Side-effects of protein kinase inhibitors on ion channels

[1]  K. Das,et al.  Protein kinase C, an elusive therapeutic target? , 2012, Nature Reviews Drug Discovery.

[2]  A. Jimeno,et al.  Axitinib, a new therapeutic option in renal cell carcinoma. , 2012, Drugs of today.

[3]  T. Brümmendorf,et al.  Bosutinib is active in chronic phase chronic myeloid leukemia after imatinib and dasatinib and/or nilotinib therapy failure. , 2012, Blood.

[4]  S. Hahn,et al.  Inhibition of Kv4.3 by genistein via a tyrosine phosphorylation-independent mechanism. , 2011, American journal of physiology. Cell physiology.

[5]  Y. Zhang,et al.  Tyrosine kinase-independent inhibition by genistein on spermatogenic T-type calcium channels attenuates mouse sperm motility and acrosome reaction. , 2009, Cell calcium.

[6]  C. Alzheimer,et al.  1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione (U73122) Selectively Inhibits Kir3 and BK Channels in a Phospholipase C-Independent Fashion , 2008, Molecular Pharmacology.

[7]  Qingzhong Jia,et al.  Molecular basis for genistein-induced inhibition of Kir2.3 currents , 2008, Pflügers Archiv - European Journal of Physiology.

[8]  Qingzhong Jia,et al.  Genistein inhibits voltage-gated sodium currents in SCG neurons through protein tyrosine kinase-dependent and kinase-independent mechanisms , 2008, Pflügers Archiv - European Journal of Physiology.

[9]  Shang-zhi Xu Rottlerin induces calcium influx and protein degradation in cultured lenses independent of effects on protein kinase C delta. , 2007, Basic & clinical pharmacology & toxicology.

[10]  D. Mochly‐Rosen,et al.  Cardioprotective mechanisms of PKC isozyme-selective activators and inhibitors in the treatment of ischemia-reperfusion injury. , 2007, Pharmacological research.

[11]  Ming-Wei Lin,et al.  Potent stimulation of large‐conductance Ca2+‐activated K+ channels by rottlerin, an inhibitor of protein kinase C‐δ, in pituitary tumor (GH3) cells and in cortical neuronal (HCN‐1A) cells , 2007, Journal of cellular physiology.

[12]  Jin Han,et al.  Direct modulation of Ca2+-activated K+ current by H-89 in rabbit coronary arterial smooth muscle cells , 2007 .

[13]  A. Lochner,et al.  The many faces of H89: a review. , 2006, Cardiovascular drug reviews.

[14]  Jin Han,et al.  Direct inhibition of a PKA inhibitor, H-89 on KV channels in rabbit coronary arterial smooth muscle cells. , 2006, Biochemical and biophysical research communications.

[15]  Jae-Hong Ko,et al.  Slowing of the inactivation of voltage-dependent sodium channels by staurosporine, the protein kinase C inhibitor, in rabbit atrial myocytes. , 2006, European journal of pharmacology.

[16]  Jin Han,et al.  The protein kinase A inhibitor, H-89, directly inhibits KATP and Kir channels in rabbit coronary arterial smooth muscle cells. , 2006, Biochemical and biophysical research communications.

[17]  M. Berger,et al.  Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. , 2006, Cancer research.

[18]  S. Marx,et al.  Activation of the BK (SLO1) Potassium Channel by Mallotoxin* , 2005, Journal of Biological Chemistry.

[19]  R. Campbell,et al.  The Protein Kinase Cβ–Selective Inhibitor, Enzastaurin (LY317615.HCl), Suppresses Signaling through the AKT Pathway, Induces Apoptosis, and Suppresses Growth of Human Colon Cancer and Glioblastoma Xenografts , 2005 .

[20]  Jae-Hong Ko,et al.  The protein kinase C inhibitor, bisindolylmaleimide (I), inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells. , 2005, Life sciences.

[21]  O. Werz,et al.  The Aminosteroid Phospholipase C Antagonist U-73122 (1-[6-[[17-β-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione) Potently Inhibits Human 5-Lipoxygenase in Vivo and in Vitro , 2005, Molecular Pharmacology.

