Revisiting CFTR inhibition: A comparative study of CFTRinh-172 and GlyH-101 inhibitors

British Journal of Pharmacology

Volumn 171, Issue 15, 2014, Pages 3716-3727

  Melis, N ^a   Tauc, M ^a   Cougnon, M ^a   Bendahhou, S ^a   Giuliano, S ^a   Rubera, I ^a   Duranton, C ^a  

^a UNIVERSITÉ CÔTE D'AZUR   (France)

Author keywords

CaCC; CFTR; chloride channel; chloride conductance; cystic fibrosis; inhibitors; patch clamp; VSORC; whole cell

Indexed keywords

3 [(3 TRIFLUOROMETHYL)PHENYL] 5 [(4 CARBOXYPHENYL)METHYLENE] 2 THIOXO 4 THIAZOLIDINONE; CHLORIDE CHANNEL BLOCKING AGENT; N (2 NAPHTHALENYL) ((3,5 DIBROMO 2,4 DIHYDROXYPHENYL)METHYLENE)GLYCINE HYDRAZIDE; UNCLASSIFIED DRUG; 3-((3-TRIFLUOROMETHYL)PHENYL)-5-((3-CARBOXYPHENYL)METHYLENE)-2-THIOXO-4-THIAZOLIDINONE; BENZOIC ACID DERIVATIVE; CHLORIDE; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; GLYCINE; HYDRAZINE DERIVATIVE; N-(2-NAPHTHALENYL)-((3,5-DIBROMO-2,4-DIHYDROXYPHENYL)METHYLENE)GLYCINE HYDRAZIDE; THIAZOLIDINE DERIVATIVE;

ANIMAL CELL; ARTICLE; CALCIUM ACTIVATED CHLORIDE CONDUCTANCE; CELL PROLIFERATION ASSAY; CELL VIABILITY; CHLORIDE CURRENT; COMPARATIVE STUDY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY; DRUG EFFICACY; DRUG INHIBITION; DRUG POTENCY; DRUG SPECIFICITY; IMMORTALIZED CELL LINE; MOUSE; NONHUMAN; PATCH CLAMP TECHNIQUE; PRIORITY JOURNAL; VOLUME SENSITIVE OUTWARDLY RECTIFYING CHLORIDE CONDUCTANCE; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; CELL SURVIVAL; DRUG EFFECTS; HAMSTER; PHYSIOLOGY;

ANIMALS; BENZOATES; CELL LINE; CELL SURVIVAL; CHLORIDES; CRICETINAE; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; GLYCINE; HYDRAZINES; MICE; THIAZOLIDINES;

EID: 84904551001     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.12726     Document Type: Article

References (41)

1. Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Catterall WA, etal. (2013). The Concise Guide to PHARMACOLOGY 2013/14: Ion Channels. Br J Pharmacol 170: 1607-1651.
2. - channels by CFTR is mediated by the second nucleotide-binding domain. Pflugers Arch 445: 177-186.
3. Baniak N, Luan X, Grunow A, Machen TE, Ianowski JP, (2012). The cytokines interleukin-1beta and tumor necrosis factor-alpha stimulate CFTR-mediated fluid secretion by swine airway submucosal glands. Am J Physiol Lung Cell Mol Physiol 303: L327-L333.
4. Barman PP, Choisy SC, Gadeberg HC, Hancox JC, James AF, (2011). Cardiac ion channel current modulation by the CFTR inhibitor GlyH-101. Biochem Biophys Res Commun 408: 12-17.
5. Barriere H, Poujeol C, Tauc M, Blasi JM, Counillon L, Poujeol P, (2001). CFTR modulates programmed cell death by decreasing intracellular pH in Chinese hamster lung fibroblasts. Am J Physiol Cell Physiol 281: C810-C824.
6. - currents in primary cultures of mouse nephron. Am J Physiol Renal Physiol 284: F796-F811.
7. - secretion by lubiprostone requires the cystic fibrosis transmembrane conductance regulator. Gastroenterology 137: 976-985.
8. Billet A, Hanrahan JW, (2013). The secret life of CFTR as a calcium-activated chloride channel. J Physiol 591 (Pt 21): 5273-5278.
9. Caci E, Caputo A, Hinzpeter A, Arous N, Fanen P, Sonawane N, etal. (2008). Evidence for direct CFTR inhibition by CFTR(inh)-172 based on Arg347 mutagenesis. Biochem J 413: 135-142.
10. Caputo A, Caci E, Ferrera L, Pedemonte N, Barsanti C, Sondo E, etal. (2008). TMEM16A, a membrane protein associated with calcium-dependent chloride channel activity. Science 322: 590-594.
11. Champigny G, Verrier B, Gerard C, Mauchamp J, Lazdunski M, (1990). Small conductance chloride channels in the apical membrane of thyroid cells. FEBS Lett 259: 263-268.
12. Di Stefano A, Wittner M, Schlatter E, Lang HJ, Englert H, Greger R, (1985). Diphenylamine-2-carboxylate, a blocker of the Cl(-)-conductive pathway in Cl(-)-transporting epithelia. Pflugers Arch 405 (Suppl. 1): S95-S100.
13. Drumm ML, Pope HA, Cliff WH, Rommens JM, Marvin SA, Tsui LC, etal. (1990). Correction of the cystic fibrosis defect in vitro by retrovirus-mediated gene transfer. Cell 62: 1227-1233.
14. Duranton C, Huber SM, Lang F, (2002). Oxidation induces a Cl(-)-dependent cation conductance in human red blood cells. J Physiol 539 (Pt 3): 847-855.
15. Fisher JT, Tyler SR, Zhang Y, Lee BJ, Liu X, Sun X, etal. (2013). Bioelectric characterization of epithelia from neonatal CFTR knockout ferrets. Am J Respir Cell Mol Biol 49: 837-844.
16. Furukawa T, Ogura T, Katayama Y, Hiraoka M, (1998). Characteristics of rabbit ClC-2 current expressed in Xenopus oocytes and its contribution to volume regulation. Am J Physiol 274 (2 Pt 1): C500-C512.
17. Gray MA, Greenwell JR, Argent BE, (1988). Secretin-regulated chloride channel on the apical plasma membrane of pancreatic duct cells. J Membr Biol 105: 131-142.
18. - channel. Trends Pharmacol Sci 20: 448-453.
19. - secretion and innate immune responses in airway epithelia: role for p38. Am J Physiol Lung Cell Mol Physiol 295: L531-L542.
20. Julien M, Verrier B, Cerutti M, Chappe V, Gola M, Devauchelle G, etal. (1999). Cystic fibrosis transmembrane conductance regulator (CFTR) confers glibenclamide sensitivity to outwardly rectifying chloride channel (ORCC) in Hi-5 insect cells. J Membr Biol 168: 229-239.
21. Kelly M, Trudel S, Brouillard F, Bouillaud F, Colas J, Nguyen-Khoa T, etal. (2010). Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther 333: 60-69.
22. l'Hoste S, Chargui A, Belfodil R, Corcelle E, Duranton C, Rubera I, etal. (2010). CFTR mediates apoptotic volume decrease and cell death by controlling glutathione efflux and ROS production in cultured mice proximal tubules. Am J Physiol Renal Physiol 298: F435-F453.
