본문 바로가기
KERD
논문KCI 등재

Direct effect of protein kinase C inhibitors on cardiovascular ion channels

Youn Kyoung Son|Da Hye Hong|Dae-Joong Kim|Amy L Firth|Won Sun Park
생화학분자생물학회 (Korean Society Of Biochemistry And Molecular Biology)|2011.09|BMB Reports|제44권 제9호|pp. 559-565

2

조회

0

다운로드

3

인용

0

참고문헌

키워드

Protein kinase CStaurosporineIon channelBisindolylmaleimide (I)ChelerythrineRo 31-8220Rottlerin
주제분류화학

초록

Protein kinase C (PKC) is a central enzyme that modulates numerous biological functions. For this reason, specific PKC inhibitors/activators are required to study PKC-related signaling mechanisms. To date, although many PKC inhibitors have been developed, they are limited by poor selectivity and nonspecificity. In this review, we focus on the nonspecific actions of PKC inhibitors on cardiovascular ion channels in addition to their PKC-inhibiting functions. The aim of this paper is to urge caution when using PKC inhibitors to block PKC function. This information may help to better understand PKC-related physiological/biochemical studies. [BMB reports 2011; 44(9): 559-565]

Abstract

Protein kinase C (PKC) is a central enzyme that modulates numerous biological functions. For this reason, specific PKC inhibitors/activators are required to study PKC-related signaling mechanisms. To date, although many PKC inhibitors have been developed, they are limited by poor selectivity and nonspecificity. In this review, we focus on the nonspecific actions of PKC inhibitors on cardiovascular ion channels in addition to their PKC-inhibiting functions. The aim of this paper is to urge caution when using PKC inhibitors to block PKC function. This information may help to better understand PKC-related physiological/biochemical studies. [BMB reports 2011; 44(9): 559-565]

참고문헌 (55)

