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Items: 1 to 20 of 114

1.

Are hERG channel blockers also phospholipidosis inducers?

Sun H, Xia M, Shahane SA, Jadhav A, Austin CP, Huang R.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4587-90. doi: 10.1016/j.bmcl.2013.06.034. Epub 2013 Jun 20.

2.

Why are most phospholipidosis inducers also hERG blockers?

Slavov S, Stoyanova-Slavova I, Li S, Zhao J, Huang R, Xia M, Beger R.

Arch Toxicol. 2017 May 27. doi: 10.1007/s00204-017-1995-9. [Epub ahead of print]

PMID:
28551711
3.
4.

Pharmacophore modeling for hERG channel facilitation.

Yamakawa Y, Furutani K, Inanobe A, Ohno Y, Kurachi Y.

Biochem Biophys Res Commun. 2012 Feb 3;418(1):161-6. doi: 10.1016/j.bbrc.2011.12.153. Epub 2012 Jan 8.

PMID:
22244872
5.

In silico prediction of the chemical block of human ether-a-go-go-related gene (hERG) K+ current.

Inanobe A, Kamiya N, Murakami S, Fukunishi Y, Nakamura H, Kurachi Y.

J Physiol Sci. 2008 Dec;58(7):459-70. doi: 10.2170/physiolsci.RV-0114-08-07-R1. Epub 2008 Nov 27.

PMID:
19032804
6.

A novel hypothesis for the binding mode of HERG channel blockers.

Choe H, Nah KH, Lee SN, Lee HS, Lee HS, Jo SH, Leem CH, Jang YJ.

Biochem Biophys Res Commun. 2006 May 26;344(1):72-8. Epub 2006 Mar 31.

PMID:
16616004
7.

A critical assessment of combined ligand- and structure-based approaches to HERG channel blocker modeling.

Du-Cuny L, Chen L, Zhang S.

J Chem Inf Model. 2011 Nov 28;51(11):2948-60. doi: 10.1021/ci200271d. Epub 2011 Oct 13.

8.

Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.

Roth GJ, Heckel A, Kley JT, Lehmann T, Müller SG, Oost T, Rudolf K, Arndt K, Budzinski R, Lenter M, Lotz RR, Schindler M, Thomas L, Stenkamp D.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3270-4. doi: 10.1016/j.bmcl.2015.05.074. Epub 2015 May 30.

PMID:
26077492
9.

Human ether-a-go-go-related gene channel blockers and its structural analysis for drug design.

Narayana Moorthy NS, Ramos MJ, Fernandes PA.

Curr Drug Targets. 2013 Jan 1;14(1):102-13. Review.

PMID:
23061466
10.

Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel.

Ekins S, Crumb WJ, Sarazan RD, Wikel JH, Wrighton SA.

J Pharmacol Exp Ther. 2002 May;301(2):427-34.

11.

Predictive QSAR models development and validation for human ether-a-go-go related gene (hERG) blockers using newer tools.

Moorthy NS, Ramos MJ, Fernandes PA.

J Enzyme Inhib Med Chem. 2014 Jun;29(3):317-24. doi: 10.3109/14756366.2013.779264. Epub 2013 Apr 8.

PMID:
23560722
12.
13.

Effects of antipsychotic drugs on I(to), I (Na), I (sus), I (K1), and hERG: QT prolongation, structure activity relationship, and network analysis.

Crumb WJ Jr, Ekins S, Sarazan RD, Wikel JH, Wrighton SA, Carlson C, Beasley CM Jr.

Pharm Res. 2006 Jun;23(6):1133-43. Epub 2006 May 25.

PMID:
16715368
14.

Recent developments in computational prediction of HERG blockage.

Wang S, Li Y, Xu L, Li D, Hou T.

Curr Top Med Chem. 2013;13(11):1317-26. Review.

PMID:
23675938
15.

Comparative effects of liensinine and neferine on the human ether-a-go-go-related gene potassium channel and pharmacological activity analysis.

Dong ZX, Zhao X, Gu DF, Shi YQ, Zhang J, Hu XX, Hu MQ, Yang BF, Li BX.

Cell Physiol Biochem. 2012;29(3-4):431-42. doi: 10.1159/000338497. Epub 2012 Apr 3.

16.

Phospholipidosis as a function of basicity, lipophilicity, and volume of distribution of compounds.

Hanumegowda UM, Wenke G, Regueiro-Ren A, Yordanova R, Corradi JP, Adams SP.

Chem Res Toxicol. 2010 Apr 19;23(4):749-55. doi: 10.1021/tx9003825.

PMID:
20356072
17.

Comparative evaluation of hERG potassium channel blockade by antipsychotics.

Silvestre JS, Prous JR.

Methods Find Exp Clin Pharmacol. 2007 Sep;29(7):457-65.

PMID:
17982510
18.

Physicochemical determinants for drug induced blockade of HERG potassium channels: effect of charge and charge shielding.

Zolotoy AB, Plouvier BP, Beatch GB, Hayes ES, Wall RA, Walker MJ.

Curr Med Chem Cardiovasc Hematol Agents. 2003 Oct;1(3):225-41. Review.

PMID:
15326914
19.

Detection of phospholipidosis induction: a cell-based assay in high-throughput and high-content format.

Shahane SA, Huang R, Gerhold D, Baxa U, Austin CP, Xia M.

J Biomol Screen. 2014 Jan;19(1):66-76. doi: 10.1177/1087057113502851. Epub 2013 Sep 3.

20.

Computer simulations of structure-activity relationships for HERG channel blockers.

Boukharta L, Keränen H, Stary-Weinzinger A, Wallin G, de Groot BL, Aqvist J.

Biochemistry. 2011 Jul 12;50(27):6146-56. doi: 10.1021/bi200173n. Epub 2011 Jun 16.

PMID:
21657256

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