An automated electrophysiology serum shift assay for KV channels

Assay and Drug Development Technologies

Volumn 6, Issue 2, 2008, Pages 243-253

  Ratliff, Kevin S ^a   Petrov, Aleksandr ^a   Eiermann, George J ^a   Deng, Qiaolin ^a   Green, Mitchell D ^a   Kaczorowski, Gregory J ^a   McManus, Owen B ^a   Herrington, James ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 PHENYL 4 [3 (2 METHOXYPHENYL) 3 OXO 2 AZAPROP 1 YL]CYCLOHEXANONE; CYCLOHEXANONE DERIVATIVE; GUANGXITOXIN 1E; PEPTIDE; PLASMA PROTEIN; POTASSIUM CHANNEL KV2.1; VOLTAGE GATED POTASSIUM CHANNEL;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; AUTOMATION; BIOASSAY; CONTROLLED STUDY; ELECTROPHYSIOLOGY; MALE; MOUSE; NONHUMAN; POTASSIUM CURRENT;

ANIMALS; AUTOANALYSIS; BLOOD PROTEINS; CHO CELLS; CRICETINAE; CRICETULUS; DATA INTERPRETATION, STATISTICAL; DELAYED RECTIFIER POTASSIUM CHANNELS; DIALYSIS; DRUG EVALUATION, PRECLINICAL; ELECTROPHYSIOLOGY; HUMANS; ION CHANNEL GATING; MICE; MICE, INBRED C57BL; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNEL BLOCKERS; PROTEIN BINDING;

EID: 43449102785     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2008.128     Document Type: Article

References (19)

1. Trainor GL: The importance of plasma protein binding in drug discovery. Expert Opin Drug Discov 2007;2:51-64.
2. Kageyama S, Anderson BD, Hoesterey BL, Hayashi H, Kiso Y, Flora KP, et al.: Protein binding of the human immunodeficiency virus protease inhibitor KNI-272 and alteration of its in vitro antiretroviral activity in the presence of high concentrations of proteins. Antimicrob Agents Chemother 1994;38:1107-1111.
3. Bilello JA, Bilello PA, Stellrecht K, Leonard J, Norbeck DW, Kempf DJ, et al.: Human serum α1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother 1996;40:1491-1497.
4. Fischl MA, Richman DD, Flexner C, Para MF, Haubrich R, Karim A, et al.: Phase I/II study of the toxicity, pharmacokinetics, and activity of the HIV protease inhibitor SC-52151. J Acquir Immune Defic Syndr Hum Retrovirol 1997;15:28-34.
5. Goldberg MR, Lo MW, Christ DD, Chiou R, Furtek CI, Amit O, et al.: DuP 532, an angiotensin II receptor antagonist: first administration and comparison with losartan. Clin Pharmacol Ther 1997;61:59-69.
6. Maillard MP, Centeno C, Frostell-Karlsson A, Brunner HR, Burnier M: Does protein binding modulate the effect of angiotensin II receptor antagonists? J Renin Angiotensin Aldosterone Syst 2001;2(Suppl 1):S54-S58.
7. Webster R, Leishman D, Walker D: Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Curr Opin Drug Discov Dev 2002;5:116-126.
8. Shah RR: Drug-induced QT interval prolongation-regulatory guidance and perspectives on hERG channel studies. Novartis Found Symp 2005;266:251-280.
9. Willis CL, Brazell C, Foster AC: Plasma and CSF levels of dizocilpine (MK-801) required for neuroprotection in the quinolinate-injected rat striatum. Eur J Pharmacol 1991;196:285-290.
10. Finkel A, Wittel A, Yang N, Handran S, Hughes J, Costantin J: Population patch clamp improves data consistency and success rates in the measurement of ionic currents. J Biomol Screen 2006;11:488-496.
11. Herrington J, Zhou YP, Bugianesi RM, Dulski PM, Feng Y, Warren VA, et al.: Blockers of the delayed rectifier potassium current in pancreatic β-cells enhance glucose-dependent insulin secretion. Diabetes 2006;55:1034-1042.
12. V1.3, with immunosuppressant properties. Biochemistry 2002;41:7781-7794.
13. V1.3. Biochemistry 2003;42:4733-4743.
14. Copeland RA: Determination of serum protein binding affinity of inhibitors from analysis of concentration-response plots in biochemical activity assays. J Pharm Sci 2000;89:1000-1007.
15. 50 shift analysis for in vitro assays. Bioorg Med Chem Lett 2004;14:2309-2312.
16. Felix JP, Bugianesi RM, Schmalhofer WA, Borris R, Goetz MA, Hensens OD, et al.: Identification and biochemical characterization of a novel nortriterpene inhibitor of the human lymphocyte voltage-gated potassium channel, Kv1.3. Biochemistry 1999;38:4922-4930.
17. Koo GC, Blake JT, Shah K, Staruch MJ, Dumont F, Wunderler D, et al.: Correolide and derivatives are novel immunosuppressants blocking the lymphocyte Kv1.3 potassium channels. Cell Immunol 1999;197:99-107.
18. Schmitt H, Meves H: Bovine serum albumin selectively increases the low-voltage-activated calcium current of NG108-15 neuroblastoma X glioma cells. Brain Res 1994;656:375-380.
19. Rahn K, Brinkmeier H, Rüdel R: Human serum albumin enhances sodium currents in NH15-CA2 neuroblastoma X glioma hybrid cells. Neurosci Lett 1995;194:25-28.