Cysteine-independent inhibition of the CFTR chloride channel by the cysteine-reactive reagent sodium (2-sulphonatoethyl) methanethiosulphonate

British Journal of Pharmacology

Volumn 157, Issue 6, 2009, Pages 1065-1071

  Li, M S ^a   Demsey, A F A ^a   Qi, J ^a   Linsdell, P ^a  

^a DALHOUSIE UNIVERSITY   (Canada)

Author keywords

Chloride channel; Cysteine reactive reagents; Cystic fibrosis transmembrane conductance regulator; Methanethiosulphonate; MTSES; MTSET; Open channel block; Patch clamp; Substituted cysteine accessibility mutagenesis

Indexed keywords

(2 SULFONATOETHYL)METHANETHIOSULFONIC ACID; CHLORIDE CHANNEL BLOCKING AGENT; CYSTEINE; MESYLIC ACID DERIVATIVE; TRANSMEMBRANE CONDUCTANCE REGULATOR; UNCLASSIFIED DRUG;

AMPLITUDE MODULATION; ANIMAL CELL; ARTICLE; CHANNEL GATING; CHLORIDE CURRENT; CONCENTRATION RESPONSE; CONTROLLED STUDY; COVALENT BOND; DRUG MECHANISM; ELECTRIC POTENTIAL; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN MODIFICATION;

ANIMALS; CELL LINE; CRICETINAE; CYSTEINE; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; HUMANS; MESYLATES; SULFHYDRYL REAGENTS;

EID: 70350336877     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2009.00258.x     Document Type: Article

References (39)