[22]  Jae-Hong Ko,et al.  The protein kinase inhibitor, staurosporine, inhibits L-type Ca2+ current in rabbit atrial myocytes. , 2005, Biochemical and biophysical research communications.

[23]  Jin Han,et al.  Staurosporine Inhibits Voltage-Dependent K+ Current Through a PKC-Independent Mechanism in Isolated Coronary Arterial Smooth Muscle Cells , 2005, Journal of cardiovascular pharmacology.

[24]  F. Hofmann,et al.  Inhibition of L-Type Cav1.2 Ca2+ Channels by 2,(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002) and 2-[1-(3-Dimethyl-aminopropyl)-5-methoxyindol-3-yl]-3-(1H-indol-3-yl) Maleimide (Gö6983) , 2005, Molecular Pharmacology.

[25]  Susan S. Taylor,et al.  Regulation of protein kinases; controlling activity through activation segment conformation. , 2004, Molecular cell.

[26]  T. Kirchner,et al.  In Vivo Activity of a Phospholipase C Inhibitor, 1-(6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione (U73122), in Acute and Chronic Inflammatory Reactions , 2004, Journal of Pharmacology and Experimental Therapeutics.

[27]  L. Johnson,et al.  Protein Kinase Inhibitors: Insights into Drug Design from Structure , 2004, Science.

[28]  W. Ho,et al.  Direct block by bisindolylmaleimide of the voltage-dependent K+ currents of rat mesenteric arterial smooth muscle. , 2004, European journal of pharmacology.

[29]  M. Weckström,et al.  Chelerythrine and bisindolylmaleimide I prolong cardiac action potentials by protein kinase C-independent mechanism. , 2003, European journal of pharmacology.

[30]  T. Hunter,et al.  The Protein Kinase Complement of the Human Genome , 2002, Science.

[31]  P. Rock,et al.  Role of nitric-oxide synthase, free radicals, and protein kinase C delta in opioid-induced cardioprotection. , 2002, The Journal of pharmacology and experimental therapeutics.

[32]  P. Cohen Protein kinases — the major drug targets of the twenty-first century? , 2002, Nature reviews. Drug discovery.

[33]  R. Engh,et al.  Structural aspects of protein kinase control-role of conformational flexibility. , 2002, Pharmacology & therapeutics.

[34]  R. MacKinnon,et al.  Chemistry of ion coordination and hydration revealed by a K+ channel–Fab complex at 2.0 Å resolution , 2001, Nature.

[35]  H. Kajiya,et al.  Genistein, a soybean isoflavone, inhibits inward rectifier K(+) channels in rat osteoclasts. , 2001, The Japanese journal of physiology.

[36]  W. Ho,et al.  Inhibition of acetylcholine-activated K(+) current by chelerythrine and bisindolylmaleimide I in atrial myocytes from mice. , 2001, European journal of pharmacology.

[37]  J. Melo,et al.  Targeting the BCR-ABL tyrosine kinase in chronic myeloid leukemia. , 2001, The New England journal of medicine.

[38]  C. Sawyers,et al.  Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome. , 2001, The New England journal of medicine.

[39]  D. Min,et al.  Inhibition of Kv1.3 channels by H-89 (N--[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) independent of protein kinase A. , 2001, Biochemical pharmacology.

[40]  M. Gould,et al.  Inactivation of Ca(2+) action potential channels by the MEK inhibitor PD98059. , 2000, Experimental cell research.

[41]  Zhi-Hao Zhang,et al.  Modulation of a cloned human A-type voltage-gated potassium channel (hKv1.4) by the protein tyrosine kinase inhibitor genistein , 2000, Pflügers Archiv.

[42]  H. Hemmings,et al.  Inhibition of voltage‐dependent sodium channels by Ro 31‐8220, a ‘specific’ protein kinase C inhibitor , 2000, FEBS letters.

[43]  S. Yoon,et al.  Direct block by bisindolylmaleimide of rat Kv1.5 expressed in Chinese hamster ovary cells. , 2000, The Journal of pharmacology and experimental therapeutics.

