Suppression of insulin signalling by a synthetic peptide KIFMK suggests the cytoplasmic linker between DIII-S6 and DIV-S1 as a local anaesthetic binding site on the sodium channel

British Journal of Pharmacology

Volumn 142, Issue 1, 2004, Pages 222-228

  Hirose, Munetaka ^a   Kuroda, Yoshihiro ^b   Sawa, Shinichi ^b   Nakagawa, Terumichi ^b   Hirata, Masashi ^a   Sakaguchi, Masahiro ^a   Tanaka, Yoshifumi ^a  

^a KYOTO PREFECTURAL UNIVERSITY OF MEDICINE   (Japan)

^b KYOTO UNIVERSITY   (Japan)

Author keywords

Insulin receptor; KIFMK; Lidocaine; Lignocaine; Phosphorylation; Sodium channel; Tyrosine kinase

Indexed keywords

ACETYLLYSYLISOLEUCYLPHENYLALANYLMETHIONYLLYSINAMIDE; ASPARTYLISOLEUCYLTYROSYLGLUTAMYLTHREONINE; INSULIN; INSULIN RECEPTOR; LEUCYLPROLYLPHENYLALANYLPHENYLALANYLASPARTIC ACID; LIDOCAINE; LOCAL ANESTHETIC AGENT; LYSYLISOLEUCYLGLUTAMINYLMETHIONYLLYSINE; LYSYLISOLEUCYLTYROSYLGLUTAMYLLYSINE; PEPTIDE; RECEPTOR SUBUNIT; SODIUM CHANNEL; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; AUTOPHOSPHORYLATION; BINDING SITE; HORMONE INHIBITION; IN VITRO STUDY; INSULIN SYNTHESIS; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROTEIN DEPHOSPHORYLATION; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN PHOSPHORYLATION; PROTEIN PURIFICATION; PROTEIN STRUCTURE; RECEPTOR BINDING; SIGNAL TRANSDUCTION; WESTERN BLOTTING;

AMINO ACID SEQUENCE; ANESTHETICS, LOCAL; ANIMALS; BINDING SITES; CYTOPLASM; DOSE-RESPONSE RELATIONSHIP, DRUG; INSULIN; LIDOCAINE; MOLECULAR SEQUENCE DATA; OLIGOPEPTIDES; RATS; RECEPTOR, INSULIN; SIGNAL TRANSDUCTION; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS;

EID: 2142780003     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705575     Document Type: Article

References (37)

