Chloride channel-targeted therapy for secretory diarrheas

Current Opinion in Pharmacology

Volumn 13, Issue 6, 2013, Pages 888-894

  Thiagarajah, Jay R ^a,b   Verkman, A S ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b BOSTON CHILDREN S HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM ACTIVATED CHLORIDE CHANNEL; CALCIUM ACTIVATED CHLORIDE CHANNEL INHIBITOR; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR INHIBIOR; GLYCINE HYDRAZIDE 101; ION TRANSPORT AFFECTING AGENT; PROTEIN INHIBITOR; STOMACH SECRETION INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CYSTIC FIBROSIS; DIARRHEA; DRUG EFFICACY; DRUG MECHANISM; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; HUMAN; INTESTINE ABSORPTION; INTESTINE EPITHELIUM; KIDNEY POLYCYSTIC DISEASE; MOLECULARLY TARGETED THERAPY; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN SECRETION; PROTEIN TARGETING; SECRETORY DIARRHEA; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

ANIMALS; CHLORIDE CHANNELS; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; DIARRHEA; ENTEROCYTES; HUMANS; INTESTINES;

EID: 84888204096     PISSN: 14714892     EISSN: 14714973     Source Type: Journal    
DOI: 10.1016/j.coph.2013.08.005     Document Type: Review

References (45)

