Mechanism of lonidamine inhibition of the CFTR chloride channel

British Journal of Pharmacology

Volumn 137, Issue 6, 2002, Pages 928-936

  Gong, Xiandi ^a   Burbridge, Susan M ^a   Lewis, Angie C ^a   Wong, Patrick Y D ^b   Linsdell, Paul ^a  

^a DALHOUSIE UNIVERSITY   (Canada)

^b CHINESE UNIVERSITY OF HONG KONG   (Hong Kong)

Author keywords

Binding site; CFTR; Chloride channel; Indazole; Open channel block; Spectral analysis

Indexed keywords

CHLORIDE CHANNEL; CHLORIDE CHANNEL BLOCKING AGENT; INDAZOLE DERIVATIVE; LONIDAMINE; TRANSMEMBRANE CONDUCTANCE REGULATOR;

ANIMAL CELL; ARTICLE; BINDING SITE; CHANNEL GATING; DRUG MECHANISM; MAMMAL CELL; NONHUMAN; PATCH CLAMP; POINT MUTATION; PRIORITY JOURNAL; SPECTROSCOPY;

ANIMALS; BINDING SITES; CHO CELLS; CRICETINAE; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; INDAZOLES; KINETICS; MEMBRANE POTENTIALS; MUTATION; TRANSFECTION;

EID: 0036856159     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0704932     Document Type: Article

References (40)