  1. Divecha, N, "Phospholipid signaling", Cell, 80, pp.269~278 (1995)
  2. Nishizuka, Y, "Protein kinase C and lipid signaling for sustained cellular responses", FASEB. J, 9, pp.484~496 (1995)
  3. Tamaoki, T, "Staurosporine, a potent inhibitor of phospholipid", Ca2+ dependent protein kinase, 1986, pp.135, 397~402
  4. Toullec, D, "The bisindolylmaleimide GF 109203X is potent and selective inhibitor of protein kinase C", J. Biol. Chem, 266, pp.15771~15781 (1991)
  5. Roffey, J, "Protein kinase C intervention: the state of play", Curr. Opin. Cell Biol, 21, pp.268~279 (2009)
  6. Furusaki, A, "X-Ray crystal structure of staurosporine: a new alkaloid from a Streptomyces strain", J. Chem. Soc. Chem. Commun, 18, pp.800~801 (1978)
  7. Meggio, F, "Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2", Eur. J. Biochem, 234, pp.317~322 (1995)
  8. oxadiazacyclohexadecene-1,3 (2H)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta, "J. Med. Chem", 1996, 2664~2671
  9. Green, L. J, "Development and validation of a drug activity biomarker that shows target inhibition in cancer patients receiving enzastaurin, a novel protein kinase C-beta inhibitor", Clin. Cancer Res, 12, pp.3408~3415 (2006)
  10. Kobayashi, E, "Calphostins (UCN- 1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physic-chemical properties and biological activities", J. Antibiot, 42, pp.1470~1474 (1989)
  11. Kazanietz, M. G, "Characterization of the cysteine-rich region of the Caenorhabditis elegans protein Unc-13 as a high affinity phorbol ester receptor. Analysis of ligandbinding interactions, lipid cofactor requirements, and inhibitor sensitivity", J. Biol. Chem, 270, pp.10777~10783 (1995)
  12. Bruns, R. F, "Inhibition of protein kinase C by calphostin C is light-dependent", Biochem. Biophys. Res. Commun, 176, pp.288~293 (1991)
  13. Churchill, E. N, "Rationally designed peptide regulators of protein kinase C", Trends Endocrinol. Metab, 20, pp.25~33 (2009)
  14. Herbert, J. M, "chelerythrine is a potent and specific inhibitor of protein kinase C", Biochem. Biophys. Res. Commun, 172, pp.993~999 (1990)
  15. Eckly-Michel, A. E, "Chelerythrine, a protein kinase C inhibitor, interacts with cyclic nucleotide phosphodiesterases", Eur. J. Pharmacol, 324, pp.85~88 (1997)
  16. Zamora, M. A, "BQ123, and ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human artery smooth muscle cells", Am. J. Respir. Cell Mol. Biol, 9, pp.429~433 (1993)
  17. Newton, A. C, "Regulation of protein kinase C", Curr. Opin. Cell Biol, 9, pp.161~167 (1997)
  18. Shimoda, L. A, "Inhibition of voltage-gated K+ current in rat intrapulmonary arterial myocytes by endothelin-1", Am. J. Physiol, 274, pp.842~853 (1998)
  19. Li, P. F, "Requirement for protein kinase C in reactive oxygen species-induced apoptosis of vascular smooth muscle cells", Circulation, 100, pp.967~973 (1999)
  20. Inoue, Y, "Endothelin augments unitary calcium channel currents on the smooth muscle cell membrane of guinea-pig portal vein", J. Physiol, 423, pp.171~191 (1990)
  21. Van Renterghem, C, "Endothelin and vasopressin activate low conductance chloride channels in aortic smooth muscle cells", Pflugers. Arch, 425, pp.156~163 (1993)
  22. Nakajima, T, "Endothelin-1 and vasopressin activate Ca2+-permeable non-selective cation channels in aortic smooth muscle cells: mechanism of receptor-mediated Ca2+ influx", J. Mol. Cell Cardiol, 28, pp.707~722 (1996)
  23. Park, W. S, "Endothelin-1 acts via protein kinase C to block KATP channels in rabbit coronary and pulmonary arterial smooth muscle cells", J. Cardiovasc. Pharmacol, 45, pp.99~108 (2005)
  24. Park, W. S, "Endothelin-1 inhibits inward rectifier K+ channels in rabbit coronary arterial smooth muscle cells through protein kinase C", JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 46, pp.681~689 (2005), LIPPINCOTT WILLIAMS & WILKINS
  25. Park, W. S, "Staurosporine inhibits voltage-dependent K+ current through a PKC-independent mechanism in isolated coronary arterial smooth muscle cells", JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 45, pp.260~269 (2005), LIPPINCOTT WILLIAMS & WILKINS
  26. French, R. J, "Blockage of squid axon potassium conductance by internal tetra-N-alkylammonium ions of various sizes", Biophys. J, 34, pp.271~291 (1981)
  27. Hoshi, T, "Biophysical and molecular mechanisms of Shaker potassium channel inactivation", Science, 250, pp.533~538 (1990)
  28. Heginbotham, L, "The aromatic binding site for tetraethylammonium ion on potassium channels", Neuron, 8, pp.483~491 (1992)
  29. Snyders, D. J, "Determinants of antiarrhythmic drug action. Electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel", Circ. Res, 77, pp.575~583 (1995)
  30. del Camino, D, "Camino, D., Holmgren, M., Liu, Y. and Yellen, G. (2000) Blocker protection in the pore of a voltage-gated K+ channel and its structural implications", Nature, 403, pp.321~325 (2000)
  31. Kageyama, M, "Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries", J. Pharmacol. Exp. Ther, 259, pp.1019~1026 (1991)
  32. Ko, J. H, "The protein kinase inhibitor, staurosporine, inhibits L-type Ca2+ current in rabbit atrial myocytes", Biochem. Biophys. Res. Commun, 329, pp.531~537 (2005)
  33. Ko, J. H, "Slowing of the inactivation of voltage-dependent sodium channels by staurosporine, the protein kinase C inhibitor, in rabbit atrial myocytes", EUROPEAN JOURNAL OF PHARMACOLOGY, 534, pp.48~54 (2006), ELSEVIER SCIENCE BV
  34. Narahashi, T, "Neuronal ion channels as the target sites of insecticides", Pharmacol. Toxico, 79, pp.1~14 (1996)
  35. Catterall, W. A, "From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels", Neuron, 26, pp.13~25 (2000)
  36. Goldin, A. L, "Resurgence of sodium channel research", Annu. Rev. Physiol, 63, pp.871~894 (2001)
  37. Lo, C. F, "Protein kinase-independent inhibition of muscarinic K+ channels by staurosporine", Am. J. Physiol, 266, pp.1128~1132 (1994)
  38. 최진성, "Staurosporine directly blocks Kv1.3 channels expressed in Chinese hamster ovary cells", NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 359, pp.256~261 (1999), SPRINGER
  39. Valenzuela, C, "Class III antiarrhythmic effects of zatebradine. Time-, state-, use-, and voltage-dependent block of hKv1.5 channels", Circulation, 94, pp.562~570 (1996)
  40. Park, W. S, "The protein kinase C inhibitor, bisindolylmaleimide (I), inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells", LIFE SCIENCES, 77, pp.512~527 (2005), PERGAMON-ELSEVIER SCIENCE LTD
  41. Kim, A, "Direct block by bisindolylmaleimide of the voltage-dependent K+ currents of rat mesenteric arterial smooth muscle", Eur. J. Pharmacol, 483, pp.117~126 (2004)
  42. Voutilainen-Mylylä, S, "Chelerythrine and bisindolylmaleimide I prolong cardiac action potentials by protein kinase C-independent mechanism", Eur. J. Pharmacol, 466, pp.41~51 (2003)
  43. Cho, H, "Inhibition of acetylcholine-activated K+ current by chelerythrine and bisindolylmaleimide I in atrial myocytes from mice", Eur. J. Pharmacol, 424, pp.173~178 (2001)
  44. 박원선, "A Carbohydrate Fraction, AIP1, from Artemisia Iwayomogi Reduces the Action Potential Duration by Activation of Rapidly Activating Delayed Rectifier K＋ Channels in Rabbit Ventricular Myocytes", The Korean Journal of Physiology & Pharmacology, 14(3), pp.119~125 (2010), 대한약리학회
  45. Thomas, D, "Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X)", Cardiovasc. Res, 64, pp.467~476 (2004)
  46. Ficker, E, "Mechanisms of arsenic-induced prolongation of cardiac repolarization", Mol. Pharmacol, 66, pp.33~44 (2004)
  47. 최진성, "Direct block by bisindolylmaleimide of rat Kv1.5 expressed in Chinese hamster ovary cells", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 293, pp.634~640 (2000), AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
  48. Lingameneni, R, "Inhibition of voltage-dependent sodium channels by Ro 31-8220, a ‘specific’ protein kinase C inhibitor", FEBS Lett, 473, pp.265~268 (2000)
  49. Shi, L, "Inhibitory effect of the kinase inhibitor chelerythrine on acetylcholine-induced current in PC12 cells", Arch. Biochem. Biophys, 368, pp.40~44 (1999)
  50. Murphy, C. T, "Selective inhibition of protein kinase C. Effect on platelet-activating- factor-induced platelet functional responses", Biochem. J, 283, pp.159~164 (1992)
  51. Keenan, C, "Isoform specificity of activators and inhibitors of protein kinase C gamma and delta", FEBS Lett, 415, pp.101~108 (1997)
  52. Zakharov, S. I, "Activation of the BK (SLO1) potassium channel by mallotoxin", J. Biol. Chem, 280, pp.30882~30887 (2005)
  53. Wu, S. N, "Potent stimulation of large-conductance Ca2+-activated K+ channels by rottlerin, an inhibitor of protein kinase C-delta, in pituitary tumor (GH3) cells and in cortical neuronal (HCN-1A) cells", J. Cell Physiol, 210, pp.656~666 (2007)
  54. Butler, A, "mSlo, a complex mouse gene encoding “maxi” calcium-activated potassium channels", Science, 261, pp.221~224 (1993)
  55. Ghatta, S, "Large-conductance, calcium-activated potassium channels: Structural and functional implications", Pharmacol. Ther, 110, pp.103~116 (2006)