1. C.L. Walker, I. Rudan, L. Liu, H. Nair, E. Theodoratou, Z.A. Bhutta, K.L. O'Brien, H. Campbell, and R.E. Black Global burden of childhood pneumonia and diarrhoea Lancet 381 2013 1405 1416
2. S.R. Moore, N.L. Lima, A.M. Soares, R.B. Oriá, R.C. Pinkerton, L.J. Barrett, R.L. Guerrant, and A.A. Lima Prolonged episodes of acute diarrhea reduce growth and increase risk of persistent diarrhea in children Gastroenterology 139 2010 1156 1164
3. D.C. Payne, J. Vinjé, P.G. Szilagyi, K.M. Edwards, M.A. Staat, G.A. Weinberg, C.B. Hall, J. Chappell, D.I. Bernstein, and A.T. Curns Norovirus and medically attended gastroenteritis in U.S. children N Engl J Med 368 2013 1121 1130
4. M.K. Munos, C.L. Walker, R.E. Black, J. Lipecka, M. Bali, A. Thomas, P. Fanen, and A. Edelman The effect of oral rehydration solution and recommended home fluids on diarrhoea mortality Int J Epidemiol 39 2010 i75 i87
5. R.D. MacArthur, and H.L. DuPont Etiology and pharmacologic management of noninfectious diarrhea in HIV-infected individuals in the highly active antiretroviral therapy era Clin Infect Dis 55 2012 860 867
6. + exchange regulatory factor 2-dependent process Gastroenterology 140 2011 560 571
7. - secretion across murine duodenum Gastroenterology 136 2009 893 901
8. L.R. Gawenis, C.L. Franklin, J.E. Simpson, B.A. Palmer, N.M. Walker, T.M. Wiggins, and L.L. Clarke cAMP inhibition of murine intestinal Na/H exchange requires CFTR-mediated cell shrinkage of villus epithelium Gastroenterology 125 2003 1148 1163 (Pubitemid 37193461)
9. R. Murtazina, O. Kovbasnjuk, T.E. Chen, N.C. Zachos, Y. Chen, H.S. Kocinsky, B.M. Hogema, U. Seidler, H.R. de Jonge, and M. Donowitz NHERF2 is necessary for basal activity, second messenger inhibition, and LPA stimulation of NHE3 in mouse distal ileum Am J Physiol Cell Physiol 301 2011 C126 C136
10. H. Teramae, T. Yoshikawa, R. Inoue, K. Ushida, K. Takebe, J. Nio-Kobayashi, and T. Iwanaga The cellular expression of SMCT2 and its comparison with other transporters for monocarboxylates in the mouse digestive tract Biomed Res 31 2010 239 249
11. J. Fritsch Distribution of ClC-2 chloride channel in rat and human epithelial tissues Am J Physiol Cell Physiol 282 2002 C805 C816
12. K. Yu, R. Lujan, A. Marmorstein, S. Gabriel, and H.C. Hartzell Bestrophin-2 mediates bicarbonate transport by goblet cells in mouse colon J Clin Invest 120 2010 1722 1735
13. M. Field, D. Fromm, Q. al-Awqati, and W.B. Greenough 3rd Effect of cholera enterotoxin on ion transport across isolated ileal mucosa J Clin Invest 51 1972 796 804
14. M.C. Rao, S. Guandalini, P.L. Smith, and M. Field Mode of action of heat-stable Escherichia coli enterotoxin. Tissue and subcellular specificities and role of cyclic GMP Biochim Biophys Acta 632 1980 35 46 (Pubitemid 11233185)
15. J.M. Ball, P. Tian, C.Q. Zeng, A.P. Morris, and M.K. Estes Age-dependent diarrhea induced by a rotaviral nonstructural glycoprotein Science 272 1996 101 104 (Pubitemid 26110759)
16. - influx into intestinal crypts of CF mice Am J Physiol 277 1999 G431 G444
17. K.M. Hoque, O.M. Woodward, D.B. van Rossum, N.C. Zachos, L. Chen, G.P. Leung, W.B. Guggino, S.E. Guggino, and C.M. Tse Epac1 mediates protein kinase A-independent mechanism of forskolin-activated intestinal chloride secretion J Gen Physiol 135 2010 43 58
18. W. Namkung, W.E. Finkbeiner, and A.S. Verkman CFTR-adenylyl cyclase I association responsible for UTP activation of CFTR in well-differentiated primary human bronchial cell cultures Mol Biol Cell 21 2010 2639 2648
19. L. Tradtrantip, B. Yangthara, P. Padmawar, C. Morrison, and A.S. Verkman Thiophenecarboxylate suppressor of cyclic nucleotides discovered in a small-molecule screen blocks toxin-induced intestinal fluid secretion Mol Pharmacol 75 2009 134 142
20. C. Li, K.S. Dandridge, A. Di, K.L. Marrs, E.L. Harris, K. Roy, J.S. Jackson, N.V. Makarova, Y. Fujiwara, and P.L. Farrar Lysophosphatidic acid inhibits cholera toxin-induced secretory diarrhea through CFTR-dependent protein interactions J Exp Med 202 2005 975 986 (Pubitemid 41396897)
21. A. Ren, W. Zhang, S. Yarlagadda, C. Sinha, K. Arora, C.S. Moon, and A.P. Naren MAST205 competes with cystic fibrosis transmembrane conductance regulator (CFTR)-associated ligand for binding to CFTR to regulate CFTR-mediated fluid transport J Biol Chem 288 2013 12325 12334