[44]  W. Catterall,et al.  From Ionic Currents to Molecular Mechanisms The Structure and Function of Voltage-Gated Sodium Channels , 2000, Neuron.

[45]  Yi Liu,et al.  Blocker protection in the pore of a voltage-gated K+ channel and its structural implications , 2000, Nature.

[46]  C. A. Wang,et al.  Inhibitory effect of the kinase inhibitor chelerythrine on acetylcholine-induced current in PC12 cells. , 1999, Archives of biochemistry and biophysics.

[47]  Y. Marunaka,et al.  Effects of PKA inhibitors, H-compounds, on epithelial Na+ channels via PKA-independent mechanisms. , 1999, Life sciences.

[48]  D. Rhie,et al.  Staurosporine directly blocks Kv1.3 channels expressed in Chinese hamster ovary cells , 1999, Naunyn-Schmiedeberg's Archives of Pharmacology.

[49]  I. Laher,et al.  Nonspecific inhibition of myogenic tone by PD98059, a MEK1 inhibitor, in rat middle cerebral arteries. , 1999, Biochemical and biophysical research communications.

[50]  M. Horie,et al.  Genistein inhibits slow component delayed-rectifier K currents via a tyrosine kinase-independent pathway. , 1998, Journal of molecular and cellular cardiology.

[51]  F. Hobbs,et al.  Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase* , 1998, The Journal of Biological Chemistry.

[52]  B. Chait,et al.  The structure of the potassium channel: molecular basis of K+ conduction and selectivity. , 1998, Science.

[53]  A. Newton,et al.  Regulation of protein kinase C. , 1997, Current opinion in cell biology.

[54]  E. Carlier,et al.  Direct block of voltage-sensitive sodium channels by genistein, a tyrosine kinase inhibitor. , 1997, The Journal of pharmacology and experimental therapeutics.

[55]  R. Huber,et al.  Crystal Structures of Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Isoquinolinesulfonyl Protein Kinase Inhibitors H7, H8, and H89 , 1996, The Journal of Biological Chemistry.

[56]  M. Gschwendt,et al.  Inhibition of protein kinase C μ by various inhibitors. Inhibition from protein kinase c isoenzymes , 1996 .

[57]  M. Faul,et al.  (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. , 1996, Journal of medicinal chemistry.

[58]  T. Narahashi,et al.  Neuronal ion channels as the target sites of insecticides. , 1996, Pharmacology & toxicology.

[59]  C. Chiang,et al.  Genistein directly inhibits L-type calcium currents but potentiates cAMP-dependent chloride currents in cardiomyocytes. , 1996, Biochemical and biophysical research communications.

[60]  H. C. Hartzell,et al.  Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels. , 1996, The American journal of physiology.

[61]  S. Jaken Protein kinase C isozymes and substrates. , 1996, Current opinion in cell biology.

[62]  Philip R. Cohen,et al.  PD 098059 Is a Specific Inhibitor of the Activation of Mitogen-activated Protein Kinase Kinase in Vitro and in Vivo(*) , 1995, The Journal of Biological Chemistry.

[63]  D. Fabbro,et al.  Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. , 1995, European journal of biochemistry.

[64]  P. Sugden,et al.  Intracellular signalling through protein kinases in the heart. , 1995, Cardiovascular research.

[65]  D. Snyders,et al.  Determinants of antiarrhythmic drug action. Electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel. , 1995, Circulation research.

[66]  P. Cuatrecasas,et al.  Mitogen-activated Protein Kinase Kinase Inhibition Does Not Block the Stimulation of Glucose Utilization by Insulin (*) , 1995, The Journal of Biological Chemistry.

[67]  A. Bridges,et al.  A synthetic inhibitor of the mitogen-activated protein kinase cascade. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[68]  A. Saltiel,et al.  Inhibition of MAP Kinase Kinase Blocks the Differentiation of PC-12 Cells Induced by Nerve Growth Factor(*) , 1995, The Journal of Biological Chemistry.

[69]  Y. Nishizuka Protein kinase C and lipid signaling for sustained cellular responses , 1995, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[70]  P. Gilon,et al.  Multiple effects and stimulation of insulin secretion by the tyrosine kinase inhibitor genistein in normal mouse islets , 1995, British journal of pharmacology.

