Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2

Molecular Pharmacology

Volumn 66, Issue 5, 2004, Pages 1236-1247

  Dilmac, Nejmi ^b   Hilliard, Nathan ^a   Hockerman, Gregory H ^a,c  

^a PURDUE UNIVERSITY   (United States)

^b PURDUE UNIVERSITY   (United States)

^c NONE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; CALCIUM CHANNEL; CALCIUM ION; GLUTAMIC ACID; MUTANT PROTEIN; THREONINE; VERAPAMIL;

ALPHA CHAIN; AMINO ACID COMPOSITION; AMINO ACID SUBSTITUTION; ARTICLE; BETA CHAIN; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; DRUG POTENTIATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; MUTANT; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; VOLTAGE CLAMP; WILD TYPE;

ALANINE; AMINO ACID SUBSTITUTION; BARIUM; BINDING SITES; CALCIUM; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, L-TYPE; CELLS, CULTURED; DRUG SYNERGISM; GLUTAMIC ACID; GLUTAMINE; GLYCINE; HUMANS; KINETICS; MUTATION; PERMEABILITY; PHENYLALANINE; THREONINE; VERAPAMIL;

EID: 6944255278     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.104.000893     Document Type: Article

References (29)

1. Almers W and McCleskey EW (1984) Non-selective conductance in calcium channels of frog muscle: calcium selectivity in a single-file pore. J Physiol 353:585-608.
2. 2+-channels. Br J Pharmacol 119:1197-1202.
3. Bers DM and Perez-Reyes E (1999) Ca channels in cardiac myocytes: structure and function in Ca influx and intracellular Ca release. Cardiovasc Res 42:339-360.
4. 2+ channels by benzothiazepines and phenylalkylamines: class-specific pharmacology and underlying molecular determinants. Mol Pharmacol 51:872-881.
5. v1.2. Mol Pharmacol 64:491-501.
6. Diochot S, Richard S, Baldy-Moulinier M, Nargeot J, and Valmier J (1995) Dihydropyridines, phenylalkylamines, and benzothiazepines block N-, P/Q- and R-type calcium currents. Pflueg Arch Eur J Physiol 431:10-19.
7. Doring F, Degtiar VE, Grabner M, Striessnig J, Hering S, and Glossman H (1996) Transfer of L-type calcium channel IVS6 segment increases phenylalkylamine sensitivity of α1a. J Biol Chem 271:11745-11749.
8. Ellis SB, Williams ME, Ways NR, Brenner R, Sharp AH, Leung AT, Campbell KP, McKenna E, Koch WJ, Hui A, et al. (1988) Sequence and expression of mRNAs encoding the alpha 1 and alpha 2 subunits of a DHP-sensitive calcium channel. Science (Wash DC) 241:1661-1664.
9. Fleckenstein A and Fleckenstein-Grun G (1980) Cardiovascular protection by Ca antagonists. Eur Heart J 1 (Suppl B):15-21.
10. 2+ channel probe. Binding characteristics and target size analysis of its receptor in skeletal muscle. FEBS Lett 176:371-377.
11. 2+ channels. Mol Pharmacol 58:1264-1270.
12. Hockerman GH, Johnson BD, Abbott MR, Scheuer T, and Catterall WA (1997a) Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels in transmembrane segment IIIS6 and the pore region of the α1 subunit. J Biol Chem 272:18759-18765.
13. Hockerman GH, Johnson BD, Scheuer T, and Catterall WA (1995) Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels. J Biol Chem 270:22119-22122.
14. Hockerman GH, Peterson BZ, Johnson BD, and Catterall WA (1997b) Molecular determinants of drug binding and action on L-type calcium channels. Annu Rev Pharmacol Toxicol 37:361-396.
15. 2+ channel. Proc Natl Acad Sci USA 94:14906-14911.
16. 2+ channels in freshly dissociated rat cerebellar Purkinje neurons by diltiazem and verapamil. Brain Res 695:88-91.
17. Johnson BD, Hockerman GH, Scheuer T, and Catterall WA (1996) Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines. Mol Pharmacol 50:1388-1400.
18. Jones SW (1998) Overview of voltage-dependent calcium channels. J Bioenerg Biomembr 30:299-312.
19. Lee KS and Tsien RW (1983) Mechanism of calcium channel blockade by verapamil, D600, diltiazem and nitrendipine in single dialysed heart cells. Nature (Lond) 302:790-794.
20. Nawrath H and Wegener JW (1997) Kinetics and state-dependent effects of verapamil on cardiac L-type calcium channels. Naunyn Schmiedeberg's Arch Pharmacol 355:79-88.
21. Peterson BZ and Catterall WA (1995) Calcium binding in the pore of L-type calcium channels modulates high affinity dihydropyridine binding. J Biol Chem 270:18201-18204.
22. 2+-dependent inactivation of L-type calcium channels. Neuron 22:549-558.
23. Pragnell M, Sakamoto J, Jay SD, and Campbell KP (1991) Cloning and tissue-specific expression of the brain calcium channel beta-subunit. FEBS Lett 291:253-258.
24. Snutch TP, Tomlinson WJ, Leonard JP, and Gilbert MM (1991) Distinct calcium channels are generated by alternative splicing and are differentially expressed in the mammalian CNS. Neuron 7:45-57.
25. 2+- and voltage-dependent inactivation in Ca(v)1.2 sensitivity for the phenylalkylamine (-)gallopamil. Circ Res 89:700-708.
26. Tanabe T, Takeshima H, Mikami A, Flockerzi V, Takahashi H, Kangawa K, Kojima M, Matsuo H, Hirose T, and Numa S (1987) Primary structure of the receptor for calcium channel blockerg from skeletal muscle. Nature (Lond) 328:313-318.
27. 2+ channel. J Biol Chem 275:31778-31785.
28. 2+ channels. Nature (Lond) 366:158-161.
29. Zuhlke RD, Pitt GS, Deisseroth K, Tsien RW, and Reuter H (1999) Calmodulin supports both inactivation and facilitation of L-type calcium channels. Nature (Lond) 399:159-162.