Model of the cAMP activation of chloride transport by CFTR channel and the mechanism of potentiators

Journal of Theoretical Biology

Volumn 262, Issue 1, 2010, Pages 73-79

  Moran, Oscar ^a  

^a CNR   (Italy)

Author keywords

CFTR; Cystic fibrosis; Potentiators

Indexed keywords

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; CHEMICAL COMPOUND; CHLORIDE ION; CYCLIC AMP; CYCLIC AMP DEPENDENT PROTEIN KINASE; TRANSMEMBRANE CONDUCTANCE REGULATOR; TRANSMEMBRANE CONDUCTANCE REGULATOR POTENTIATOR; UNCLASSIFIED DRUG; CHLORIDE;

CHLORIDE; DISEASE; INHIBITION; MEMBRANE; MUTATION; NUMERICAL MODEL; TRANSPORT PROCESS;

ARTICLE; CHLORIDE TRANSPORT; CYSTIC FIBROSIS; DRUG MECHANISM; ENZYME ACTIVATION; EQUILIBRIUM CONSTANT; PRIORITY JOURNAL; PROTEIN DEPHOSPHORYLATION; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; STEADY STATE; BIOLOGICAL MODEL; CHANNEL GATING; CHEMISTRY; COMPUTER SIMULATION; DRUG EFFECT; DRUG POTENTIATION; ENZYME ACTIVE SITE; EVALUATION; HUMAN; METABOLISM; PHOSPHORYLATION; PHYSIOLOGY; PROTEIN BINDING; SIGNAL TRANSDUCTION;

ADENOSINE TRIPHOSPHATE; CATALYTIC DOMAIN; CHLORIDES; COMPUTER SIMULATION; CYCLIC AMP; CYCLIC AMP-DEPENDENT PROTEIN KINASES; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; DRUG SYNERGISM; ENZYME ACTIVATION; HUMANS; ION CHANNEL GATING; MODELS, BIOLOGICAL; PHOSPHORYLATION; PROTEIN BINDING; SIGNAL TRANSDUCTION;

EID: 76449098928     PISSN: 00225193     EISSN: 10958541     Source Type: Journal    
DOI: 10.1016/j.jtbi.2009.08.032     Document Type: Article

References (21)

