Towards selective pharmacological modulation of protein kinase C--opportunities for the development of novel antineoplastic agents.

[1]  T. Bradshaw,et al.  Modulation by staurosporine of phorbol‐ester‐induced effects on growth and protein kinase C localization in a549 human lung‐carcinoma cells , 1992, International journal of cancer.

[2]  R. Rando,et al.  Structural basis of protein kinase C activation by diacylglycerols and tumor promoters. , 1992, Biochemistry.

[3]  Z. Darżynkiewicz,et al.  Different effects of staurosporine, an inhibitor of protein kinases, on the cell cycle and chromatin structure of normal and leukemic lymphocytes. , 1992, Cancer research.

[4]  I. Weinstein,et al.  The modulation of growth by HMBA in PKC overproducing HT29 colon cancer cells. , 1991, Biochemical and biophysical research communications.

[5]  F. Hucho,et al.  The phospholipid analogue, hexadecylphosphocholine, inhibits protein kinase C in vitro and antagonises phorbol ester-stimulated cell proliferation. , 1991, European journal of cancer.

[6]  E. Fitzke,et al.  RO 31-8220 and RO 31-7549 show improved selectivity for protein kinase C over staurosporine in macrophages. , 1991, Biochemical and biophysical research communications.

[7]  S. Hakomori,et al.  Cell membrane signaling as target in cancer therapy. II: Inhibitory effect of N,N,N-trimethylsphingosine on metastatic potential of murine B16 melanoma cell line through blocking of tumor cell-dependent platelet aggregation. , 1991, Cancer research.

[8]  D. Fabbro,et al.  Differential recovery of protein kinase C-α and -ɛ isozymes after long-term phorbol ester treatment in rat renal mesangial cells , 1991 .

[9]  H. Hidaka,et al.  Protein kinase C activation and protooncogene expression in differentiation/retrodifferentiation of human U-937 leukemia cells. , 1991, Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.

[10]  H. Grunicke,et al.  Inhibition of cell proliferation, protein kinase C, and phorbol ester-induced fos expression by the dihydropyridine derivative B859-35. , 1991, Cancer research.

[11]  S. Baylin,et al.  c-myc gene-induced alterations in protein kinase C expression: a possible mechanism facilitating myc-ras gene complementation. , 1991, Cancer research.

[12]  L. Verdonck,et al.  Alkyllysophospholipid ET‐18‐OCH3 acts as an activator of protein kinase C in HL‐60 cells , 1991, FEBS letters.

[13]  S. Akinaga,et al.  Antitumor activity of UCN-01, a selective inhibitor of protein kinase C, in murine and human tumor models. , 1991, Cancer research.

[14]  C. Borner,et al.  Failure of wild-type or a mutant form of protein kinase C-α to transform fibroblasts , 1991, Nature.

[15]  S. Yuspa,et al.  Staurosporine induces protein kinase C agonist effects and maturation of normal and neoplastic mouse keratinocytes in vitro. , 1991, Cancer research.

[16]  M. Johnson,et al.  Phorbol diester-induced alterations in the expression of protein kinase C isozymes and their mRNAs. Analysis in wild-type and phorbol diester-resistant HL-60 cell clones. , 1991, The Journal of biological chemistry.

[17]  H. Hidaka,et al.  Expression of three major protein kinase C isozymes in various types of human leukemic cells. , 1991, Cancer research.

[18]  D. Mochly‐Rosen,et al.  Intracellular receptors for activated protein kinase C. Identification of a binding site for the enzyme. , 1991, The Journal of biological chemistry.

[19]  J. Utsunomiya,et al.  Protein kinase C activity as marker for colorectal cancer , 1991, International journal of cancer.

[20]  M. Ohta,et al.  Expression of a novel immediate early gene during 12-O-tetradecanoylphorbol-13-acetate-induced macrophagic differentiation of HL-60 cells. , 1991, The Journal of biological chemistry.

[21]  P. Parker,et al.  Down‐regulation of a kinase defective PKC‐α , 1991 .

[22]  G. Brooks,et al.  Protein kinase C down-regulation, and not transient activation, correlates with melanocyte growth. , 1991, Cancer research.

[23]  J. Ramsdell,et al.  Bryostatins selectively regulate protein kinase C-mediated effects on GH4 cell proliferation. , 1991, The Journal of biological chemistry.

[24]  J. Lazo,et al.  Cellular sensitization to cis-diamminedichloroplatinum(II) by novel analogues of the protein kinase C activator lyngbyatoxin A. , 1991, Cancer research.