관련 논문AI추천

Ca²+-regulated ion channelsDaniel H. Cox생화학분자생물학회 · BMB Reports2011 · 제44권 제10호PKC inhibitors RO 31-8220 and Gö 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation윤혜숙, Doyeun Oh, Eek-hoon Jho, Jeong Mi Kim, Seonyang Park, Sewoon Kim, Sun Young Kim생화학분자생물학회 · BMB Reports2011 · 제44권 제2호Physiological functions of the TRPM4 channels via protein interactions김은주, 박재용, 이영선, 조장훈, 황은미생화학분자생물학회 · BMB Reports2015 · 제48권 제1호Vasodilation of BCT is Associated with Inhibition of PKCα Translocation and LC20 Phosphorylation신흥묵, DongHoonShin, GilWhonKim, OhKuiKwon한의병리학회 · 동의생리병리학회지2003 · 제17권 제5호Canonical Transient Receptor Potential Channels and Vascular Smooth Muscle Cell PlasticityAkiyuki Nishimura, Kazuhiro Nishiyama, Motohiro Nishida, Supachoke Mangmool, Tomohiro Tanaka한국지질동맥경화학회 · 지질·동맥경화학회지2020 · 제9권 제1호Bupivacaine-induced Vasodilation Is Mediated by Decreased Calcium Sensitization in Isolated Endothelium-denuded Rat Aortas Precontracted with Phenylephrine권성춘, 김우찬, 박경은, 박정철, 배성일, 손주태, 신일우, 옥성호, 이헌근, 정영균, 최문정대한통증학회 · The Korean Journal of Pain2014 · 제27권 제3호

이 간행물의 다른 논문 (8건)

Altered PLCβ-1 expression in the gerbil hippocampal complex following spontaneous seizureYun-Jung Oh, 김덕수, 박경호, 박대균, 고정식, Ji-Heon Jeong, Saet-Byeol Lee, Jae-Kwang Chung, Sang-Duk Leepp. 566-571The C-terminal domain of PLD2 participates in degradation of protein kinase CKII β subunit in human colorectal carcinoma cellsJi-Young Kang, 김은경, 윤수현, Young-Seuk Bae, Young-Hoon Lee, Jong-Su Uhm, Beom Sik Kang, 민도식pp. 572-577A replication study of genome-wide CNV association for hepatic biomarkers identifies nine genes associated with liver functionMi-Jeong Byun, Hyo-Young Kim, 김희발pp. 578-583Phosphorylation of SAV1 by mammalian ste20-like kinase promotes cell death이용희, 박병희pp. 584-589Production of methionine γ- lyase in recombinant Citrobacter freundii bearing the hemoglobin geneHüseyin Kahraman, Emel Aytan, Aslı Giray Kurtpp. 590-594
원문 보기