inhibits colon cancer cell growth by ..
  37. ncbi Fission yeast genes that confer resistance to staurosporine encode an AP-1-like transcription factor and a protein kinase related to the mammalian ERK1/MAP2 and budding yeast FUS3 and KSS1 kinases
    T Toda
    Department of Biophysics, Faculty of Science, Kyoto University, Japan
    Genes Dev 5:60-73. 1991
    b>Staurosporine, a potent inhibitor of protein kinase C, arrests fission yeast cell elongation specifically at a stage immediately after cell division...
  38. ncbi Preclinical and clinical development of cyclin-dependent kinase modulators
    A M Senderowicz
    DTP Clinical Trials Unit, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD 20892, USA
    J Natl Cancer Inst 92:376-87. 2000
    ..Thus, modulation of cdk activity is an attractive target for cancer chemotherapy, and several agents that modulate cdk activity are in or are approaching entry into clinical trials...
  39. pmc Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation
    Jason Gotlib
    Department of Medicine, Division of Hematology, Stanford University, Stanford Cancer Center, 875 Blake Wilbur Dr, Rm 2327B, Stanford, CA 94305 5821, USA
    Blood 106:2865-70. 2005
    ..This case indicates that KIT tyrosine kinase inhibition is a feasible approach in SM, but single-agent clinical efficacy may be limited by clonal evolution in the advanced leukemic phase of this disease...
  40. ncbi JNK- and p38 kinase-mediated phosphorylation of Bax leads to its activation and mitochondrial translocation and to apoptosis of human hepatoma HepG2 cells
    Bong Jo Kim
    Laboratory of Membrane Biochemistry and Biophysics, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Biol Chem 281:21256-65. 2006
    ..Phosphorylation of Bax by JNK and p38 kinase activated after treatment with staurosporine, H(2)O(2), etoposide, and UV light was demonstrated by the shift in the pI value of Bax on two-dimensional ..
  41. ncbi Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines
    Y Furukawa
    Department of Stem Cell Regulation, Center for Molecular Medicine, Jichi Medical School, Tochigi, Japan
    Leukemia 21:1005-14. 2007
    ..Our findings may be of help for the design of PKC412-based combination chemotherapy...
  42. ncbi Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase
    T Tamaoki
    Biochem Biophys Res Commun 135:397-402. 1986
    b>Staurosporine, microbial alkaloid which has been known to have antifungal activity was found to inhibit markedly phospholipid/Ca++dependent protein kinase (protein kinase C) from rat brain, with an IC50 value of 2.7 nM...
  43. pmc Apoptotic mechanisms in T47D and MCF-7 human breast cancer cells
    L M Mooney
    Institute for Cancer Studies, Division of Genomic Medicine, Medical School, University of Sheffield, Sheffield S10 2RX, UK
    Br J Cancer 87:909-17. 2002
    To investigate the mechanisms underlying apoptosis in breast cancer cells, staurosporine was used as an apoptotic stimulus in the human breast cancer cell lines MCF-7 and T47D...
  44. ncbi Calpain-mediated cleavage of Atg5 switches autophagy to apoptosis
    Shida Yousefi
    Department of Pharmacology, University of Bern, CH 3010 Bern, Switzerland
    Nat Cell Biol 8:1124-32. 2006
    ..Taken together, calpain-mediated Atg5 cleavage provokes apoptotic cell death, therefore, represents a molecular link between autophagy and apoptosis--a finding with potential importance for clinical anticancer therapies...
  45. ncbi Dissecting temporal and spatial control of cytokinesis with a myosin II Inhibitor
    Aaron F Straight
    Department of Cell Biology and Institute of Chemistry and Cell Biology, Harvard Medical School, 250 Longwood Avenue, Boston, MA 02115, USA
    Science 299:1743-7. 2003
    ..Continuous signals from microtubules are required to maintain the position of the cleavage furrow, and these signals control the localization of myosin II independently of other furrow components...
  46. ncbi An increase in intracellular Ca2+ is required for the activation of mitochondrial calpain to release AIF during cell death
    E Norberg
    Institute of Environmental Medicine, Division of Toxicology, Karolinska Institutet, Stockholm, Sweden
    Cell Death Differ 15:1857-64. 2008
    ..Hence, import of extracellular Ca(2+) into staurosporine-treated cells caused the activation of a calpain, located in the intermembrane space of mitochondria...
  47. ncbi Apoptosis induced by staurosporine alters chaperone and endoplasmic reticulum proteins: Identification by quantitative proteomics
    Duncan M Short
    Astellas CNS Research in Edinburgh ACE, University of Edinburgh, Edinburgh, UK
    Proteomics 7:3085-96. 2007
    ..proteomics approach has been employed to define alterations in protein levels in apoptosis induced with staurosporine (STS). Human neuroblastoma derived SH-SY5Y cells were treated with STS (500 nM for 6 h) to induce apoptosis...
  48. ncbi Human Scythe contains a functional nuclear localization sequence and remains in the nucleus during staurosporine-induced apoptosis
    S T Manchen
    Department of Biological Sciences, University of Windsor, Windsor, Ontario, N9B 3P4, Canada
    Biochem Biophys Res Commun 287:1075-82. 2001
    ..Furthermore, induction of apoptosis by staurosporine does not cause redistribution or cleavage of Scythe, suggesting that Scythe remains localized in the nucleus ..
