Differential sensitivities of CaV1.2 IIS5-S6 mutants to 1,4-dihydropyridine analogs

European Journal of Pharmacology

Volumn 602, Issue 2-3, 2009, Pages 255-261

  Hui, Kwokyin ^a   Kwok, Trevor C Y ^a,b   Kostelecki, Wojciech ^a   Leen, Jessica ^a   Roy, Peter John ^a   Feng, Zhong Ping ^a  

^a UNIVERSITY OF TORONTO   (Canada)

^b Departments of Physiology and Pharmacology   (Canada)

Author keywords

Calcium channel blocker; DHP (1,4 dihydropyridine); L type calcium channel ( 1C subunit); Nemadipine; Nicardipine; Nifedipine

Indexed keywords

1,4 DIHYDROPYRIDINE DERIVATIVE; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL L TYPE; CALCIUM CHANNEL L TYPE M1161A; CALCIUM CHANNEL L TYPE S666V; NEMADIPINE; NICARDIPINE; NIFEDIPINE; PROTEIN SUBUNIT; UNCLASSIFIED DRUG; VOLTAGE GATED CALCIUM CHANNEL; VOLTAGE GATED CALCIUM CHANNEL 1.2; 1,4 DIHYDROPYRIDINE; 1,4-DIHYDROPYRIDINE; DIHYDROPYRIDINE DERIVATIVE; MUTANT PROTEIN; NEMADIPINE A; NEMADIPINE-A; PYRIDINE DERIVATIVE;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; CALCIUM CURRENT; CONTROLLED STUDY; DRUG PROTEIN BINDING; DRUG SENSITIVITY; GENE MUTATION; IC 50; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN DOMAIN; RAT; STATISTICAL SIGNIFICANCE; STRUCTURE ACTIVITY RELATION; WILD TYPE; ANIMAL; CELL LINE; CHEMISTRY; DOSE RESPONSE; DRUG ANTAGONISM; ENZYME SPECIFICITY; GENETICS; METABOLISM; PROTEIN TERTIARY STRUCTURE;

ANIMALS; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, L-TYPE; CELL LINE; DIHYDROPYRIDINES; DOSE-RESPONSE RELATIONSHIP, DRUG; INHIBITORY CONCENTRATION 50; MUTANT PROTEINS; NICARDIPINE; POINT MUTATION; PROTEIN STRUCTURE, TERTIARY; PYRIDINES; RATS; SUBSTRATE SPECIFICITY;

EID: 58149149628     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2008.11.051     Document Type: Article

References (40)