[25]  F. Marks,et al.  Down-regulation of protein kinase C in Swiss 3T3 fibroblasts is independent of its phosphorylating activity. , 1991, Biochemical and biophysical research communications.

[26]  J. Brown,et al.  Dissociation of protein kinase C redistribution from the phosphorylation of its substrates. , 1991, The Journal of biological chemistry.

[27]  D. Fan,et al.  In vitro model for intrinsic drug resistance: effects of protein kinase C activators on the chemosensitivity of cultured human colon cancer cells. , 1991, Molecular pharmacology.

[28]  A. Kraft,et al.  Bryostatin 1: a potential anti-leukemic agent for chronic myelomonocytic leukemia. , 1991, Leukemia.

[29]  H. Grunicke,et al.  Hexadecylphosphocholine inhibits inositol phosphate formation and protein kinase C activity. , 1991, Cancer research.

[30]  L. Schuchter,et al.  Successful treatment of murine melanoma with bryostatin 1. , 1991, Cancer research.

[31]  B. Strulovici,et al.  Distinct mechanisms of regulation of protein kinase C epsilon by hormones and phorbol diesters. , 1991, The Journal of biological chemistry.

[32]  P. Fialkow,et al.  Evidence that weak promotion of carcinogen-initiated cells prevents their progression to malignancy. , 1990, Carcinogenesis.

[33]  G. Schwartz,et al.  Inhibition of invasion of invasive human bladder carcinoma cells by protein kinase C inhibitor staurosporine. , 1990, Journal of the National Cancer Institute.

[34]  P. Parker,et al.  Protein kinase C heterogeneity in GH4C1 rat pituitary cells. Characterization of a Ca2(+)-independent phorbol ester receptor. , 1990, The Journal of biological chemistry.

[35]  J. M. Ford,et al.  Pharmacology of drugs that alter multidrug resistance in cancer. , 1990, Pharmacological reviews.

[36]  I. Weinstein,et al.  Overexpression of protein kinase C in HT29 colon cancer cells causes growth inhibition and tumor suppression , 1990, Molecular and cellular biology.

[37]  T. Sugimura,et al.  Tumor-promoting activity of staurosporine, a protein kinase inhibitor on mouse skin. , 1990, Cancer research.

[38]  M. Herlyn,et al.  Differential expression of protein kinase C and cAMP-dependent protein kinase in normal human melanocytes and malignant melanomas. , 1990, Oncogene.

[39]  T. Tamaoki,et al.  Potent and Specific Inhibitors of Protein Kinase C of Microbial Origin , 1990, Bio/Technology.

[40]  P. Parker,et al.  Proteolytic activation of protein kinase C-epsilon. , 1990, European journal of biochemistry.

[41]  E. Chambaz,et al.  Differential inhibition of protein kinase C subtypes. , 1990, Biochemical and biophysical research communications.

[42]  B. Teicher,et al.  Involvement of protein kinase C in phorbol ester-induced sensitization of HeLa cells to cis-diamminedichloroplatinum(II). , 1990, The Journal of biological chemistry.

[43]  W. Berdel,et al.  Inhibition of protein kinase C, (sodium plus potassium)-activated adenosine triphosphatase, and sodium pump by synthetic phospholipid analogues. , 1990, Cancer research.

[44]  K. Huang,et al.  Effects of suramin, an anti-human immunodeficiency virus reverse transcriptase agent, on protein kinase C. Differential activation and inhibition of protein kinase C isozymes. , 1990, The Journal of biological chemistry.

[45]  R. Heinrikson,et al.  Amino acid sequence and characterization of a protein inhibitor of protein kinase C. , 1990, The Journal of biological chemistry.

[46]  S. Howell,et al.  Increased sensitivity to cis-diamminedichloroplatinum(II) in human ovarian carcinoma cells in response to treatment with 12-O-tetradecanoylphorbol 13-acetate. , 1990, The Journal of biological chemistry.

[47]  H. Ploegh,et al.  A pseudosubstrate peptide inhibits protein kinase C‐mediated phosphorylation in permeabilized Rat‐1 cells , 1990, FEBS letters.

[48]  A. Altman,et al.  Selective post-transcriptional down-regulation of protein kinase C isoenzymes in leukemic T cells chronically treated with phorbol ester. , 1990, The Journal of biological chemistry.

[49]  L. Obeid,et al.  Transcriptional regulation of protein kinase C by 1,25-dihydroxyvitamin D3 in HL-60 cells. , 1990, The Journal of biological chemistry.