  49. ncbi Caspase-3-mediated processing of poly(ADP-ribose) glycohydrolase during apoptosis
    E B Affar
    Health and Environment Unit, Laval University Medical Research Center, Centre Hospitalier Universitaire de Quebec, Canada
    J Biol Chem 276:2935-42. 2001
    ..In this work, we report that PARG is cleaved during etoposide-, staurosporine-, and Fas-induced apoptosis in human cells...
  50. ncbi Staurosporine inhibits protein kinase C and prevents phorbol ester-mediated leukotriene D4 receptor desensitization in RBL-1 cells
    R V Vegesna
    Department of Molecular Pharmacology, Smith Kline and French Laboratories, Philadelphia, Pennsylvania 19101
    Mol Pharmacol 33:537-42. 1988
    The aim of the present study was to investigate the effects of staurosporine on phorbol-myristate acetate (PMA)-induced activation of protein kinase C (PKC) and the desensitization of leukotriene D4 (LTD4)-stimulated Ca2+ mobilization in ..
  51. ncbi Staurosporine induces apoptosis and necroptosis in cultured rat astrocytes
    Janez Simenc
    Medical Faculty, Institute of Pharmacology and Experimental Toxicology, University of Ljubljana, Ljubljana, Slovenia
    Drug Chem Toxicol 35:399-405. 2012
    ..In this study, apoptosis and necroptosis were induced in cultured rat astrocytes by staurosporine. When a low concentration (10(-7) M) of staurosporine was applied, a significantly increased proportion of ..
  52. ncbi Staurosporine inhibits phosphorylation of translational regulators linked to mTOR
    A R Tee
    School of Life Sciences, Medical Sciences Institute Wellcome Trust Building Complex, University of Dundee, Dow Street, Dundee, DD1 5EH, UK
    Cell Death Differ 8:841-9. 2001
    Treatment of Swiss 3T3 cells with staurosporine resulted in dephosphorylation of two proteins which play key roles in regulating mRNA translation. This occurred before the execution of apoptosis, assessed by caspase-3 activity...
  53. ncbi Staurosporine-induced apoptosis in astrocytes is prevented by A1 adenosine receptor activation
    Patrizia Ballerini
    Department of Biomedical Sciences, G D Annunzio University, Chieti, Italy
    Neurosci Lett 418:66-71. 2007
    ..Our research shows that rat astrocyte exposure to 100 nM staurosporine for 3h caused apoptotic death accompanied by caspase-3, p38 mitogen-ed protein kinase (MAPK) and glycogen ..
  54. ncbi Protein kinase C inhibitors
    Helen C Swannie
    CRC Department of Medical Oncology, Royal Marsden Hospital, Sutton, Surrey, UK SM2 5NG
    Curr Oncol Rep 4:37-46. 2002
    ..This paper reviews the rationale for using PKC inhibitors in cancer therapy, the challenges for clinical trial design, and the recent clinical experience with modulators of PKC activity...
  55. ncbi Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C
    D J Propper
    Cancer Research Campaign Department of Medical Oncology, Beatson Oncology Centre, Glasgow, UK
    J Clin Oncol 19:1485-92. 2001
    PURPOSE: N-Benzoyl staurosporine (PKC412) is a protein kinase C inhibitor with antitumor activity in laboratory models. We determined the toxicity of oral PKC412 administered daily for repeat cycles of 28 days...
  56. pmc Tissue inhibitor of metalloproteinases-1 protects human neurons from staurosporine and HIV-1-induced apoptosis: mechanisms and relevance to HIV-1-associated dementia
    - Ashutosh
    Department of Cell Biology and Anatomy, University of North Texas Health Science Center, Fort Worth, TX 76107, USA
    Cell Death Dis 3:e332. 2012
    ..In this study, we report that staurosporine (STS) and HIV-1(ADA) virus, both led to induction of apoptosis in cultured primary human neurons...
  57. ncbi Staurosporine-induced cell death in salmonid cells: the role of apoptotic volume decrease, ion fluxes and MAP kinase signaling
    Gerhard Krumschnabel
    Department of Ecophysiology, Institute of Zoology, University of Innsbruck, Technikerstrasse 25, Innsbruck, 6020, Austria
    Apoptosis 12:1755-68. 2007
    ..In salmonid hepatoma and gill cells staurosporine induced apoptosis, as assessed by activation of effector caspases, nuclear condensation, and a decrease of ..
  58. ncbi Staurosporine-induced apoptosis presents with unexpected cholinergic effects in a differentiated neuroblastoma cell line
    Guangfeng Li
    Department of Pharmacology, Goethe University Frankfurt, Frankfurt am Main, Germany
    Neurochem Int 61:1011-20. 2012
    ..SH-SY5Y neuroblastoma cells differentiated to the cholinergic phenotype were exposed to 100nM staurosporine. Over a treatment period of 24h, the pro- and anti-apoptotic factors, caspase-3 and Bcl-2, as well as LDH ..
  59. ncbi Memantine attenuates staurosporine-induced activation of caspase-3 and LDH release in mouse primary neuronal cultures
    Danuta Jantas-Skotniczna
    Department of Experimental Neuroendocrinology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Brain Res 1069:145-53. 2006
    ..elucidate this problem, we investigated effect of memantine, an uncompetitive NMDA receptor antagonist and staurosporine alone and in combination on caspase-3 activity and lactate dehydrogenase (LDH) release in primary hippocampal, ..
