Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels

American Journal of Physiology - Cell Physiology

Volumn 270, Issue 5 39-5, 1996, Pages

  Hartzell, H Criss ^a   Rinderknecht, Amber ^a  

^a EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

adenosine 3',5' cyclic monophosphate; light; patch clamp; phosphorylation; photosensitivity

Indexed keywords

CALCIUM CHANNEL; CALPHOSTIN C; PROTEIN KINASE C;

ANIMAL CELL; ARTICLE; CALCIUM CURRENT; DRUG EFFECT; DRUG PROTEIN BINDING; ENZYME INHIBITION; FROG; NONHUMAN; PHOTOSENSITIVITY; PRIORITY JOURNAL;

ANIMALIA; ANURA;

EID: 0029977396     PISSN: 03636143     EISSN: None     Source Type: Journal    
DOI: 10.1152/ajpcell.1996.270.5.c1293     Document Type: Article

References (30)

1. Altschul, S. F., W. Gish, W. Miller, E. W. Myers, and D. J. Lipman. Basic local alignment search tool. J. Mol. Biol. 215: 403-410, 1990.
2. Argibay, J. A., R. Fischmeister, and H. C. Hartzell. Inactivation, reactivation and pacing dependence of calcium current in frog cardiocytes: correlation with current density. J. Physiol. Lond. 401: 201-226, 1988.
3. Bruns, R. F., F. D. Miller, R. L. Merriman, J. J. Howbert, W. F. Heath, E. Kobayashi, I. Takahashi, T. Tamaoki, and H. Nakano. Inhibition of protein kinase C by calphostin C is light-dependent. Biochem. Biophys. Res. Commun. 176: 288-293, 1991.
4. Divecha, N., and R. F. Irvine. Phospholipid signalling. Cell 80: 269-278, 1995.
5. Diwu, Z., and J. W. Lown. Photosensitization with anticancer agents 19. EPR studies of photodynamic action of calphostin C: formation of semiquinone radical and activated oxygen on illumination with visible light. Free Radical Biol. Med. 16: 645-652, 1994.
6. Dösemeci, A., R. S. Dhallan, N. M. Cohen, W. J. Lederer, and T. B. Rogers. Phorbol ester increases calcium current and simulates the effects of angiotensin on cultured neonatal rat heart myocytes. Circ. Res. 62: 347-357, 1988.
7. Fischmeister, R., and H. C. Hartzell. Mechanism of action of acetylcholine on calcium current in single cells from frog ventricle. J. Physiol. Lond. 376: 183-202, 1986.
8. Frace, A. M., and H. C. Hartzell. Opposite effects of phosphatase inhibitors on L-type calcium and delayed rectifier currents in frog cardiac myocytes. J. Physiol. Lond. 472: 305-326, 1993.
9. Gopalakrishna, R., Z. H. Chen, and U. Gundimeda. Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C. FEBS Lett. 314: 149-154, 1992.
10. Gordge, P. C., and W. J. Ryves. Inhibitors of protein kinase C. Cell. Signal. 6: 871-882, 1994.
11. Hartzell, H. C. Regulation of cardiac ion channels by catecholamines, acetylcholine and second messenger systems. Prog. Biophys. Mol. Biol. 52: 165-247, 1988.
12. Hartzell, H. C., and I. Duchatelle-Gourdon. Structure and neural modulation of cardiac calcium channels. J. Cardiovasc. Electrophysiol. 3: 567-578, 1992.
13. Hartzell, H. C., and R. Fischmeister. Effect of forskolin and acetylcholine on calcium current in single cells from frog ventricle. Mol. Pharmacol. 32: 639-645, 1987.
14. Hartzell, H. C., Y. Hirayama, and J. Petit-Jacques. Effects of protein phosphatase and kinase inhibitors on the cardiac L-type Ca current suggest two sites are phosphorylated by protein kinase A and another protein kinase. J. Gen. Physiol. 106: 393-414, 1995.
15. Hartzell, H. C., P.-F. Mery, R. Fischmeister, and G. Szabo. Sympathetic regulation of cardiac calcium current is due exclusively to cAMP-dependent phosphorylation. Nature Lond. 351: 573-576, 1991.
16. Honkanen, R., J. Zwiller, R. Moore, S. Daily, B. Khatra, M. Dukelow, and A. Boyton. Characterization of microcystin-LR, a potent inhibitor of type 1 and type 2A protein phosphatases. J. Biol. Chem. 265: 19401-19404, 1990.
17. House, C., and B. E. Kemp. Protein kinase C pseudosubstrate prototope: structure-function relationships. Cell. Signal. 2: 187-190, 1990.
18. Kobayashi, E., H. Nakano, M. Morimoto, and T. Tamaoki. Calphostin C (UNC-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. Biochem. Biophys. Res. Commun. 159: 548-553, 1989.
19. Lacerda, A. E., D. Rampe, and A. M. Brown. Effects of protein kinase C activators on cardiac Ca2+ channels. Nature Lond. 335: 249-251, 1988.
20. MacKintosh, C., K. A. Beattie, S. Klumpp, P. Cohen, and G. A. Codd. Cyanobacterial microcystin-LR is a potent and specific inhibitor of protein phosphatases 1 and 2A from both mammals and higher plants. FEBS Lett. 264: 187-192, 1990.
21. Nishizuka, Y. Protein kinase C and lipid signalling for sustained cellular responses. FASEB J. 9: 484-496, 1995.
22. Rinehart, K. L., K.-I. Harada, M. Namikoshi, C. Chen, and C. A. Harvis. Nodularin, microcystin, and the configuration of Adda. J. Am. Chem. Soc. 110: 8559-8560, 1988.
23. Rotenberg, S.A., M. H. Huang, J. Zhu, L. Su, and H. Riedel. Deletion analysis of protein kinase C inactivation by calphostin C. Mol. Carcinog. 12: 42-49, 1995.
24. 2+ channels in Xenopus oocytes by protein kinase C. FEBS Lett. 306: 113-118, 1992.
25. Tamaoki, T., H. Nomoto, I. Takahashi, Y. Kato, M. Morimoto, and F. Tomita. Staurosporine, a potent inhibitor or phospholipid/Ca dependent protein kinase. Biochem. Biophys. Res. Commun. 135: 397-402, 1986.
26. Tamaoki, T., I. Takahashi, E. Kobayashi, H. Nakano, S. Akinaga, and K. Suzuki. Calphostin (UCN1028) and calphostin related compounds, a new class of specific and potent inhibitors of protein kinase C. Adv. Second Messenger Phosphoprotein Res. 24: 497-501, 1990.
27. Trautwein, W., and J. Hescheler. Regulation of cardiac L-type calcium current by phosphorylation and G proteins. Annu. Rev. Physiol. 52: 257-274, 1990.
28. Tsien, R. W., B. P. Bean, P. Hess, J. B. Lansman, B. Nilius, and M. Nowycky. Mechanism of calcium channel modulation by β-adrenergic agents and dihydropyridine calcium channel agonists. J. Mol. Cell. Cardiol. 18: 691-710, 1986.
29. Walsh, K. B., T. B. Begenisich, and R. S. Kass. β-Adrenergic modulation of cardiac ion channels. J. Gen. Physiol. 93: 841-854, 1989.
30. Wang, S. S., C. Mathes, and S. H. Thompson. Membrane toxicity of the protein kinase C inhibitor calphostin A by a free-radical mechanism. Neurosci. Lett. 156: 145-148, 1993.