[50]  M. Ueffing,et al.  Inhibition of rodent protein kinase C by the anticarcinoma agent dequalinium. , 1990, Cancer research.

[51]  H. Hidaka,et al.  Decreased expression of type II protein kinase C in HL-60 variant cells resistant to induction of cell differentiation by phorbol diester. , 1990, Cancer research.

[52]  V. Stevens,et al.  Characteristics of the growth inhibition and cytotoxicity of long-chain (sphingoid) bases for Chinese hamster ovary cells: evidence for an involvement of protein kinase C. , 1990, Biochimica et biophysica acta.

[53]  B. Horecker,et al.  Isozymes of protein kinase C in human neutrophils and their modification by two endogenous proteinases. , 1990, The Journal of biological chemistry.

[54]  F. Huang,et al.  Differential sensitivity of protein kinase C isozymes to phospholipid-induced inactivation. , 1990, The Journal of biological chemistry.

[55]  K. Suzuki,et al.  Expression and properties of two distinct classes of the phorbol ester receptor family, four conventional protein kinase C types, and a novel protein kinase C. , 1990, The Journal of biological chemistry.

[56]  P. Davis,et al.  Potent selective inhibitors of protein kinase C , 1989, FEBS letters.

[57]  N. Mazurek,et al.  A mutant protein kinase C that can transform fibroblasts , 1989, Nature.

[58]  R. Epand,et al.  Inhibition of protein kinase C by sphingosine correlates with the presence of positive charge. , 1989, Biochemical and biophysical research communications.

[59]  C. Laughton,et al.  Sterically hindered analogues of diacylglycerols. synthesis, binding to the phorbol ester receptor and metabolism in a549 human lung carcinoma cells , 1989, International journal of cancer.

[60]  P. Parker,et al.  Protein kinase C — a family affair , 1989, Molecular and Cellular Endocrinology.

[61]  N. Shimizu,et al.  Cell genetic evidence of correlation of intracellular translocation of protein kinase C (PKC) and PKC-mediated phosphorylation of 80-kDa protein with mitogenic action of tumor promoters , 1989, Somatic cell and molecular genetics.

[62]  Y. Hannun,et al.  The adriamycin-iron(III) complex is a potent inhibitor of protein kinase C. , 1989, The Journal of biological chemistry.

[63]  S. Singletary,et al.  Elevated protein kinase C expression in human breast tumor biopsies relative to normal breast tissue. , 1989, Cancer research.

[64]  Tracey D. Bradshaw,et al.  Comparison of effects of bryostatins 1 and 2 and 12-O-tetradecanoylphorbol-13-acetate on protein kinase C activity in A549 human lung carcinoma cells. , 1989, Cancer research.

[65]  E. Hecker,et al.  Two isozymes of PKC found in HL‐60 cells show a difference in activation by the phorbol ester TPA , 1989, FEBS letters.

[66]  D. Fabbro,et al.  A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and In vitro anti‐proliferative as well as In vivo anti‐tumor activity , 1989, International journal of cancer.

[67]  Y. Nishizuka,et al.  Protein kinase C zeta subspecies from rat brain: its structure, expression, and properties. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[68]  Y. Hannun,et al.  Structural requirements for long-chain (sphingoid) base inhibition of protein kinase C in vitro and for the cellular effects of these compounds. , 1989, Biochemistry.

[69]  T. Tamaoki,et al.  Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. , 1989, Biochemical and biophysical research communications.

[70]  F. Huang,et al.  Differential down-regulation of protein kinase C isozymes. , 1989, The Journal of biological chemistry.

[71]  G. Brooks,et al.  Effects of biologically active tumour-promoting and non-promoting phorbol esters on in vitro growth of melanocytic cells. , 1989, Pigment cell research.

[72]  Makoto Kobayashi,et al.  Lung Cancer Cells Often Express High Levels of Protein Kinase C Activity , 1989, Japanese journal of cancer research : Gann.

[73]  A. Aitken,et al.  Tumour-promoting and hyperplastic effects of phorbol and daphnane esters in CD-1 mouse skin and a synergistic effect of calcium ionophore with the non-promoting activator of protein kinase C, sapintoxin A. , 1989, Carcinogenesis.

[74]  C. Laughton,et al.  Studies on bioactive compounds. 13. Synthesis and lack of growth-inhibitory properties of cyclohexane-1,2,4-triol 1,2-diesters, which resemble ring C of the phorbol ester molecule. , 1989, Journal of medicinal chemistry.