22. J. Geibel, K. Sritharan, R. Geibel, P. Geibel, J.S. Persing, A. Seeger, T.K. Roepke, M. Deichstetter, C. Prinz, and S.X. Cheng Calcium-sensing receptor abrogates secretagogue-induced increases in intestinal net fluid secretion by enhancing cyclic nucleotide destruction Proc Natl Acad Sci U S A 103 2006 9390 9397 (Pubitemid 43955837)
23. S.X. Cheng Calcium-sensing receptor inhibits secretagogue-induced electrolyte secretion by intestine via the enteric nervous system Am J Physiol Gastrointest Liver Physiol 303 2012 G60 G70
24. J. Thiagarajah, T. Broadbent, E. Hsieh, and A.S. Verkman Prevention of toxin-induced intestinal ion and fluid secretion by a small-molecule CFTR inhibitor Gastroenterology 126 2004 511 519 (Pubitemid 38182308)
25. H.M. Berschneider, M.R. Knowles, R.G. Azizkhan, R.C. Boucher, N.A. Tobey, R.C. Orlando, and D.W. Powell Altered intestinal chloride transport in cystic fibrosis FASEB J 2 1988 2625 2629
26. 2+ signaling Am J Physiol Cell Physiol 286 2004 C998 C1008
27. T. Ma, J.R. Thiagarajah, H. Yang, N.D. Sonawane, C. Folli, L.J. Galietta, and A.S. Verkman Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion J Clin Invest 110 2002 1651 1658 (Pubitemid 35424243)
28. inh-172 based on arginine 347 mutagenesis Biochem J 413 2008 135 142 (Pubitemid 351946869)
29. N.D. Sonawane, C. Muanprasat, R. Nagatani, Y. Song, and A.S. Verkman In vivo pharmacology and antidiarrheal efficacy of a thiazolidinone CFTR inhibitor in rodents J Pharm Sci 94 2005 134 143 (Pubitemid 40116377)
30. N.D. Sonawane, and A.S. Verkman Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis Bioorg Med Chem 16 2008 8187 8195
31. L. Tradtrantip, N.D. Sonawane, W. Namkung, and A.S. Verkman Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model J Med Chem 52 2009 6447 6455
32. D. Snyder, L. Tradtrantip, C. Yao, J. Fettinger, M.J. Kurth, and A.S. Verkman Absolute configuration and biological properties of enantiometers of CFTR inhibitor BPO-27 ACS Med Chem Lett 4 2013 456 459
33. D.S. Snyder, L. Tradtrantip, C. Yao, M.J. Kurth, and A.S. Verkman Potent, metabolically stable benzopyrimido-pyrrolo-oxazine-dione (BPO) CFTR inhibitors for polycystic kidney disease J Med Chem 54 2011 5468 5477
34. C. Muanprasat, N.D. Sonawane, D. Salinas, A. Taddei, L.J. Galietta, and A.S. Verkman Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy J Gen Physiol 124 2004 125 137 (Pubitemid 39038187)
35. N.D. Sonawane, D. Zhao, O. Zegarra-Moran, L.J. Galietta, and A.S. Verkman Nanomolar CFTR inhibition by pore-occluding divalent polyethylene glycol-malonic acid hydrazides Chem Biol 15 2008 718 728 (Pubitemid 351965502)
36. Y. Norimatsu, A. Ivetac, C. Alexander, N. O'Donnell, L. Frye, M.S. Sansom, and D.C. Dawson Locating a plausible binding site for an open channel blocker, GlyH-101, in the pore of the cystic fibrosis transmembrane conductance regulator Mol Pharmacol 82 2012 1042 1055
37. E.L. de Hostos, R.K. Choy, and T. Nguyen Developing novel antisecretory drugs to treat infectious diarrhea Future Med Chem 3 2011 1317 1325
38. N.D. Sonawane, D. Zhao, O. Zegarra-Mora, L.J.V. Galietta, and A.S. Verkman Lectin conjugates as potent, nonabsorbable CFTR inhibitors for reducing intestinal fluid secretion in cholera Gastroenterology 132 2007 1234 1244 (Pubitemid 46627584)
39. R. De La Fuente, W. Namkung, S. Mills, and A.S. Verkman Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloride channel Mol Pharmacol 73 2008 758 768 (Pubitemid 351397881)
40. W. Namkung, P. Phuan, and A.S. Verkman TMEM16A inhibitors reveal TMEM16A as a minor component of CaCC conductance in airway and intestinal epithelial cells J Biol Chem 286 2011 2365 2374
41. W. Namkung, Z. Yao, W.E. Finkbeiner, and A.S. Verkman Small-molecule activators of TMEM16A, a calcium-activated chloride channel, stimulate epithelial chloride secretion and intestinal contraction FASEB J 25 2011 4048 4062
42. B.J. Jin, J.R. Thiagarajah, and A.S. Verkman Convective washout reduces the antidiarrheal efficacy of enterocyte surface-targeted antisecretory drugs J Gen Physiol 141 2013 261 272
43. Q.M. Yeo, R. Crutchley, J. Cottreau, A. Tucker, and K.W. Garey Crofelemer, a novel antisecretory agent approved for the treatment of HIV-associated diarrhea Drugs Today (Barc) 49 2013 239 252
44. L. Tradtrantip, W. Namkung, and A.S. Verkman Crofelemer, an antidiarrheal proanthocyanidin oligomer extracted from Croton lechleri, targets two distinct intestinal chloride channels Mol Pharmacol 77 2010 69 78
45. - channels by gallotannins as a possible molecular basis of health benefits of green tea and red wine FASEB J 24 2010 4178 4186