  60. ncbi Staurosporine induces megakaryocytic differentiation through the upregulation of JAK/Stat3 signaling pathway
    Hsuan Yu Peng
    Department of Biochemical Science and Technology, National Chiayi University, Chiayi 600, Taiwan
    Ann Hematol 90:1017-29. 2011
    ..b>Staurosporine (STS) is an inhibitor of protein kinase C (PKC) with an inhibitory effect on cancer cells through apoptosis ..
  61. pmc Rotenone enhances the antifungal properties of staurosporine
    Ana Castro
    Instituto de Biologia Molecular e Celular, Universidade do Porto, Rua do Campo Alegre 823, Porto, Portugal
    Eukaryot Cell 9:906-14. 2010
    We studied staurosporine-induced cell death in the filamentous fungus Neurospora crassa...
  62. pmc Inhibition of Drp1-dependent mitochondrial fragmentation and apoptosis by a polypeptide antagonist of calcineurin
    G M Cereghetti
    Department of Cellular Physiology and Metabolism, University of Geneva, Switzerland
    Cell Death Differ 17:1785-94. 2010
    ..Cells expressing PPD1 display enhanced clonogenic ability after exposure to staurosporine. A genetic analysis revealed that the activity of PPD1 is independent of the BH3-only protein BAD, another ..
  63. ncbi Profilin 1 potentiates apoptosis induced by staurosporine in cancer cells
    W Yao
    Department of Pancreas and Hepatobiliary Surgery, Fudan University Shanghai Cancer Center, Shanghai, 200032, P R China
    Curr Mol Med 13:417-28. 2013
    ..Further studies showed that mutant p53R273H was involved in apoptosis induced by Staurosporine (STS) via transcription-independent mitochondrial functions...
  64. pmc FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML
    Keith W Pratz
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
    Blood 115:1425-32. 2010
    ..These results have important implications for the potential therapeutic use of FLT3 inhibitors in that patients with newly diagnosed FLT3-mutant AML might be less likely to respond clinically to highly selective FLT3 inhibition...
  65. ncbi Staurosporine-induced apoptosis in human cornea epithelial cells in vitro
    Steffen Hartel
    University of Bremen, Institute of Biophysics, Bremen, Germany
    Cytometry A 55:15-23. 2003
    ..Additionally, we introduce a sensitive analysis of confocal microscopic images to measure the kinetics of staurosporine (STS) induced phosphatidylserine (PS) membrane translocation and early nuclear morphological changes.
  66. pmc Mechanisms of staurosporine induced apoptosis in a human corneal endothelial cell line
    G Thuret
    Cell Death and Neoplasia Laboratory, EA 3063, University of Saint Etienne, France
    Br J Ophthalmol 87:346-52. 2003
    ..The response of a human corneal endothelial cell (HCEC) line to staurosporine, a known inducer of apoptosis, was investigated to gain insights into the intracellular modulators that ..
  67. pmc Apoptotic marker expression in the absence of cell death in staurosporine-treated Leishmania donovani
    Aude L Foucher
    Institut Pasteur CNRS URA2581, Unité de Parasitology Moléculaire et Signalisation, Paris, France
    Antimicrob Agents Chemother 57:1252-61. 2013
    ..Here, we used the generic protein kinase inhibitor staurosporine to gain insight into how interference with phosphotransferase activities affects the viability, growth, and ..
  68. pmc Premature chromosome condensation induced by caffeine, 2-aminopurine, staurosporine and sodium metavanadate in S-phase arrested HeLa cells is associated with a decrease in Chk1 phosphorylation, formation of phospho-H2AX and minor cytoskeletal rearrangemen
    Dorota Rybaczek
    Department of Cytophysiology, University of Łódź, Pilarskiego 14, 90 231, Łódź, Poland
    Histochem Cell Biol 135:263-80. 2011
    ..Additionally, we show that caffeine, 2-aminopurine, staurosporine and sodium metavanadate can induce premature chromosome condensation (PCC) by the abrogation of the S-M ..
  69. ncbi Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2
    A M Lawrie
    Nat Struct Biol 4:796-801. 1997
    b>Staurosporine exhibits nanomolar IC50 values against a wide range of protein kinases...
  70. pmc Smac mimetics: implications for enhancement of targeted therapies in leukemia
    E Weisberg
    Department of Medical Oncology Hematologic Neoplasia, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Leukemia 24:2100-9. 2010
    ..These results support the idea of using IAP inhibitors in conjunction with targeted tyrosine kinase inhibition to override drug resistance and suppress or eradicate residual disease...
  71. ncbi Caspase-3 is required for alpha-fodrin cleavage but dispensable for cleavage of other death substrates in apoptosis
    R U Jänicke
    Institute of Molecular and Cell Biology, The National University of Singapore, 30 Medical Dr, Singapore 117609, Republic of Singapore
    J Biol Chem 273:15540-5. 1998
    ..Tumor necrosis factor- or staurosporine-induced apoptosis of caspase-3-deficient MCF-7 cells resulted in cleavage of the death substrates PARP, Rb, ..
  72. ncbi UCN-01 (7-hydoxystaurosporine) inhibits in vivo growth of human cancer cells through selective perturbation of G1 phase checkpoint machinery
    S Abe
    Department of Surgery, School of Medicine, Keio University, Shinjuku-ku, Tokyo 160-8582, Japan
    Jpn J Cancer Res 92:537-45. 2001
    ..In conclusion, it appears that a determining factor of in vivo UCN-01 sensitivity involves the balance of CDK2 kinase activity and p21 protein induction, resulting in augmented pRb phosphorylation, G1 cell cycle arrest and apoptosis...
