DOI: 10.1124/jpet.301.2.427. Three-Dimensional Quantitative Structure-Activity Relationship for Inhibition of Human Ether-a-Go-Go-Related Gene Potassium Channel

Three-Dimensional Quantitative Structure-Activity Relationship for Inhibition of Human Ether-a-Go-Go-Related Gene Potassium Channel

10.1124/jpet.301.2.427

Crossref journal-article

Elsevier BV

The Journal of Pharmacology and Experimental Therapeutics (78)

Bibliography

Ekins, S., Crumb, W. J., Sarazan, R. D., Wikel, J. H., & Wrighton, S. A. (2002). Three-Dimensional Quantitative Structure-Activity Relationship for Inhibition of Human Ether-a-Go-Go-Related Gene Potassium Channel. The Journal of Pharmacology and Experimental Therapeutics, 301(2), 427â434.

Authors 5

Sean Ekins (first)
William J. Crumb (additional)
R. Dustan Sarazan (additional)
James H. Wikel (additional)
Steven A. Wrighton (additional)

References 30 Referenced 230

10.1016/S1461-5347(99)00172-8 / Pharm Sci Technol Today / QT interval prolongation by non-cardiovascular drugs: issues and solutions for novel drug development. by Crumb (1999)
10.1016/S0022-3565(24)35285-1 / J Pharmacol Exp Ther / Loratidine blockade of K+channels in human heart: comparison with terfenadine under physiological conditions. by Crumb (2000)
Crumb WJ, Ekins S, Sarazan D, Wikel JH, Wrighton SA, Carlson C, and Beasley JCM (2002) hERG block by antipsychotic drugs: a relationship between QT prolongation and ion channel blockade. J Clin Psychiatry, in press.
10.1016/0092-8674(95)90358-5 / Cell / A molecular basis for the cardiac arrhythmia: HERG mutations cause long QT syndrome. by Curran (1995)
10.1007/s002280050714 / Eur J Clin Pharmacol / QT-interval prolongation by non-cardiac drugs: lessons to be learned from recent experience. by De Ponti (2000)
10.1016/S0022-3565(24)37646-3 / J Pharmacol Exp Ther / Blockade of HERG and Kv1.5 by ketoconazole. by Dumaine (1998)
{'key': '10.1124/jpet.301.2.427_bib7', 'series-title': 'Pharmacophore Perception, Development, and Use in Drug Design', 'first-page': '270', 'article-title': 'Predicting drug-drug interactions in silico using pharmacophores: a paradigm for the next millennium', 'author': 'Ekins', 'year': '2000'} / Pharmacophore Perception, Development, and Use in Drug Design / Predicting drug-drug interactions in silico using pharmacophores: a paradigm for the next millennium by Ekins (2000)
10.1016/S1093-3263(01)00127-9 / J Mol Graph / In silico ADME/TOX The state of the art at the 220th ACS meeting. by Ekins (2002)
10.1016/S1056-8719(00)00109-X / J Pharmacol Toxicol Methods / Progress in predicting human ADME parameters in silico. by Ekins (2000)
10.1161/01.CIR.102.3.275 / Circulation / Sildenafil (Viagra) prolongs cardiac repolarization by blocking the rapid component of the delayed rectifier potassium current. by Geelen (2000)
{'key': '10.1124/jpet.301.2.427_bib11', 'first-page': '122', 'article-title': 'Interactions of a series of fluoroquinolone antibacterial drugs with the human cardiac K+ channel HERG.', 'volume': '59', 'author': 'Kang', 'year': '2001', 'journal-title': 'Mol Pharmacol'} / Mol Pharmacol / Interactions of a series of fluoroquinolone antibacterial drugs with the human cardiac K+ channel HERG. by Kang (2001)
10.1016/S0022-3565(24)39075-5 / J Pharmacol Exp Ther / Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K(+) channels expressed in a mammalian cell line. by Katayama (2000)
10.1016/S0022-3565(24)38946-3 / J Pharmacol Exp Ther / Interactions of the 5-hydroxytryptamine 3 antagonist class of antiemetic drugs with human cardiac ion channels. by Kuryshev (2000)
10.1073/pnas.210244497 / Proc Natl Acad Sci USA / A structural basis for the drug-induced log QT syndrome. by Mitcheson (2000)