1. Akabas MH (1998). Channel-lining residues in the M3 membrane-spanning segment of the cystic fibrosis transmembrane conductance regulator. Biochemistry 37: 12233-12240.
2. Akabas MH, Kaufmann C, Cook TA, Archdeacon P (1994). Amino acid residues lining the chloride channel of the cystic fibrosis transmem-brane conductance regulator. J Biol Chem 269: 14865-14868.
3. Alexander SPH, Mathie A, Peters JA (2008). Guide to Receptors and Channels (GRAC), 3rd edn (2008 revision). Br J Pharmacol 153 (Suppl. 2): S1-S209.
4. Beck EJ, Yang Y, Yaemsiri S, Raghuram V (2008). Conformational changes in a pore-lining helix coupled to CFTR channel gating. J Biol Chem 283: 4957-4966.
5. Cai Z, Scott-Ward TS, Li H, Schmidt A, Sheppard DN (2004). Strategies to investigate the mechanism of action of CFTR modulators. J Cyst Fibros 3 (Suppl. 2): 141-147.
6. Cheung M, Akabas MH (1996). Identification of cystic fibrosis trans-membrane conductance regulator channel-lining residues in and flanking the M6 membrane-spanning segment. Biophys J 70: 2688-2695.
7. Cui L, Aleksandrov L, Hou Y-X, Gentzsch M, Chen J-H, Riordan JR et al. (2006). The role of cystic fibrosis transmembrane conductance regulator phenylalanine 508 side chain in ion channel gating. J Physiol 572: 347-358.
8. Fatehi M, Linsdell P (2008). State-dependent access of anions to the cystic fibrosis transmembrane conductance regulator chloride channel pore. J Biol Chem 283: 6102-6109.
9. Fatehi M, St. Aubin CN, Linsdell P (2007). On the origin of asymmetric interactions between permeant anions and the CFTR chloride channel pore. Biophys J 92: 1241-1253.
10. Fu J, Kirk KL (2001). Cysteine substitutions reveal dual functions of the amino-terminal tail in cystic fibrosis transmembrane conductance regulator channel gating. J Biol Chem 276: 35660-35668.
11. Gadsby DC, Vergani P, Csanády L (2006). The ABC protein turned chloride channel whose failure causes cystic fibrosis. Nature 440: 477-483.
12. Ge N, Linsdell P (2006). Interactions between impermeant blocking ions in the CFTR chloride channel pore. Evidence for anion-induced conformational changes. J Membr Biol 210: 31-42.
13. Ge N, Muise CN, Gong X, Linsdell P (2004). Direct comparison of the functional roles played by different transmembrane regions in the cystic fibrosis transmembrane conductance regulator chloride channel pore. J Biol Chem 279: 55283-55289.
14. Gong X, Burbridge SM, Cowley EA, Linsdell P (2002). Molecular determinants of Au(CN)2-binding and permeability within the cystic fibrosis transmembrane conductance regulator Cl-channel pore. J Physiol 540: 39-47. (Pubitemid 35174985)
15. Gong X, Linsdell P (2003). Mutation-induced blocker permeability and multiion block of the CFTR chloride channel pore. J Gen Physiol 122: 673-687.
16. Hartzell C, Putzier I, Arreola J (2005). Calcium-activated chloride channels. Annu Rev Physiol 67: 719-758.
17. Hwang T-C, Sheppard DN (1999). Molecular pharmacology of the CFTR Cl-channel. Trends Pharmacol Sci 20: 448-453.
18. Jentsch TJ, Stein V, Weinreich F, Zdebik AA (2002). Molecular structure and physiological function of chloride channels. Physiol Rev 82: 503-568.
19. Karlin A, Akabas MH (1998). Substituted-cysteine accessibility method. Meths Enzymol 293: 23-144.
20. Linsdell P (2001). Direct block of the cystic fibrosis transmembrane conductance regulator Cl-channel by butyrate and phenylbutyrate. Eur J Pharmacol 411: 255-260. (Pubitemid 32119594)
21. Linsdell P (2005). Location of a common inhibitor binding site in the cytoplasmic vestibule of the cystic fibrosis transmembrane conductance regulator chloride channel pore. J Biol Chem 280: 8945-8950.
22. Linsdell P (2006). Mechanism of chloride permeation in the cystic fibrosis transmembrane conductance regulator chloride channel. Exp Physiol 91: 123-129.
23. Linsdell P, Gong X (2002). Multiple inhibitory effects of Au(CN)2-ions on cystic fibrosis transmembrane conductance regulator Cl-channel currents. J Physiol 540: 29-38.
24. Linsdell P, Hanrahan JW (1996a). Disulphonic stilbene block of cystic fibrosis transmembrane conductance regulator Cl-channels expressed in a mammalian cell line and its regulation by a critical pore residue. J Physiol 496: 687-693.
25. Linsdell P, Hanrahan JW (1996b). Flickery block of single CFTR chloride channels by intracellular anions and osmolytes. Am J Physiol 271: C628-C634.
26. Linsdell P, Hanrahan JW (1998). Adenosine triphosphate-dependent asymmetry of anion permeation in the cystic fibrosis transmem-brane conductance regulator chloride channel. J Gen Physiol 111: 601-614.
27. Linsdell P, Hanrahan JW (1999). Substrates of multidrug resistance-associated proteins block the cystic fibrosis transmembrane conductance regulator chloride channel. Br J Pharmacol 126: 1471-1477.
28. Liu X, Zhang Z-R, Fuller MD, Billingsley J, McCarty NA, Dawson DC (2004). CFTR: a cysteine at position 338 in TM6 senses a positive electrostatic potential in the pore. Biophys J 87: 3826-3841.
29. Mense M, Vergani P, White DM, Altberg G, Nairn AC, Gadsby DC (2006). In vivo phosphorylation of CFTR promotes formation of a nucleotide-binding domain heterodimer. EMBO J 25: 4728-4739.
30. Scott-Ward TS, Li H, Schmidt A, Cai Z, Sheppard DN (2004). Direct block of the cystic fibrosis transmembrane conductance regulator Cl-channel by niflumic acid. Mol Membr Biol 21: 27-38.
31. Smith SS, Liu X, Zhang Z-R, Sun F, Kriewall TE, McCarty NA et al. (2001). CFTR: covalent and noncovalent modification suggests a role for fixed charges in anion conduction. J Gen Physiol 118: 407-431.
32. St. Aubin CN, Linsdell P (2006). Positive charges at the intracellular mouth of the pore regulate anion conduction in the CFTR chloride channel. J Gen Physiol 128: 535-545.
33. St. Aubin CN, Zhou J-J, Linsdell P (2007). Identification of a second blocker binding site at the cytoplasmic mouth of the cystic fibrosis transmembrane conductance regulator chloride channel pore. Mol Pharmacol 71: 1360-1368. (Pubitemid 46658689)
34. Venglarik CJ, Schultz BD, DeRoos ADG, Singh AK, Bridges RJ (1996). Tolbutamide causes open channel blockade of cystic fibrosis: transmembrane conductance regulator Cl-channels. Biophys J 70: 2696-2703.
35. Wang Y, Loo TW, Bartlett MC, Clarke DM (2007). Correctors promote maturation of cystic fibrosis transmembrane conductance regulator (CFTR)-processing mutants by binding to the protein. J Biol Chem 282: 33247-33251.
36. Woodhull AM (1973). Ionic blockage of sodium channels in nerve. J Gen Physiol 61: 687-708.
37. Zhang Z-R, Song B, McCarty NA (2005). State-dependent chemical reactivity of an engineered cysteine reveals conformational changes in the outer vestibule of the cystic fibrosis transmembrane conductance regulator. J Biol Chem 280: 41997-42003.
38. Zhou J-J, Fatehi M, Linsdell P (2007). Direct and indirect effects of mutations at the outer mouth of the cystic fibrosis transmembrane conductance regulator chloride channel pore. J Membr Biol 216: 129-142. (Pubitemid 47479556)
39. Zhu Q, Casey JR (2007). Topology of transmembrane proteins by scanning cysteine accessibility mutagenesis methodology. Methods 41: 439-450.