1. Bean B.P. Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc.Natl.Acad.Sci.U.S.A 81 (1984) 6388-6392
2. Burns A.R., Kwok T.C., Howard A., Houston E., Johanson K., Chan A., Cutler S.R., McCourt P., and Roy P.J. High-throughput screening of small molecules for bioactivity and target identification in Caenorhabditis elegans. Nat.Protoc. 1 (2006) 1906-1914
3. Chobanian A.V., Bakris G.L., Black H.R., Cushman W.C., Green L.A., Izzo Jr. J.L., Jones D.W., Materson B.J., Oparil S., Wright Jr. J.T., and Roccella E.J. The seventh report of the Joint National Committee on prevention, detection, evaluation, and treatment of high blood pressure: the JNC 7 report. JAMA 289 (2003) 2560-2572
4. Coburn R.A., Wierzba M., Suto M.J., Solo A.J., Triggle A.M., and Triggle D.J. 1,4-Dihydropyridine antagonist activities at the calcium channel: a quantitative structure-activity relationship approach. J.Med.Chem. 31 (1988) 2103-2107
5. 2+ channel: model construction and docking calculations. J.Med.Chem. 50 (2007) 1504-1513
6. + conduction and selectivity. Science 280 (1998) 69-77
7. Ertel E.A., Campbell K.P., Harpold M.M., Hofmann F., Mori Y., Perez-Reyes E., Schwartz A., Snutch T.P., Tanabe T., Birnbaumer L., Tsien R.W., and Catterall W.A. Nomenclature of voltage-gated calcium channels. Neuron 25 (2000) 533-535
8. Feng Z.P., Hamid J., Doering C., Bosey G.M., Snutch T.P., and Zamponi G.W. Residue Gly1326 of the N-type calcium channel alpha 1B subunit controls reversibility of omega-conotoxin GVIA and MVIIA block. J.Biol.Chem. 276 (2001) 15728-15735
9. Furukawa T., Yamakawa T., Midera T., Sagawa T., Mori Y., and Nukada T. Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J.Pharmacol.Exp.Ther. 291 (1999) 464-473
10. Grabner M., Wang Z., Hering S., Striessnig J., and Glossmann H. Transfer of 1,4-dihydropyridine sensitivity from L-type to class A (BI) calcium channels. Neuron 16 (1996) 207-218
11. 2+ channel block and inactivation: common molecular determinants. Trends Pharmacol.Sci. 19 (1998) 439-443
12. Hockerman G.H., Johnson B.D., Scheuer T., and Catterall W.A. Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels. J.Biol.Chem. 270 (1995) 22119-22122
13. Hockerman G.H., Peterson B.Z., Johnson B.D., and Catterall W.A. Molecular determinants of drug binding and action on L-type calcium channels. Annu.Rev.Pharmacol.Toxicol. 37 (1997) 361-396
14. 2+ channel. Proc.Natl.Acad.Sci.U.S.A 94 (1997) 14906-14911
15. Hohaus A., Beyl S., Kudrnac M., Berjukow S., Timin E.N., Marksteiner R., Maw M.A., and Hering S. Structural determinants of L-type channel activation in segment IIS6 revealed by a retinal disorder. J.Biol.Chem. 280 (2005) 38471-38477
16. Hui K., Gardzinski P., Sun H.S., Backx P.H., and Feng Z.P. Permeable ions differentially affect gating kinetics and unitary conductance of L-type calcium channels. Biochem.Biophys.Res.Commun. 338 (2005) 783-792
17. Ito H., Klugbauer N., and Hofmann F. Transfer of the high affinity dihydropyridine sensitivity from L-type to non-L-type calcium channel. Mol.Pharmacol. 52 (1997) 735-740
18. Kokubun S., Prod'hom B., Becker C., Porzig H., and Reuter H. Studies on Ca channels in intact cardiac cells: voltage-dependent effects and cooperative interactions of dihydropyridine enantiomers. Mol.Pharmacol. 30 (1986) 571-584
19. Kwok T.C., Hui K., Kostelecki W., Ricker N., Selman G., Feng Z.P., and Roy P.J. A genetic screen for dihydropyridine (DHP)-resistant worms reveals new residues required for DHP-blockage of mammalian calcium channels. PLoS.Genet. 4 (2008) e1000067
20. Kwok T.C., Ricker N., Fraser R., Chan A.W., Burns A., Stanley E.F., McCourt P., Cutler S.R., and Roy P.J. A small-molecule screen in C. elegans yields a new calcium channel antagonist. Nature 441 (2006) 91-95
21. Lacinova L., An R.H., Xia J., Ito H., Klugbauer N., Triggle D., Hofmann F., and Kass R.S. Distinctions in the molecular determinants of charged and neutral dihydropyridine block of L-type calcium channels. J. Pharmacol. Exp. Ther. 289 (1999) 1472-1479
22. Lacinova L., Klugbauer N., Hu M., and Hofmann F. Reconstruction of the dihydropyridine site in a non-L-type calcium channel: the role of the IS6 segment. FEBS Lett. 451 (1999) 152-156
23. Li J., Stevens L., Klugbauer N., and Wray D. Roles of molecular regions in determining differences between voltage dependence of activation of CaV3.1 and CaV1.2 calcium channels. J. Biol. Chem. 279 (2004) 26858-26867
24. 2+ channel. Mol. Pharmacol. 63 (2003) 499-511
25. Mitterdorfer J., Wang Z., Sinnegger M.J., Hering S., Striessnig J., Grabner M., and Glossmann H. Two amino acid residues in the IIIS5 segment of L-type calcium channels differentially contribute to 1,4-dihydropyridine sensitivity. J. Biol. Chem. 271 (1996) 30330-30335
26. Mohajeri A., Hemmateenejad B., Mehdipour A., and Miri R. Modeling calcium channel antagonistic activity of dihydropyridine derivatives using QTMS indices analyzed by GA-PLS and PC-GA-PLS. J. Mol. Graph. Model. 26 (2008) 1057-1065
27. Peterson B.Z., and Catterall W.A. Calcium binding in the pore of L-type calcium channels modulates high affinity dihydropyridine binding. J. Biol. Chem. 270 (1995) 18201-18204
28. Peterson B.Z., and Catterall W.A. Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore. Mol. Pharmacol. 70 (2006) 667-675
29. Peterson B.Z., Johnson B.D., Hockerman G.H., Acheson M., Scheuer T., and Catterall W.A. Analysis of the dihydropyridine receptor site of L-type calcium channels by alanine-scanning mutagenesis. J. Biol. Chem. 272 (1997) 18752-18758
30. Schuster A., Lacinova L., Klugbauer N., Ito H., Birnbaumer L., and Hofmann F. The IVS6 segment of the L-type calcium channel is critical for the action of dihydropyridines and phenylalkylamines. EMBO J. 15 (1996) 2365-2370
31. Sinnegger M.J., Wang Z., Grabner M., Hering S., Striessnig J., Glossmann H., and Mitterdorfer J. Nine L-type amino acid residues confer full 1,4-dihydropyridine sensitivity to the neuronal calcium channel alpha1A subunit. Role of L-type Met1188. J. Biol. Chem. 272 (1997) 27686-27693
32. 2+ channel. J. Membr. Biol. 177 (2000) 129-135
33. 2+ channels. Trends Pharmacol. Sci. 19 (1998) 108-115
34. Tang S., Yatani A., Bahinski A., Mori Y., and Schwartz A. Molecular localization of regions in the L-type calcium channel critical for dihydropyridine action. Neuron 11 (1993) 1013-1021
35. Triggle D.J. 1,4-Dihydropyridines as calcium channel ligands and privileged structures. Cell Mol. Neurobiol. 23 (2003) 293-303
36. 2+ channel alpha 1 subunits. J. Biol. Chem. 276 (2001) 12730-12735
37. 2+ channels. Circ. Res. 81 (1997) 526-532
38. 2+ channel agonists. J. Biol. Chem. 275 (2000) 41504-41511
39. 2+ channel agonists. Mol. Pharmacol. 64 (2003) 235-248
40. 2+ channel sensitivity towards the blocker isradipine is affected by alternative splicing of the human alpha1C subunit gene. FEBS Lett. 427 (1998) 220-224