  73. pmc A phase II study of cell cycle inhibitor UCN-01 in patients with metastatic melanoma: a California Cancer Consortium trial
    Tianhong Li
    Division of Hematology and Oncology, University of California Davis Cancer Center, 4501 X Street, Suite 3016, Sacramento, CA 95817, USA
    Invest New Drugs 30:741-8. 2012
    ..No dose modification was required as these patients had disease progression. Conclusion Although well tolerated, UCN-01 as a single agent did not have sufficient clinical activity to warrant further study in refractory melanoma...
  74. ncbi Neuroprotection of microglia conditioned media from apoptotic death induced by staurosporine and glutamate in cultures of rat cerebellar granule cells
    Simona Eleuteri
    Department of Biology, University of Bologna, Via Selmi 3, 40126 Bologna, Italy
    Neurosci Lett 448:74-8. 2008 to apoptotic neurons, towards neuroprotection of rat cerebellar granule cells (CGCs) challenged with staurosporine or glutamate...
  75. ncbi Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification
    Scott A Armstrong
    Dana Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
    Cancer Cell 3:173-83. 2003
    ..Finally, we developed a mouse model of MLL and used bioluminescent imaging to determine that PKC412 is active against MLL in vivo...
  76. ncbi Staurosporine sensitizes T lymphoma cells to glucocorticoid-induced apoptosis: role of Nur77 and Bcl-2
    Shlomit Kfir
    The Lautenberg Center of Immunology, Institute of Medical Research, Faculty of Medicine, Hebrew University, Jerusalem, Israel
    Cell Cycle 6:3086-96. 2007
    ..Here we demonstrate that the broad-acting kinase inhibitor staurosporine (STS) confers GC-sensitivity on GC-resistant T lymphoma cells expressing elevated levels of either Bcl-2 or ..
  77. ncbi Regulation of mitochondrial Smac/DIABLO-selective release by survivin
    G Ceballos-Cancino
    Molecular Biology Laboratory, Subdireccion de Investigacion Basica, Instituto Nacional de Cancerologia, Tlalpan, Mexico City, Mexico
    Oncogene 26:7569-75. 2007
    ..These results provide an explanation for the observed differences in the release of mitochondrial intermembrane proteins in various apoptotic models and present a new mechanism for the anti-apoptotic effects of survivin in cancer cells...
  78. ncbi Blockade of adenosine A(2A) receptors prevents staurosporine-induced apoptosis of rat hippocampal neurons
    Carla G Silva
    Center for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    Neurobiol Dis 27:182-9. 2007
    ..noxious brain insults involving apoptosis, we directly tested if A(2A)R blockade prevents apoptosis induced by staurosporine (STS)...
  79. pmc Activity-dependent and -independent nuclear fluxes of HDAC4 mediated by different kinases in adult skeletal muscle
    Yewei Liu
    Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, Baltimore, MD 21201, USA
    J Cell Biol 168:887-97. 2005
    ..shuttling of HDAC4-GFP in unstimulated resting fibers was not altered by KN-62, but was blocked by staurosporine, indicating that different kinases underlie nuclear efflux of HDAC4 in resting and stimulated muscle fibers.
  80. pmc Upregulation of survivin in G2/M cells and inhibition of caspase 9 activity enhances resistance in staurosporine-induced apoptosis
    Anmol Chandele
    National Centre for Cell Science, NCCS Complex, Ganeshkhind, Pune 411 007, India
    Neoplasia 6:29-40. 2004
    ..In this study, we demonstrate a phase-specific resistance due to survivin in staurosporine (STS)-induced apoptosis in the human neuroblastoma cell line SK-N-MC...
  81. ncbi Modulation of cell cycle progression in human tumors: a pharmacokinetic and tumor molecular pharmacodynamic study of cisplatin plus the Chk1 inhibitor UCN-01 (NSC 638850)
    Raymond P Perez
    Section of Hematology Oncology, Department of Medicine, Dartmouth Medical School, Norris Cotton Cancer Center, Lebanon, New Hampshire 03756, USA
    Clin Cancer Res 12:7079-85. 2006
    ..A phase I trial tested the hypothesis that UCN-01 abrogates cisplatin-induced cell cycle arrest (in tumors) at tolerable doses...
  82. pmc Staurosporine-induced apoptosis and hydrogen peroxide-induced necrosis in two human breast cell lines
    A L McKeague
    School of Biology and Biochemistry, The Queen s University of Belfast, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, UK
    Br J Cancer 88:125-31. 2003
    ..b>Staurosporine (SSP)-induced apoptosis and H(2)O(2)-induced necrosis were evaluated by two cytotoxicity assays, neutral red (..
  83. pmc Inhibition of staurosporine-induced apoptosis of endothelial cells by activated protein C requires protease-activated receptor-1 and endothelial cell protein C receptor
    Laurent O Mosnier
    Department of Molecular and Experimental Medicine, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Biochem J 373:65-70. 2003
    In a model of staurosporine-induced apoptosis using EAhy926 endothelial cells, inhibition of apoptosis by activated protein C was dose-dependent and required the enzyme's active site, implicating activated protein C-mediated proteolysis...
  84. ncbi Distinct roles for p53 transactivation and repression in preventing UCN-01-mediated abrogation of DNA damage-induced arrest at S and G2 cell cycle checkpoints
    Aime A Levesque
    Department of Pharmacology and Toxicology, Dartmouth Medical School, Lebanon, NH 03756, USA
    Oncogene 24:3786-96. 2005
    ..These studies provide a mechanistic explanation for how this therapeutic strategy can selectively target tumor cells...