1. - channels by non-sulphonylurea hypoglycaemic agents. Brit. J. Pharmacol., 128, 108-118.
2. Dawson, D.C., Smith, S.S. & Mansoura, M.K. (1999). CFTR: Mechanism of anion conduction. Physiol. Rev., 79, S47-S75.
3. Fischer, H. & Machen, T.E. (1994). CFTR displays voltage dependence and two gating modes during stimulation. J. Gen. Physiol., 104, 541-566.
4. Floridi, A., Bruno, T., Miccadei, S., Fanciulli, M., Federico, A. & Paggi, M.G. (1998). Enhancement of doxorubicin content by the antitumor drug lonidamine in resistant Ehrlich ascites tumor cells through modulation of energy metabolism. Biochem. Pharmacol., 56, 841-849.
5. - channel pore. J. Physiol., 540, 39-47.
6. Gong, X.D., Leung, G.P., Cheuk, B.L. & Wong, P.Y. (2000a). Interference with the formation of the epididymal microenvironment - A new strategy for male contraception? Asian J. Androl., 2, 39-45.
7. Gong, X. & Linsdell, P. (2002). Mechanism and molecular basis of lonidamine block of the human CFTR chloride channel. Biophys. J., 82 (abstract), 239a.
8. Gong, X.D. & Wong, P.Y.D. (2000). Characterization of lonidamine and AF2785 blockade of the cyclic AMP-activated chloride current in rat epididymal cells. J. Membr. Biol., 178, 225-233.
9. Gong, X.D., Wong, Y.L., Leung, G.P.H., Cheng, C.Y., Silvestrini, B. & Wong, P.Y.D. (2000b). Lonidamine and analogue AF2785 block the cyclic adenosine 3′,5′-monophosphate-activated chloride current and chloride secretion in the rat epididymis. Biol. Reprod., 63, 833-838.
10. Gupta, J. & Linsdell, P. (2002). Point mutations in the pore region directly or indirectly affect glibenclamide block of the CFTR chloride channel. Pflügers Arch., 443, 739-747.
11. - channel. Trends Pharmacol. Sci., 20, 448-453.
12. Lindemann, B. & Van Driessche, W. (1977). Sodium-specific membrane channels of frog skin are pores: Current fluctuations reveal high turnover. Science, 195, 292-294.
13. - channel by butyrate and phenylbutyrate. Eur. J. Pharmacol., 411, 255-260.
14. Linsdell, P. (2001b). Relationship between anion binding and anion permeability revealed by mutagenesis within the cystic fibrosis transmembrane conductance regulator chloride channel pore. J. Physiol., 531, 51-66.
15. Linsdell, P., Evagelidis, A. & Hanrahan, J.W. (2000). Molecular determinants of anion selectivity in the cystic fibrosis transmembrane conductance regulator chloride channel pore. Biophys. J., 78, 2973-2982.
16. - channel currents. J. Physiol., 540, 29-38.
17. - channels expressed in a mammalian cell line and its regulation by a critical pore residue. J. Physiol., 496, 687-693.
18. Linsdell, P. & Hanrahan, J.W. (1998). Adenosine triphosphate-dependent asymmetry of anion permeation in the cystic fibrosis transmembrane conductance regulator chloride channel. J. Gen. Physiol., 111, 601-614.
19. Linsdell, P. & Hanrahan, J.W. (1999). Substrates of multidrug resistance-associated proteins block the cystic fibrosis transmembrane conductance regulator chloride channel. Brit. J. Pharmacol., 126, 1471-1477.
20. - channel expressed in mammalian cell lines. J. Physiol., 512, 1-16.
21. Mathews, C.J., Macleod, R.J., Zheng, S.-X., Hanrahan, J.W., Bennett, H.P.J. & Hamilton, J.R. (1999). Characterization of the inhibitory effect of boiled rice on intestinal chloride secretion in guinea pig crypt cells. Gastroenterology, 116, 1342-1347.
22. - channel by two closely related arylaminobenzoates. J. Gen. Physiol., 102, 1-23.
23. McDonough, S., Davidson, N., Lester, H.A. & McCarty, N.A. (1994). Novel pore-lining residues in CFTR that govern permeation and open-channel block. Neuron, 13, 623-634.
24. Nagel, G. (1999). Differential function of the two nucleotide binding domains on cystic fibrosis transmembrane conductance regulator. Biochim. Biophys. Acta, 1461, 263-274.
25. Schultz, B.D., Deroos, A.D.G., Venglarik, C.J., Singh, A.K., Frizzell, R.A. & Bridges, R.J. (1996). Glibenclamide blockade of CFTR chloride channels. Am. J. Physiol., 271, L192-L200.
26. Schultz, B.D., Singh, A.K., Devor, D.C. & Bridges, R.J. (1999). Pharmacology of CFTR chloride channel activity. Physiol. Rev., 79, S109-S144.
27. - channels expressed in a murine cell line. J. Physiol., 503, 333-346.
28. + channel regulators on cystic fibrosis transmembrane conductance regulator chloride currents. J. Gen. Physiol., 100, 573-591.
29. Sheppard, D.N. & Welsh, M.J. (1999). Structure and function of the CFTR chloride channel. Physiol. Rev., 79, S23-S45.
30. Smith, S.S., Liu, X., Zhang, Z.-R., Sun, F., Kriewall, T.E., McCarty, N.A. & Dawson, D.C. (2001). CFTR: Covalent and noncovalent modification suggests a role for fixed charges in anion conduction. J. Gen. Physiol., 118, 407-431.
31. Stanton, B.A. (1997). Cystic fibrosis transmembrane conductance regulator (CFTR) and renal function. Wien. Klin. Wochenschr., 109, 457-464.
32. Super, M. (2000). CFTR and disease: Implications for drug development. Lancet, 355, 1840-1842.
33. - channels. Biophys. J., 70, 2696-2703.
34. Venglarik, C.J., Schultz, B.D., Frizzell, R.A. & Bridges, R.J. (1994). ATP alters current fluctuations of cystic fibrosis transmembrane conductance regulator: Evidence for a three state activation mechanism. J. Gen. Physiol., 104, 123-146.
35. Walsh, K.B., Long, K.J. & Shen, X. (1999). Structural and ionic determinants of 5-nitro-2-(3-phenylpropyl-amino)-benzoic acid block of the CFTR chloride channel. Brit. J. Pharmacol., 127, 369-376.
36. Woodhull, A.M. (1973). Ionic blockage of sodium channels in nerve. J. Gen. Physiol., 61, 687-708.
37. Zeitlin, P.L. (2000). Future pharmacological treatment of cystic fibrosis. Respiration, 67, 351-357.
38. Zhang, Z.-R., Zeltwanger, S. & McCarty, N.A. (2000). Direct comparison of NPPB and DPC as probes of CFTR expressed in Xenopus oocytes. J. Membr. Biol., 175, 35-52.
39. Zhou, Z., Hu, S. & Hwang, T.-C. (2001). Voltage-dependent flickery block of an open cystic fibrosis transmembrane conductance regulator (CFTR) channel pore. J. Physiol., 532, 435-448.
40. Zou, X. & Hwang, T.-C. (2001). ATP hydrolysis-coupled gating of CFTR chloride channels: Structure and function. Biochemistry, 40, 5579-5585.