1. Button B., Reuss L., Altenberg G.A. Pkc-mediated stimulation of amphibian cftr depends on a single phosphorylation consensus site. Insertion of this site confers pkc sensitivity to human cftr. J. Gen. Physiol. 2001, 117:457-468.
2. Caci E., Folli C., Zegarra-Moran O., Ma T., Springsteel M.F., Sammelson R.E., Nantz M.H., Kurth M.J., Verkman A.S., Galietta L.J. CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds. Am. J. Physiol. Lung Cell Mol. Physiol. 2003, 285:L180-L188.
3. Cai Z., Sheppard D.N. Phloxine B interacts with the cystic fibrosis transmembrane conductance regulator at multiple sites to modulate channel activity. J. Biol. Chem. 2002, 277:19546-19553.
4. Chang X.B., Tabcharani J.A., Hou Y.X., Jensen T.J., Kartner N., Alon N., Hanrahan J.W., Riordan J.R. Protein kinase A (PKA) still activates CFTR chloride channel after mutagenesis of all 10 PKA consensus phosphorylation sites. J. Biol. Chem. 1993, 268:11304-11311.
5. Chappe V., Hinkson D.A., Howell L.D., Evagelidis A., Liao J., Chang X., Riordan J.R., Hanrahan J.W. Stimulatory and inhibitory protein kinase c consensus sequences regulate the cystic fibrosis transmembrane conductance regulator. Proc. Natl. Acad. Sci. USA 2004, 101:390-395.
6. Csanady L., Seto-Young D., Chan K.W., Cenciarelli C., Angel B.B., Qin J., McLachlin D.T., Krutchinsky A.N., Chait B.T., Nairn A.C, Gadsby D.C. Preferential phosphorylation of R-domain Serine 768 dampens activation of CFTR channels by PKA. J. Gen. Physiol. 2005, 125:171-186.
7. Dao K.K., Teigen K., Kopperud R., Hodneland E., Schwede F., Christensen A.E., Martinez A., Doskeland S.O. Epac1 and cAMP-dependent protein kinase holoenzyme have similar cAMP affinity, but their cAMP domains have distinct structural features and cyclic nucleotide recognition. J. Biol. Chem. 2006, 281:21500-21511.
8. Ferrera L., Pincin C., Moran O. Characterization of a 7,8-benzoflavone double effect on CFTR Cl(-) channel activity. J. Membr. Biol. 2007, 220:1-9.
9. Galietta L.J., Moran O. Identification of CFTR activators and inhibitors: chance or design?. Curr. Opin. Pharmacol. 2004, 4:497-503.
10. James A.M., Sheard P.W., Wei Y.H., Murphy M.P. Decreased ATP synthesis is phenotypically expressed during increased energy demand in fibroblasts containing mitochondrial tRNA mutations. Eur. J. Biochem./FEBS 1999, 259:462-469.
11. King J.D.J., Fitch A.C., Lee J.K., McCane J.E., Mak D.D., Foskett J.K., Hallows K.R. Amp-activated protein kinase phosphorylation of the r domain inhibits pka stimulation of cftr. Am. J. Physiol., Cell Physiol. 2009, 297:C94-C101.
12. Kongsuphol P., Cassidy D., Hieke B., Treharne K.J., Schreiber R., Mehta A., Kunzelmann K. Mechanistic insight into control of cftr by ampk. J. Biol. Chem. 2009, 284:5645-5653.
13. Moran O., Galietta L.J.V., Zegarra-Moran O. Binding site of activators of the cystic fibrosis transmembrane conductance regulator in the nucleotide binding domains. Cell. Mol. Life Sci. 2005, 62:446-460.
14. Moran O., Zegarra-Moran O. A quantitative description of the activation and inhibition of CFTR by potentiators: Genistein. FEBS Lett. 2005, 579:3979-3983.
15. Moran O., Zegarra-Moran O. On the measurement of the functional properties of the CFTR. J. Cyst. Fibros. 2008, 7:483-494.
16. Seavilleklein G., Amer N., Evagelidis A., Chappe F., Irvine T., Hanrahan J.W., Chappe V. Pkc phosphorylation modulates pka-dependent binding of the r domain to other domains of cftr. Am. J. Physiol., Cell Physiol. 2008, 295:C1366-C1375.
17. Seibert F.S., Chang X.B., Aleksandrov A.A., Clarke D.M., Hanrahan J.W., Riordan J.R. Influence of phosphorylation by protein kinase A on CFTR at the cell surface and endoplasmic reticulum. Biochim. Biophys. Acta 1999, 1461:275-283.
18. Vais H., Zhang R., Reenstra W.W. Dibasic phosphorylation sites in the R domain of CFTR have stimulatory and inhibitory effects on channel activation. Am. J. Physiol., Cell Physiol. 2004, 287:C737-C745.
19. Vergani P., Lockless S.W., Nairn A.C., Gadsby D.C. CFTR channel opening by ATP-driven tight dimerization of its nucleotide-binding domains. Nature 2005, 433:876-880.
20. Zegarra-Moran O., Monteverde M., Galietta L.J., Moran O. Functional analysis of mutations in the putative binding site for cystic fibrosis transmembrane conductance regulator potentiators. Interaction between activation and inhibition. J. Biol. Chem. 2007, 282:9098-9104.
21. Zu Y.L., Wu F., Gilchrist A., Ai Y., Labadia M.E., Huang C.K. The primary structure of a human MAP kinase activated protein kinase 2. Biochem. Biophys. Res. Commun. 1994, 200:1118-1124.