  85. ncbi Heterogeneous apoptotic responses of prostate cancer cell lines identify an association between sensitivity to staurosporine-induced apoptosis, expression of Bcl-2 family members, and caspase activation
    M Marcelli
    Departments of Medicine, Molecular and Cellular Biology, Veterans Administration Medical Center and Baylor College of Medicine, Houston, Texas 77030, USA
    Prostate 42:260-73. 2000
    ..The goal of this work was to identify mechanisms for the inability of metastatic prostate cancer cells to engage the apoptotic pathway following hormonal or cytotoxic therapy...
  86. pmc A Phase 1 study of UCN-01 in combination with irinotecan in patients with resistant solid tumor malignancies
    Paula M Fracasso
    Department of Internal Medicine, Alvin J Siteman Cancer Center and Washington University School of Medicine, St Louis, MO, USA
    Cancer Chemother Pharmacol 67:1225-37. 2011
    ..We conducted a Phase I study to determine the maximum-tolerated dose (MTD), dose-limiting toxicity (DLT), pharmacokinetic, and pharmacodynamic effects of UCN-01 and irinotecan in patients with resistant solid tumors...
  87. pmc Salt-inducible kinase is involved in the regulation of corticotropin-releasing hormone transcription in hypothalamic neurons in rats
    Ying Liu
    Section on Endocrine Physiology, Developmental Endocrinology Branch, Eunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health, 10 Center Drive, Bethesda, Maryland 20892, USA
    Endocrinology 153:223-33. 2012
    ..Conversely, the nonselective SIK inhibitor, staurosporine, increased nuclear TORC2 content and stimulated CRH transcription in 4Bcells and primary neuronal cultures (..
  88. ncbi A role for Chk2 in DNA damage induced mitotic delays in human colorectal cancer cells
    Hanne Varmark
    Program in Cell and Developmental Dynamics, University of Massachusetts Medical School, Worcester, MA, USA
    Cell Cycle 9:312-20. 2010
    ..However, prolonged G(2) arrest with DNA damage can trigger Chk2 independent mitotic delays that may be secondary to kinetochore disruption...
  89. ncbi Extracts of Cynomorium songaricum protect SK-N-SH human neuroblastoma cells against staurosporine-induced apoptosis potentially through their radical scavenging activity
    Yi Lu
    Beijing University of Chinese Medicine, 100029, Beijing, China
    Phytother Res 23:257-61. 2009
    ..This study evaluated the protective effect of different extracts of C. songaricum on staurosporine-induced apoptotic cell death in SK-N-SH neuroblastoma cells...
  90. ncbi Overexpression of BCL-X(L) underlies the molecular basis for resistance to staurosporine-induced apoptosis in PC-3 cells
    X Li
    Department of Medicne, Baylor College of Medicine, Veterans Affairs Medical Center, Houston 77030, USA
    Cancer Res 61:1699-706. 2001
    ..cancer cell lines LNCaP but not PC-3 cells undergo apoptosis after treatment with the protein kinase inhibitor staurosporine (STS)...
  91. ncbi Retinoic acid potentiated the protective effect of NGF against staurosporine-induced apoptosis in cultured chick neurons by increasing the trkA protein expression
    B Ahlemeyer
    Institut fur Pharmakologie und Toxikologie, Fachbereich Pharmazie der Philipps Universität Marburg, Marburg, Germany
    J Neurosci Res 60:767-78. 2000
    ..When chick embryonic neurons were exposed to staurosporine (200 nM, 24 hr), the percentage of apoptotic neurons increased from 15% in controls to 80%, but the treatment ..
  92. pmc Phase I and pharmacokinetic study of UCN-01 in combination with irinotecan in patients with solid tumors
    Antonio Jimeno
    The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Cancer Research Building I, Baltimore, MD, USA
    Cancer Chemother Pharmacol 61:423-33. 2008
  93. ncbi Mitochondrial outer membrane permeability change and hypersensitivity to digitonin early in staurosporine-induced apoptosis
    Shili Duan
    Division of Biology, California Institute of Technology, Pasadena 91125, USA
    J Biol Chem 278:1346-53. 2003
    We have shown here that the apoptosis inducer staurosporine causes an early decrease in the endogenous respiration rate in intact 143B.TK(-) cells...
  94. ncbi The cell cycle inhibitor p57(Kip2) promotes cell death via the mitochondrial apoptotic pathway
    P Vlachos
    Karolinska Institutet, Institute of Environmental Medicine, 171 77 Stockholm, Sweden
    Cell Death Differ 14:1497-507. 2007
    ..selective p57(Kip2) expression sensitizes cancer cells to apoptotic agents such as cisplatin, etoposide and staurosporine (STS) via a mechanism, which does not require p57(Kip2)-mediated inhibition of CDK...
  95. ncbi Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML
    Jingrui Jiang
    Department of Medical Oncology, Dana Farber Cancer Institute, 44 Binney St, D720C, Boston, MA 02115, USA
    Blood 104:1855-8. 2004
    ..These results suggest that mutations at N841 represent a significant new activating mutation in patients with AML and that patients with such mutations may respond to small-molecule FLT3 inhibitors such as PKC412...