[71]  S. Cukierman,et al.  Diacylglycerol-induced activation of protein kinase C attenuates Na+ currents by enhancing inactivation from the closed state , 1994, Pflügers Archiv.

[72]  J. Woodgett,et al.  The stress-activated protein kinases are major c-Jun amino-terminal kinases activated by ischemia and reperfusion. , 1994, The Journal of biological chemistry.

[73]  J. Hsuan,et al.  Interleukin-1 activates a novel protein kinase cascade that results in the phosphorylation of hsp27 , 1994, Cell.

[74]  Michel Morange,et al.  A novel kinase cascade triggered by stress and heat shock that stimulates MAPKAP kinase-2 and phosphorylation of the small heat shock proteins , 1994, Cell.

[75]  C. Marshall,et al.  Activation of MAP kinase kinase is necessary and sufficient for PC12 differentiation and for transformation of NIH 3T3 cells , 1994, Cell.

[76]  E. Sausville,et al.  Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue. , 1994, Molecular pharmacology.

[77]  G. Breitwieser,et al.  Protein kinase-independent inhibition of muscarinic K+ channels by staurosporine. , 1994, The American journal of physiology.

[78]  F. Marks,et al.  Rottlerin, a novel protein kinase inhibitor. , 1994, Biochemical and biophysical research communications.

[79]  A. Saltiel,et al.  Thyrotropin-releasing hormone stimulates MAP kinase activity in GH3 cells by divergent pathways. Evidence of a role for early tyrosine phosphorylation. , 1994, The Journal of biological chemistry.

[80]  K. Guan,et al.  Cloning and characterization of two distinct human extracellular signal-regulated kinase activator kinases, MEK1 and MEK2. , 1993, The Journal of biological chemistry.

[81]  H. Hug,et al.  Protein kinase C isoenzymes: divergence in signal transduction? , 1993, The Biochemical journal.

[82]  Alun D. Hughes,et al.  Tyrosine kinase inhibitors block calcium channel currents in vascular smooth muscle cells. , 1992, Biochemical and biophysical research communications.

[83]  C. Crews,et al.  Phorbol ester stimulates a protein-tyrosine/threonine kinase that phosphorylates and activates the Erk-1 gene product. , 1992, Proceedings of the National Academy of Sciences of the United States of America.

[84]  J. Westwick,et al.  Selective inhibition of protein kinase C. Effect on platelet-activating-factor-induced platelet functional responses. , 1992, The Biochemical journal.

[85]  R. MacKinnon,et al.  The aromatic binding site for tetraethylammonium ion on potassium channels , 1992, Neuron.

[86]  T. Mori,et al.  Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries? , 1991, The Journal of pharmacology and experimental therapeutics.

[87]  H. Coste,et al.  The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. , 1991, The Journal of biological chemistry.

[88]  J. Zheng,et al.  Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase. , 1991, Science.

[89]  J. Zheng,et al.  Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase. , 1991, Science.

[90]  J. Herbert,et al.  Chelerythrine is a potent and specific inhibitor of protein kinase C. , 1990, Biochemical and biophysical research communications.

[91]  F. Fitzpatrick,et al.  Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. , 1990, The Journal of pharmacology and experimental therapeutics.

[92]  T Hoshi,et al.  Biophysical and molecular mechanisms of Shaker potassium channel inactivation , 1990, Science.

[93]  E. Krebs,et al.  Evidence for an epidermal growth factor-stimulated protein kinase cascade in Swiss 3T3 cells. Activation of serine peptide kinase activity by myelin basic protein kinases in vitro. , 1990, The Journal of biological chemistry.

[94]  R. Smith,et al.  Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. , 1990, The Journal of pharmacology and experimental therapeutics.

[95]  M. Hagiwara,et al.  Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. , 1990, The Journal of biological chemistry.

[96]  T. Tamaoki,et al.  Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities. , 1989, The Journal of antibiotics.

[97]  I. Takahashi,et al.  UCN-01 and UCN-02, new selective inhibitors of protein kinase C. I. Screening, producing organism and fermentation. , 1989, The Journal of antibiotics.