{'key': '10.1124/jpet.301.2.427_bib15', 'first-page': 'H2534', 'article-title': 'Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride.', 'volume': '273', 'author': 'Mohammad', 'year': '1997', 'journal-title': 'Am J Physiol'} / Am J Physiol / Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride. by Mohammad (1997)
10.1097/00005344-199902000-00002 / J Cardiovasc Pharmacol / Modulation of HERG potassium channels by extracellular magnesium and quinidine. by Po (1999)
10.1016/S0014-5793(97)01249-0 / FEBS Lett / A mechanism for the proarrhythmic effects of cisapride (Propulsid): high affinity blockade of the human cardiac potassium channel HERG. by Rampe (1997)
10.1016/0163-7258(95)02063-2 / Pharamcol Ther / Which cardiac potassium channel subtype is the preferable target for suppression of ventricular arrhythmias? by Rees (1996)
10.1016/0092-8674(95)90340-2 / Cell / A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. by Sanguinetti (1995)
10.1073/pnas.180223197 / Proc Natl Acad Sci USA / A common polymorphism associated with antibiotic-induced cardiac arrhythmia. by Sesti (2000)
10.1038/379833a0 / Nature (Lond) / the inward rectification mechanism of the HERG cardiac potassium channel. by Smith (1996)
10.1038/sj.bjp.0700989 / Br J Clin Pharmacol / The inhibitory effect of the antipsychotic drug haloperidol on HERG potassium channels expressed in Xenopus oocytes. by Suessbrich (1997)
10.1016/S0006-2952(98)00002-1 / Biochem Pharmacol / Human ether-a-go-go related gene (HERG) K+ channels as pharmacological targets. by Taglialatela (1998)
10.1038/sj.bjp.0702800 / Br J Pharmacol / Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline. by Teschemacher (1999)
10.1038/sj.bjp.0703470 / Br J Pharmacol / Inhibition of HERG potassium channels by the antimalarial agent halofantrine. by Tie (2000)
10.1038/sj.bjp.0702774 / Br J Clin Pharmacol / Inhibition of the human ether-a-go-go-related gene (HERG) potassium channel by cisapride: affinity for open and inactivated states. by Walker (1999)
10.1038/sj.bjp.0702502 / Br J Pharmacol / Inhibition of HERG channels stably expressed in a mammalian cell line by the antianginal agent perhexiline maleate. by Walker (1999)
10.1152/ajpheart.1999.277.3.H1081 / Heart Circ Physiol / Inactivation gating determines nicotine blockade of human HERG channels. by Wang (1999)
{'key': '10.1124/jpet.301.2.427_bib29', 'first-page': '221A', 'article-title': 'Mechanism of cocaine block of HERG potassium channels.', 'volume': '78', 'author': 'Zhang', 'year': '2000', 'journal-title': 'Biophys J'} / Biophys J / Mechanism of cocaine block of HERG potassium channels. by Zhang (2000)
10.1161/01.RES.84.9.989 / Circ Res / Mechanism of block and identification of the verapamil binding domain to HERG potassium channels. by Zhang (1999)

Dates

Type	When
Created	22 years, 7 months ago (Jan. 10, 2003, 1:35 p.m.)
Deposited	6 months ago (Feb. 19, 2025, 6:18 p.m.)
Indexed	1 month ago (July 20, 2025, 6:51 p.m.)
Issued	23 years, 3 months ago (May 1, 2002)
Published	23 years, 3 months ago (May 1, 2002)
Published Print	23 years, 3 months ago (May 1, 2002)

Funders 0

None

BibTeX

@article{Ekins_2002, title={Three-Dimensional Quantitative Structure-Activity Relationship for Inhibition of Human Ether-a-Go-Go-Related Gene Potassium Channel}, volume={301}, ISSN={0022-3565}, url={http://dx.doi.org/10.1124/jpet.301.2.427}, DOI={10.1124/jpet.301.2.427}, number={2}, journal={The Journal of Pharmacology and Experimental Therapeutics}, publisher={Elsevier BV}, author={Ekins, Sean and Crumb, William J. and Sarazan, R. Dustan and Wikel, James H. and Wrighton, Steven A.}, year={2002}, month=may, pages={427–434} }

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