  96. ncbi Treatment with extracellular HSP70/HSC70 protein can reduce polyglutamine toxicity and aggregation
    Tatiana V Novoselova
    Laboratory of Cell Protection Mechanisms, Institute of Cytology Russian Academy of Science, St Petersburg, Russia
    J Neurochem 94:597-606. 2005
  97. ncbi A pro-apoptotic effect of the CDK inhibitor p57(Kip2) on staurosporine-induced apoptosis in HeLa cells
    Magnus K R Samuelsson
    Department of Medical Nutrition, Karolinska Institutet, Huddinge University Hospital, Novum, Huddinge SE 141 86, Sweden
    Biochem Biophys Res Commun 296:702-9. 2002
    ..Here, we report that selective expression of the third member in this family, p57(Kip2), potentiated staurosporine-induced apoptosis in HeLa cells. This pro-apoptotic effect was associated with an increased caspase-3 activity...
  98. ncbi Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412
    Ellen Weisberg
    Dana Farber Cancer Institute, Boston, Massachusetts, USA
    Cancer Cell 1:433-43. 2002
    ..PKC412 is a potent inhibitor of mutant FLT3 and is a candidate for testing as an antileukemia agent in AML patients with mutant FLT3 receptors...
  99. pmc Neuroprotection signaling pathway of nerve growth factor and brain-derived neurotrophic factor against staurosporine induced apoptosis in hippocampal H19-7/IGF-IR [corrected]
    Truong L X Nguyen
    Department of Molecular Cell Biology, Samsung Biomedical Research Institute, Sungkyunkwan University School of Medicine, Suwon, Korea
    Exp Mol Med 42:583-95. 2010
    ..of the phosphatidyl inositol 3 kinase (PI3K)/Akt pathway is critical for protection of hippocampal cells from staurosporine (STS) induced apoptosis, characterized by nuclear condensation and activation of the caspase cascade...
  100. ncbi The prevention of the staurosporine-induced apoptosis by Bcl-X(L), but not by Bcl-2 or caspase inhibitors, allows the extensive differentiation of human neuroblastoma cells
    Victor J Yuste
    Grup de Neurobiologia Molecular, Departament de Ciencies Mediques Basiques, Universitat de Lleida, Lleida, Spain
    J Neurochem 80:126-39. 2002
    b>Staurosporine is one of the best apoptotic inducers in different cell types including neuroblastomas...
  101. ncbi Electrophoretic characterization of ribosomal subunits and proteins in apoptosis: specific downregulation of S11 in staurosporine-treated human breast carcinoma cells
    D Nadano
    Molecular Oncology Laboratory, RIKEN (Institute of Physical and Chemical Research, Tsukuba, Ibaraki 305-0074, Japan
    Biochemistry 40:15184-93. 2001
    ..gel to evaluate ribosomal subunits in apoptotic cells (human breast carcinoma MCF-7 cells treated with staurosporine and human 293T cells irradiated with ultraviolet light were used in addition to the two apoptosis systems ..

Research Grants62

  1. Bc12 regulates osteoclast survival
    Junro Yamashita; Fiscal Year: 2010
    ..are normal in their cellular activity, such as proliferation, differentiation, mineral formation, and staurosporine-induced apoptosis...
  2. Neuronal survival, HIV-1 and Astrocyte TIMP-1
    Anuja Ghorpade; Fiscal Year: 2013
    ..Further, neurotoxicity assays were performed using staurosporine, macrophage-tropic HIV-1 virus and glutamate to induce cell death in cultured human neurons...
  3. Discovery Tools for Chemotherapy Resistance to Cell Death.
    Robert W Sobol; Fiscal Year: 2012
    ..and autophagy endpoints and selective response to apoptosis inducing agents (Temozolomide, Camptothecin, staurosporine and Sulindac)...
    Vickram Ramkumar; Fiscal Year: 1999
    ..Inhibition of protein kinase C by staurosporine attenuated activation of these enzymes elicited by both R-PIA and phorbol esters...
  5. Mechanisms of CaMKII Binding to GluN2B and its Role in Synaptic Plasticity and Me
    KELSEY MARIE BARCOMB; Fiscal Year: 2013
    ..Aim will be addressed using two ATP competitive inhibitors of CaMKII, H7 and staurosporine (ST), using the following approaches: (i) measurement of CaMKII-GluN2B binding in an in vitro assay using ..
  6. A HTS Assay for Identifying Anti-Viral Drugs Against Arbovirus Infections
    Qianjun Li; Fiscal Year: 2007
    ..A secondary assay using apoptosis inducers including Staurosporine will also be implemented to confirm hits and exclude false positives including apoptosis inhibitors...
    MYRON JACOBSON; Fiscal Year: 2002
    ..include tumor necrosis factor alpha (TNF-(), anti-Fas antibodies, N-methyl-N'-nitro-N-nitrosoguanidine (MNNG), Staurosporine, and serum withdrawal...
    Larry Jenkins; Fiscal Year: 2000
    ..4) significant downregulation of total protein kinase C (PKC) occurs after TBI; 5) hippocampal microinjected staurosporine (a serine-threonine protein kinase inhibitor) or genistein (a tyrosine kinase inhibitor) both attenuate ..
  9. Complementation assay for protein kinase inhibitors
    RICHARD EGLEN; Fiscal Year: 2002
    ..sensitive, homogenous CEDIA assay to screen protein kinases for selective inhibitors based on the binding of staurosporine to protein kinases...
  10. Role of HSulf-1 Loss in Apoptosis and Drug Resistance
    Viji Shridhar; Fiscal Year: 2007
    ..clones proliferated more slowly and were more sensitive to the induction of apoptosis by cisplatin and staurosporine than their HSulf-1-deficient counterparts...
    Alan Eastman; Fiscal Year: 2001
    ..These experiments should identify a drug combination that can be tested for its selective targeting to p53-defective tumors in future clinical trials. ..