[98]  I. Takahashi,et al.  UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities. , 1989, The Journal of antibiotics.

[99]  M. Baggiolini,et al.  The protein kinase inhibitor staurosporine, like phorbol esters, induces the association of protein kinase C with membranes. , 1988, Biochemical and biophysical research communications.

[100]  M. Shibuya,et al.  Genistein, a specific inhibitor of tyrosine-specific protein kinases. , 1987, The Journal of biological chemistry.

[101]  T. Sturgill,et al.  Rapid stimulation by insulin of a serine/threonine kinase in 3T3-L1 adipocytes that phosphorylates microtubule-associated protein 2 in vitro. , 1987, Proceedings of the National Academy of Sciences of the United States of America.

[102]  T. Tamaoki,et al.  Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase. , 1986, Biochemical and biophysical research communications.

[103]  P. Cuatrecasas,et al.  Somatomedin-C stimulates the phosphorylation of the beta-subunit of its own receptor. , 1983, The Journal of biological chemistry.

[104]  M. Cobb,et al.  Insulin activates a tyrosine-specific protein kinase in extracts of 3T3-L1 adipocytes and human placenta. , 1982, Proceedings of the National Academy of Sciences of the United States of America.

[105]  C. Kahn,et al.  Insulin stimulates tyrosine phosphorylation of the insulin receptor in a cell-free system , 1982, Nature.

[106]  J. Nishimura,et al.  Platelet-derived growth factor stimulates tyrosine-specific protein kinase activity in Swiss mouse 3T3 cell membranes. , 1982, Proceedings of the National Academy of Sciences of the United States of America.

[107]  C. Heldin,et al.  Stimulation of tyrosine-specific phosphorylation by platelet-derived growth factor , 1982, Nature.

[108]  J. Shoukimas,et al.  Blockage of squid axon potassium conductance by internal tetra-N-alkylammonium ions of various sizes. , 1981, Biophysical journal.

[109]  S. Cohen,et al.  Identification of phosphotyrosine as a product of epidermal growth factor-activated protein kinase in A-431 cell membranes. , 1980, The Journal of biological chemistry.

[110]  Jin Han,et al.  The effect of tyrosine kinase inhibitor genistein on voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells. , 2009, Vascular pharmacology.

[111]  Jin Han,et al.  Direct modulation of Ca(2+)-activated K(+) current by H-89 in rabbit coronary arterial smooth muscle cells. , 2007, Vascular pharmacology.

[112]  D. Johnston,et al.  Acceleration of K+ channel inactivation by MEK inhibitor U0126. , 2006, American journal of physiology. Cell physiology.

[113]  E. Aandahl,et al.  Localized effects of cAMP mediated by distinct routes of protein kinase A. , 2004, Physiological reviews.

[114]  D. Charon,et al.  The Bisindolylmaleimide GF 109203X Is a Potent and Selective Inhibitor of Protein Kinase C* , 2001 .

[115]  A. L. Goldin,et al.  Resurgence of sodium channel research. , 2001, Annual review of physiology.

[116]  S. Rhee,et al.  Regulation of phosphoinositide-specific phospholipase C. , 2001, Annual review of biochemistry.

[117]  A. Newton Regulation of protein kinase , 1997 .

[118]  S. Steinberg,et al.  Protein kinase C isoform diversity in the heart. , 1995, Journal of molecular and cellular cardiology.

[119]  A. Saltiel,et al.  Bombesin and epidermal growth factor stimulate the mitogen-activated protein kinase through different pathways in Swiss 3T3 cells. , 1993, The Biochemical journal.

[120]  F. Fitzpatrick,et al.  Inhibition of phospholipase C dependent processes by U-73, 122. , 1989, Advances in prostaglandin, thromboxane, and leukotriene research.

[121]  P. Pilch,et al.  Stimulation of tyrosine-specific phosphorylation in vitro by insulin-like growth factor I , 1983, Nature.

[122]  S. Ōmura,et al.  X-Ray crystal structure of staurosporine: a new alkaloid from a Streptomyces strain , 1978 .