[75]  W. Gullick,et al.  Differences in phorbol-ester-induced down-regulation of protein kinase C between cell lines. , 1989, The Biochemical journal.

[76]  Y. Hannun,et al.  Functions of sphingolipids and sphingolipid breakdown products in cellular regulation. , 1989, Science.

[77]  A. Gescher,et al.  Effects of activators of protein kinase C, including bryostatins 1 and 2, on the growth of A549 human lung carcinoma cells , 1989, International journal of cancer.

[78]  W. May,et al.  Activation of human T lymphocytes by bryostatin. , 1988, Journal of immunology.

[79]  P. Blumberg,et al.  Mimicry of bryostatin 1 induced phosphorylation patterns in HL-60 cells by high-phorbol ester concentrations. , 1988, Cancer research.

[80]  P. Blumberg,et al.  Demonstration of sub-nanomolar affinity of bryostatin 1 for the phorbol ester receptor in rat brain. , 1988, Biochemical pharmacology.

[81]  R. Rando,et al.  Structural studies on the diglyceride-mediated activation of protein kinase C. , 1988, The Journal of biological chemistry.

[82]  K. Koehler,et al.  Modeling of the bryostatins to the phorbol ester pharmacophore on protein kinase C. , 1988, Proceedings of the National Academy of Sciences of the United States of America.

[83]  Y. Nishizuka,et al.  Differential down‐regulation of protein kinase C subspecies in KM3 cells , 1988, FEBS letters.

[84]  Y. Nishizuka,et al.  The molecular heterogeneity of protein kinase C and its implications for cellular regulation , 1988, Nature.

[85]  I. Weinstein,et al.  The origins of human cancer: molecular mechanisms of carcinogenesis and their implications for cancer prevention and treatment--twenty-seventh G.H.A. Clowes memorial award lecture. , 1988, Cancer research.

[86]  A. Fields,et al.  Phosphorylation of lamin B at the nuclear membrane by activated protein kinase C. , 1988, The Journal of biological chemistry.

[87]  A. Kraft,et al.  Differing modulation of protein kinase C by bryostatin 1 and phorbol esters in JB6 mouse epidermal cells. , 1988, The Journal of biological chemistry.

[88]  Y. Hannun,et al.  Aminoacridines, potent inhibitors of protein kinase C. , 1988, The Journal of biological chemistry.

[89]  C. Piantadosi,et al.  Synthesis and evaluation of neoplastic cell growth inhibition of 1-N-alkylamide analogues of glycero-3-phosphocholine. , 1988, Journal of medicinal chemistry.

[90]  Mark D. Johnson,et al.  Overproduction of protein kinase C causesdisordered growth control in rat fibroblasts , 1988, Cell.

[91]  W. Wilkison,et al.  Altered growth regulation and enhanced tumorigenicity of NIH 3T3 fibroblasts transfected with protein kinase C-I cDNA , 1988, Cell.

[92]  R. Bell,et al.  Sangivamycin, a nucleoside analogue, is a potent inhibitor of protein kinase C. , 1988, The Journal of biological chemistry.

[93]  S. Yuspa,et al.  Contrasting duration of inhibition of cell-cell communication in primary mouse epidermal cells by phorbol 12,13-dibutyrate and by bryostatin 1. , 1988, Cancer research.

[94]  B. Kemp,et al.  Protein kinase C contains a pseudosubstrate prototope in its regulatory domain. , 1987, Science.

[95]  A. Kraft,et al.  Antineoplastic bryostatins are multipotential stimulators of human hematopoietic progenitor cells. , 1987, Proceedings of the National Academy of Sciences of the United States of America.

[96]  M. Dell'aquila,et al.  Inhibition by bryostatin 1 of the phorbol ester-induced blockage of differentiation in hexamethylene bisacetamide-treated Friend erythroleukemia cells. , 1987, Cancer research.

[97]  S. Yuspa,et al.  Partial parallelism and partial blockade by bryostatin 1 of effects of phorbol ester tumor promoters on primary mouse epidermal cells. , 1987, Cancer research.

[98]  S. Yuspa,et al.  Bryostatin 1, an activator of protein kinase C, inhibits tumor promotion by phorbol esters in SENCAR mouse skin. , 1987, Carcinogenesis.

[99]  H. Rasmussen,et al.  Disparate effects of activators of protein kinase C on HL-60 promyelocytic leukemia cell differentiation. , 1987, The Journal of biological chemistry.

[100]  Y. Nishizuka,et al.  Three distinct forms of rat brain protein kinase C: differential response to unsaturated fatty acids. , 1987, Biochemical and biophysical research communications.