    RICHARD EGLEN; Fiscal Year: 2004
    ..assay which employs our proprietary CEDIA(r) technology and consists of measuring the competitive binding of staurosporine, a universal protein kinase ligand, to individual recombinant protein kinases...
    GEOFFREY CORDELL; Fiscal Year: 1993
    ..g. staurosporine); vi) evaluation of selected plants for antineoplastic activity and fractionation for their active principles; ..
  14. Studies of germinal center B cell survival
    Hector Martinez Valdez; Fiscal Year: 2009
    ..tandem repeats of the LEA (late embryogenesis abundant) motif, which can abrogate apoptosis induced by staurosporine, TNF-a and UV irradiation...
  15. Gene Therapy of Muscle Wasting From Uremia
    Xiaonan Wang; Fiscal Year: 2005
    ..we propose: 1) to test if XlAP blocks muscle protein degradation induced by growth factor withdraw and staurosporine (activating caspase-3) in human skeletal muscle cells; 2) to examine if XlAP can inhibit the CRF-induced ..
  16. Cellular Mechanisms of PPH: Role of K+ Channels
    JASON YUAN; Fiscal Year: 2006
    ..unreadable] [unreadable] In normal PASMC, our preliminary data demonstrate that apoptosis inducers, such as staurosporine (ST) and cytochrome c, increased K+ channel activity, whereas anti-apoptotic proteins (e.g...
  17. In Vivo Imaging of Retinal Apoptosis Using Activatable Permeation Peptides
    EDWARD BARNETT; Fiscal Year: 2007
    ..RGC apoptosis will be induced in rats either pharmacologically using intravitreal injection of staurosporine or through the induction of uniocular elevated intraocular pressure...
  18. Novel targets and agents to treat thrombotic disorders
    John Griffin; Fiscal Year: 2004
    ..on cells will be determined in studies of the EPCR-dependent, PAR1 -dependent abilities of APC to inhibit staurosporine-induced apoptosis and to alter endothelial cell gene expression...
    Kapil Bhalla; Fiscal Year: 2002
    ..Based on the observation that staurosporine (ST) enhances taxol-induced apoptosis, the mechanism of interaction as well as the optimum dosage and ..
  20. Potassium Channel Gene Therapy to Prevent Neuron Death
    Angela Lee; Fiscal Year: 2004
    ..In pilot data we have shown that both protect in primary hippocampal cultures against glutamate, staurosporine, and sodium cyanide...
    John Wood; Fiscal Year: 1999
    ..has been achieved in the area of indolocarbazoles and hence the archetypal naturally occurring congeners staurosporine (1) and K252a (2) have been the focus of considerable research...
    Philip Palade; Fiscal Year: 2004
    ..This grant also seeks to determine how the steroid hormone dexamethasone, the protein kinase C inhibitor staurosporine, and electrical stimulation regulate the expression of the cardiac DHPR in muscle, and to determine the ..
  23. Development and Testing of a Novel Neuroprotective Drug
    David Schubert; Fiscal Year: 2006
    ..appears to be nerve specific, for it does not block the apoptotic death of fibroblasts caused by TNF-alpha or staurosporine. The goals of this project are to use combinatorial and medicinal chemistry to improve the efficacy of this ..
  24. Proteomics of M-L antigens modulating cation transport
    PETER LAUF; Fiscal Year: 2004
  25. Third Symposium Cell Volume & Signalling Regulation
    PETER LAUF; Fiscal Year: 2003
    ..This meeting's success on U.S. soil will foster continuation of gathering of high-caliber scientists at subsequent international meetings ..
  26. Renal Cell Injury by Ischemia: a role for Bid
    Zheng Dong; Fiscal Year: 2009
    ..Finally, completion of the research will facilitate the design of genetic and pharmacological strategies to ameliorate ischemic renal failure by targeting Bid, Bax and their interaction. ..
  27. Promotion of PDT Induced phototoxicity by bile acids
    David Kessel; Fiscal Year: 2003
    ..If the results of preliminary studies are borne out by further investigation, UDCA could offer a safe and effective means for promoting clinical PDT efficacy. ..
  28. Conference on Photodynamic Therapy
    David Kessel; Fiscal Year: 2002
    ..The most recent PDT meeting, sponsored by the International Photodynamic Assn, has more than 600 participants. ..
  29. Protein ubiquitination based neuroprotection for stroke
    Robert Meller; Fiscal Year: 2006
    JOHN HENSON; Fiscal Year: 2005
    ..4. To study the inducible transformation of coelomocytes from a lamellipodial to a filopodial form. ..
  31. Rapid ischemic tolerance: Ubiquitin-mediated structural reorganization
    Robert Meller; Fiscal Year: 2007
    ..Indeed, the long-term aim of these studies is to discover endogenous protective mechanisms that can be translated into effective rapid acting neuroprotective agents for stroke. [unreadable] [unreadable] [unreadable]..
  32. Mechanisms of Renal Na+ Pump Stimulation by Angiotensin
    DOUGLAS YINGST; Fiscal Year: 2005
    ..These results have important implications for understanding normal kidney function, as well as the development of hypertension and heart failure. ..
  33. Cyclic-AMP Induced Crypt Cell Survival in the Intestine
    Jeffrey Rudolph; Fiscal Year: 2008
  34. Monitoring Oxygen Repeatedly for Hypoxic Tumor Therapy
    Mohammad Khan; Fiscal Year: 2007
    ..If successful, this approach potentially could be immediately extended for clinical applications. [unreadable] [unreadable] [unreadable]..