23. L'Hoste S, Chargui A, Belfodil R, Duranton C, Rubera I, Mograbi B, etal. (2009). CFTR mediates cadmium-induced apoptosis through modulation of ROS level in mouse proximal tubule cells. Free Radic Biol Med 46: 1017-1031.
24. Lu M, Ding C, (2012). CFTR-mediated Cl(-) transport in the acinar and duct cells of rabbit lacrimal gland. Curr Eye Res 37: 671-677.
25. Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, etal. (2002). Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest 110: 1651-1658.
26. Milosavljevic N, Duranton C, Djerbi N, Puech PH, Gounon P, Lagadic-Gossmann D, etal. (2010). Nongenomic effects of cisplatin: acute inhibition of mechanosensitive transporters and channels without actin remodeling. Cancer Res 70: 7514-7522.
27. Muanprasat C, Sonawane ND, Salinas D, Taddei A, Galietta LJ, Verkman AS, (2004). Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol 124: 125-137.
28. Muanprasat C, Wongborisuth C, Pathomthongtaweechai N, Satitsri S, Hongeng S, (2013). Protection against oxidative stress in beta thalassemia/hemoglobin E erythrocytes by inhibitors of glutathione efflux transporters. PLoS ONE 8: e55685.
29. Peyronnet R, Sharif-Naeini R, Folgering JH, Arhatte M, Jodar M, El Boustany C, etal. (2012). Mechanoprotection by polycystins against apoptosis is mediated through the opening of stretch-activated K(2P) channels. Cell Rep 1: 241-250.
30. Rich DP, Anderson MP, Gregory RJ, Cheng SH, Paul S, Jefferson DM, etal. (1990). Expression of cystic fibrosis transmembrane conductance regulator corrects defective chloride channel regulation in cystic fibrosis airway epithelial cells. Nature 347: 358-363.
31. Rubera I, Duranton C, Melis N, Cougnon M, Mograbi B, Tauc M, (2013). Role of CFTR in oxidative stress and suicidal death of renal cells during cisplatin-induced nephrotoxicity. Cell Death Dis 4: e817.
32. Sondo E, Tomati V, Caci E, Esposito AI, Pfeffer U, Pedemonte N, etal. (2011). Rescue of the mutant CFTR chloride channel by pharmacological correctors and low temperature analyzed by gene expression profiling. Am J Physiol Cell Physiol 301: C872-C885.
33. Stahl M, Stahl K, Brubacher MB, Forrest JN Jr, (2012). Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101. Am J Physiol Cell Physiol 302: C67-C76.
34. Tabcharani JA, Low W, Elie D, Hanrahan JW, (1990). Low-conductance chloride channel activated by cAMP in the epithelial cell line T84. FEBS Lett 270: 157-164.
35. Taddei A, Folli C, Zegarra-Moran O, Fanen P, Verkman AS, Galietta LJ, (2004). Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett 558: 52-56.
36. Thiagarajah JR, Broadbent T, Hsieh E, Verkman AS, (2004). Prevention of toxin-induced intestinal ion and fluid secretion by a small-molecule CFTR inhibitor. Gastroenterology 126: 511-519.
37. Vennekens R, Trouet D, Vankeerberghen A, Voets T, Cuppens H, Eggermont J, etal. (1999). Inhibition of volume-regulated anion channels by expression of the cystic fibrosis transmembrane conductance regulator. J Physiol 515 (Pt 1): 75-85.
38. Wang L, Ma W, Zhu L, Ye D, Li Y, Liu S, etal. (2012). ClC-3 is a candidate of the channel proteins mediating acid-activated chloride currents in nasopharyngeal carcinoma cells. Am J Physiol Cell Physiol 303: C14-C23.
39. Wangemann P, Wittner M, Di Stefano A, Englert HC, Lang HJ, Schlatter E, etal. (1986). Cl(-)-channel blockers in the thick ascending limb of the loop of Henle. Structure activity relationship. Pflugers Arch 407 (Suppl. 2): S128-S141.
40. Yang B, Sonawane ND, Zhao D, Somlo S, Verkman AS, (2008). Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease. J Am Soc Nephrol 19: 1300-1310.
41. Zhang WK, Wang D, Duan Y, Loy MM, Chan HC, Huang P, (2010). Mechanosensitive gating of CFTR. Nat Cell Biol 12: 507-512.