[101]  A. Ullrich,et al.  Down-regulation of protein kinase C is due to an increased rate of degradation. , 1987, The Biochemical journal.

[102]  F. Bayard,et al.  Influence of 12-O-tetradecanoylphorbol-13-acetate on proliferation and maturation of human breast carcinoma cells (MCF-7): relationship to cell cycle events. , 1987, Cancer research.

[103]  Y. Hannun,et al.  Lysosphingolipids inhibit protein kinase C: implications for the sphingolipidoses. , 1987, Science.

[104]  C. Murakata,et al.  K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. , 1987, Biochemical and biophysical research communications.

[105]  A. Wolfman,et al.  Elevated levels of diacylglycerol and decreased phorbol ester sensitivity in ras-transformed fibroblasts , 1987, Nature.

[106]  C. House,et al.  The influence of basic residues on the substrate specificity of protein kinase C. , 1987, The Journal of biological chemistry.

[107]  A. Kraft,et al.  Bryostatin, an activator of the calcium phospholipid-dependent protein kinase, blocks phorbol ester-induced differentiation of human promyelocytic leukemia cells HL-60. , 1986, Proceedings of the National Academy of Sciences of the United States of America.

[108]  G. Pettit,et al.  Bryostatins: potent, new mitogens that mimic phorbol ester tumor promoters. , 1985, Biochemical and biophysical research communications.

[109]  A. Kraft,et al.  Bryostatin, a non-phorbol macrocyclic lactone, activates intact human polymorphonuclear leukocytes and binds to the phorbol ester receptor. , 1985, Biochemical and biophysical research communications.

[110]  A. Gescher.  Antiproliferative properties of phorbol ester tumour promoters. , 1985, Biochemical pharmacology.

[111]  I. Weinstein,et al.  Inhibition of protein kinase C by tamoxifen. , 1985, Cancer research.

[112]  J. Niedel,et al.  Phorbol diesters and cellular differentiation. , 1984, Journal of the National Cancer Institute.

[113]  E. Rozengurt,et al.  Disappearance of Ca2+-sensitive, phospholipid-dependent protein kinase activity in phorbol ester-treated 3T3 cells. , 1984, Biochemical and biophysical research communications.

[114]  J. Kuo,et al.  Modes of inhibition by acylcarnitines, adriamycin and trifluoperazine of cardiac phospholipid-sensitive calcium-dependent protein kinase. , 1983, Biochemical pharmacology.

[115]  A. Kraft,et al.  Phorbol esters increase the amount of Ca2+, phospholipid-dependent protein kinase associated with plasma membrane , 1983, Nature.

[116]  J. Clardy,et al.  Isolation and structure of bryostatin 1 , 1982 .

[117]  J. F. Day,et al.  Antineoplastic Components of Marine Animals , 1970, Nature.

[118]  J. Bond,et al.  Effect of serum growth factors and phorbol ester on growth and survival of human thyroid epithelial cells expressing mutant ras , 1992, Molecular carcinogenesis.

[119]  D. Longo,et al.  Preclinical evaluation of bryostatin as an anticancer agent against several murine tumor cell lines: in vitro versus in vivo activity. , 1992, Cancer research.

[120]  G. Powis.  Signalling targets for anticancer drug development. , 1991, Trends in pharmacological sciences.

[121]  G. Pettit.  The bryostatins. , 1991, Fortschritte der Chemie organischer Naturstoffe = Progress in the chemistry of organic natural products. Progres dans la chimie des substances organiques naturelles.

[122]  M. Graham,et al.  The differential expression of protein kinase C genes in normal human neonatal melanocytes and metastatic melanomas. , 1991, Carcinogenesis.

[123]  P. Blumberg.  Complexities of the Protein Kinase C Pathway , 1991, Molecular carcinogenesis.

[124]  J. Hickman,et al.  How to kill cancer cells: membranes and cell signaling as targets in cancer chemotherapy. , 1990, Cancer cells.

[125]  Y Nishizuka,et al.  The protein kinase C family: heterogeneity and its implications. , 1989, Annual review of biochemistry.

[126]  M. Morin,et al.  Human multidrug resistant KB cells overexpress protein kinase C: involvement in drug resistance. , 1989, Cancer communications.

[127]  J. A. McBain,et al.  Bryostatin 1 antagonizes the terminal differentiating action of 12-O-tetradecanoylphorbol-13-acetate in a human colon cancer cell. , 1988, Carcinogenesis.