1. CANN, A.D. & KOHANSKI, R.A. (1997). Cis-autophosphorylation of juxtamembrane tyrosines in the insulin receptor kinase domain. Biochemistry, 36, 7681-7689.
2. CHERQUI, G., REYNET, C., CARON, M., MELIN, B., WICEK, D., CLAUSER, E., CAPEAU, J. & PICARD, J. (1990). Insulin receptor tyrosine residues 1162 and 1163 control insulin stimulation of myristoyl-diacylglycerol generation and subsequent activation of glucose transport. J. Biol. Chem., 265, 21254-21261.
3. +, and glucose in muscle, adipocytes and erythrocytes. Biochim. Biophys. Acta, 298, 393-411.
4. CUNNINGHAM, M.E., STEPHENS, R.M., KAPLAN, D.R. & GREENE, L.A. (1997). Autophosphorylation of activation loop tyrosines regulates signaling by the TRK nerve growth factor receptor. J. Biol. Chem., 272, 10957-10967.
5. DOUGHERTY, D.A. (1996). Cation-π interactions in chemistry and biology: a new view of benzene, Phe, Tyr, and Trp. Science, 271, 163-168.
6. EAHOLTZ, G., COLVIN, A., LEONARD, D., TAYLOR, C. & CATTERALL, W.A. (1999). Block of brain sodium channels by peptide mimetics of the isoleucine, phenylalanine, and methionine (IFM) motif from the inactivation gate. J. Gen. Physiol., 113, 279-293.
7. EAHOLTZ, G., SCHEUER, T. & CATTERALL, W.A. (1994). Restoration of inactivation and block of open sodium channels by an inactivation gate peptide. Neuron, 12, 1041-1048.
8. EBINA, Y., ELLIS, L., JARNAGIN, K., EDERY, M., GRAF, L., CLAUSER, E., OU, J.-H., MASIARZ, F., KAN, Y.W., GOLDFINE, I.D., ROTH, R.A. & RUTTER, W.J. (1985). The human insulin receptor cDNA: the structural basis for hormone-activated transmembrane signalling. Cell, 40, 747-758.
9. GEORGE, A.L., KOMISAROF, J., KALLEN, R.G. & BARCHI, R.L. (1992). Primary structure of the adult human skeletal muscle voltage-dependent sodium channel. Ann. Neurol., 31, 131-137.
10. HANKS, S.K., QUINN, A.M. & HUNTER, T. (1988). The protein kinase family: conserved features and deduced phylogeny of the catalytic domains. Science, 241, 42-52.
11. HIROSE, M., MARTYN, J.A.J., KURODA, Y., MARUNAKA, Y. & TANAKA, Y. (2002). Mechanism of suppression of insulin signalling with lignocaine. Br. J. Pharmacol., 136, 76-80.
12. HUBBARD, S.R. (1997). Crystal structures of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog. EMBO J., 16, 5573-5581.
13. HUNTER, C.A. & SANDERS, J.K.M. (1990). The nature of π-π interactions. J. Am. Chem. Soc., 112, 5525-5534.
14. KARNIEL, M. & BEITNER, R. (2000). Local anesthetics induce a decrease in the levels of glucose 1,6-bisphosphate, fructose 1,6-bisphosphate, and ATP, and in the viability of melanoma cells. Mol. Genet. Metab., 69, 40-45.
15. KOLACZYNSKI, J.W., MORALES, L.M., MOORE, J.R.J.H., CONSIDINE, R.V., PIETRZKOWSKI, Z., NOTO, P.F., COLBERG, J. & CARO, J.F. (1994). A new technique for biopsy of human abdominal fat under local anesthesia with lidocaine. Int. J. Obesity, 18, 161-166.
16. 1H-NMR and circular dichroism spectroscopic studies on changes in secondary structures of the sodium channel inactivation gate peptides as caused by the pentapeptide KIFMK. Biophys. J., 77, 1363-1373.
17. 1H-NMR spectroscopy. Chem. Pharm. Bull., 48, 1293-1298.
18. 1H-NMR spectroscopies. Biophys. J., 71, 1191-1207.
19. LEVITZKI, A. & GAZIT, A. (1995). Tyrosine kinase inhibition: an approach to drug development. Science, 267, 1782-1788.
20. MAEDA, Y., NAKAGAWA, T. & KURODA, Y. (2001). Helix-stabilizing effects of the pentapeptide KIFMK and its related peptides on the sodium channel inactivation gate peptides. J. Peptide Res., 58, 413-423.
21. MCPHEE, J.C., RAGSDALE, D.S., SCHEUER, T. & CATTERALL, W.A. (1995). A critical role for transmembrane segment IVS6 of the sodium channel α subunit in fast inactivation. J. Biol. Chem., 270, 12025-12034.
22. MORGAN, M.S., DARROW, R.M., NAFZ, M.A. & VARANDANI, P.T. (1985). Role of membranes and energy-producing reactions in cellular processing of insulin in primary cultures of rat hepatocytes. Biochem. Biophys. Res. Commun., 132, 749-756.
23. MURAKAMI, M.S. & ROSEN, O.M. (1991). The role of insulin receptor autophosphorylation in signal transduction. J. Biol. Chem., 266, 22653-22660.
24. + channels modulate binding affinity and stereoselectivity of local anesthetic enantiomers. Mol. Pharmacol., 56, 404-413.
25. NODA, M., IKEDA, T., KAYANO, T., SUZUKI, H., TAKESHIMA, H., KURASAKI, M., TAKAHASHI, H. & NUMA, S. (1986). Existence of distinct sodium channel messenger RNAs in rat brain. Nature, 320, 188-192.
26. NORDENBERG, J., KLEIN, S., BEERY, E., KAPLANSKY, M. & BEITNER, R. (1981). Changes in the levels of glucose 1,6-diphosphate and ATP and in the activities of phosphofructokinase and phosphoglucomutase induced by local anesthetics in the isolated rat diaphragm muscle. Int. J. Biochem., 13, 1005-1009.
27. OLSON, C.A., SHI, Z. & KALLENBACH, N.R. (2001). Polar interactions with aromatic side chains in α-helical peptides: CH⋯O H-bonding and cation-π interactions. J. Am. Chem. Soc., 123, 6451-6452.
28. 1H NMR and CD studies in alanine-lysine peptides. Biochemistry, 37, 17318-17330.
29. PÁRRIZAS, M., GAZIT, A., LEVITZKI, A., WERTHEIMER, E. & LEROITH, D. (1997). Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology, 138, 1427-1433.
30. POSNER, I., ENGEL, M., GAZIT, A. & LEVITZKI, A. (1994). Kinetics of inhibition by tyrphostins of the tyrosine kinase activity of the epidermal growth factor receptor and analysis by a new computer program. Mol. Pharmacol., 45, 673-683.
31. + channels by local anesthetics. Science, 265, 1724-1728.
32. STRICHARTZ, G.R. & RITCHIE, J.M. (1987). The action of local anesthetics on ion channels of excitable tissues. In: Local Anesthetics. ed. Strichartz, G.R. pp. 21-52. New York: Springer-Verlag.
33. + channel D2-S6 residues in batrachotoxin and local anesthetic action. Mol. Pharmacol., 59, 1100-1107.
34. + channel D3-S6 segment modulate both batrachotoxin and local anesthetic affinities. Biophys. J., 79, 1379-1387.
35. + channel D4-S6 reduce inactivated channel block by local anesthetics. Mol. Pharmacol., 54, 733-739.
36. + channel α subunit. J. Biol. Chem., 276, 20-27.
37. ZHANG, B., TAVARE, J.M., ELLIS, L. & ROTH, R.A. (1991). The regulatory role of known tyrosine autophosphorylation sites of the insulin receptor kinase domain. J. Biol. Chem., 266, 990-996.