  35. Functional Consequences of Nuclear mGlu5 Receptor Activation
    KAREN O MALLEY; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  36. Semi-artificial nanomachines for detection of DNA damage and apoptosis
    VLADIMIR DIDENKO; Fiscal Year: 2008
    ..abstract_text> ..
  37. Regulation of Mitochondrial Fission/Fusion by PP2A and PKA in Neurons
    Stefan Strack; Fiscal Year: 2009
    ..Our studies may ultimately lead to better therapies for stroke and neurodegenerative disorders. ..
  38. Metal Ion is Critical in amyloid beta Induced JNK Activation
    Xiongwei Zhu; Fiscal Year: 2009
    ..Aim 3: Determine the effect of metal ion chelation on Ab-induced JNK activation. Aim 4: Determine whether H2O2 mediates metal-augmented AB-induced JNK activation. ..
    MATTHEW BLIZIOTES; Fiscal Year: 2009
    ..This research should contribute to new treatment and prevention regimens for osteoporosis and thus have a significant positive impact on the health care of the aging population. ..
  40. PKC Modulators for the Treatment of Alzheimer's disease
    Alan Kozikowski; Fiscal Year: 2008
    ..For the best compounds from Aim 2, perform studies in triple transgenic mice to ascertain effects on Abeta and sAPPalpha levels and plaque formation in vivo. ..
  41. Chemical Genetic Analysis of Platelet Granule Secretion
    Robert Flaumenhaft; Fiscal Year: 2008
    ..Once identified, compounds will be tested in a previously established battery of platelet function tests and evaluated for antithrombotic potential in an in vivo murine model of thrombus formation. [unreadable] [unreadable] [unreadable]..
  42. Treatment of Neural Injury with MSCs
    Michael Chopp; Fiscal Year: 2007
    ..The long-term goal of this Program Project application is to translate our finding of therapeutic benefit after treatment of experimental stroke and traumatic brain injury with MSCs to the patient. ..
  43. Development of EPR and NIR Oximetry for Diabetic Foot
    Mohammad Khan; Fiscal Year: 2007
    ..If the promise of these techniques is fulfilled, clinicians will have a new powerful tool for management of peripheral vascular disease, based on fundamental pathophysiology. [unreadable] [unreadable] [unreadable]..
  44. Involvement of Na/Dicarboxylate Cotransporter in Aging
    Ana Pajor; Fiscal Year: 2002
    ..abstract_text> ..
    Martin Edelman; Fiscal Year: 2002
    ..The grant will also allow for continuation of meritorious pilot protocols and will allow GCC to monitor and collect data which will produce mutual benefit to the GCC and CALGB. ..
    John Byrd; Fiscal Year: 2003
    ..The clinical and laboratory results of this trial will provide pharmacokinetic and pharmacodynamic information for additional correlative efforts in both single agent phase II and combination phase I studies. ..
  47. Free radicals detection in aging brain by fullerenes
    VLADIMIR DIDENKO; Fiscal Year: 2003
    ..At a later stage free radicals will be monitored using magnetic resonance tracer and MRI detection. ..
    DENNIS VOELKER; Fiscal Year: 2004
  49. Role of Natriuretic Peptides in the Cochlea
    George Trachte; Fiscal Year: 2004
    ..abstract_text> ..
    DIANA GILLIGAN; Fiscal Year: 2003
    ..abstract_text> ..
  51. Polycyclic Hydrocarbons and CYP1B1 in Breast Cancer
    Colin Jefcoate; Fiscal Year: 2005
    ..The correlation with CYP1B 1 expression and activity will provide insight into the relationship of the mouse model to human breast cancer. ..
  52. IL10 and IGF1 Receptor Axis in Prostate Cancer
    Mark Stearns; Fiscal Year: 2005
    ..Development of therapeutic agents, which target the IL-10R or IGF-R1 axis should be beneficial in the treatment of the disease. ..
  53. FTI Biology & Treatment of Myeloproliferative Disorders
    Jason Gotlib; Fiscal Year: 2005
    ..If clinically efficacious, further studies of R115777 in MPDs will be warranted...
  54. Abnormal Megakaryocyte Development
    DIANA GILLIGAN; Fiscal Year: 2006
    ..Finally, these studies may help in the targeted development of better platelet lowering drugs using rational design to improve on currently available options such as anagrelide, hydroxyurea, and interferon. ..
  55. Hypoxia-induced Proteins as Lung Cancer Biomarkers
    Philip Mack; Fiscal Year: 2006
    ..abstract_text> ..
  56. Discovery of novel fluorescent reporter genes
    Ming Zhao; Fiscal Year: 2004
    ..Reporters with spectral properties that can be used for whole-body imaging of tumors in the lung and their metastases will be candidates for further development for numerous applications of multi-color imaging. ..
  57. Pathogenesis of Persistent Chlamydial STDs
    Deborah Dean; Fiscal Year: 2007
    ..1 Description, ..
  58. RhoB Signaling in Cancer Suppression and Cell Suicide
    George Prendergast; Fiscal Year: 2007
    ..Characterization of these signaling pathways offers a unique opportunity to obtain new insights into cancer pathophysiology and therapeutic response. ..
    Alan Kozikowski; Fiscal Year: 2001
    ..4. For compounds meeting set criteria, to further evaluate their behavioral pharmacological profile in animals using intravenous drug self-administration and drug discrimination procedures. ..