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Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.

Aleo MD, Luo Y, Swiss R, Bonin PD, Potter DM, Will Y.

Hepatology. 2014 Sep;60(3):1015-22. doi: 10.1002/hep.27206. Epub 2014 Jul 14.


A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

Morgan RE, van Staden CJ, Chen Y, Kalyanaraman N, Kalanzi J, Dunn RT 2nd, Afshari CA, Hamadeh HK.

Toxicol Sci. 2013 Nov;136(1):216-41. doi: 10.1093/toxsci/kft176. Epub 2013 Aug 16.


Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).

Pedersen JM, Matsson P, Bergström CA, Hoogstraate J, Norén A, LeCluyse EL, Artursson P.

Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6.


Bile salt export pump inhibitors are associated with bile acid-dependent drug-induced toxicity in sandwich-cultured hepatocytes.

Ogimura E, Sekine S, Horie T.

Biochem Biophys Res Commun. 2011 Dec 16;416(3-4):313-7. doi: 10.1016/j.bbrc.2011.11.032. Epub 2011 Nov 15.


Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.

Morgan RE, Trauner M, van Staden CJ, Lee PH, Ramachandran B, Eschenberg M, Afshari CA, Qualls CW Jr, Lightfoot-Dunn R, Hamadeh HK.

Toxicol Sci. 2010 Dec;118(2):485-500. doi: 10.1093/toxsci/kfq269. Epub 2010 Sep 9.


Current Concepts in Drug-Induced Bile Salt Export Pump (BSEP) Interference.

Kenna JG.

Curr Protoc Toxicol. 2014 Aug 7;61:23.7.1-15. doi: 10.1002/0471140856.tx2307s61.


Risk factors for development of cholestatic drug-induced liver injury: inhibition of hepatic basolateral bile acid transporters multidrug resistance-associated proteins 3 and 4.

Köck K, Ferslew BC, Netterberg I, Yang K, Urban TJ, Swaan PW, Stewart PW, Brouwer KL.

Drug Metab Dispos. 2014 Apr;42(4):665-74. doi: 10.1124/dmd.113.054304. Epub 2013 Oct 23.


In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.

Dawson S, Stahl S, Paul N, Barber J, Kenna JG.

Drug Metab Dispos. 2012 Jan;40(1):130-8. doi: 10.1124/dmd.111.040758. Epub 2011 Sep 30.


Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.

Warner DJ, Chen H, Cantin LD, Kenna JG, Stahl S, Walker CL, Noeske T.

Drug Metab Dispos. 2012 Dec;40(12):2332-41. doi: 10.1124/dmd.112.047068. Epub 2012 Sep 7.


Role of chemical structures and the 1331T>C bile salt export pump polymorphism in idiosyncratic drug-induced liver injury.

Ulzurrun E, Stephens C, Crespo E, Ruiz-Cabello F, Ruiz-Nuñez J, Saenz-López P, Moreno-Herrera I, Robles-Díaz M, Hallal H, Moreno-Planas JM, Cabello MR, Lucena MI, Andrade RJ.

Liver Int. 2013 Oct;33(9):1378-85. doi: 10.1111/liv.12193. Epub 2013 May 23.


The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions.

Fattinger K, Funk C, Pantze M, Weber C, Reichen J, Stieger B, Meier PJ.

Clin Pharmacol Ther. 2001 Apr;69(4):223-31.


Toward predicting drug-induced liver injury: parallel computational approaches to identify multidrug resistance protein 4 and bile salt export pump inhibitors.

Welch MA, Köck K, Urban TJ, Brouwer KL, Swaan PW.

Drug Metab Dispos. 2015 May;43(5):725-34. doi: 10.1124/dmd.114.062539. Epub 2015 Mar 3.


BSEP inhibition: in vitro screens to assess cholestatic potential of drugs.

Kis E, Ioja E, Rajnai Z, Jani M, Méhn D, Herédi-Szabó K, Krajcsi P.

Toxicol In Vitro. 2012 Dec;26(8):1294-9. doi: 10.1016/j.tiv.2011.11.002. Epub 2011 Nov 18. Review.


Setting Clinical Exposure Levels of Concern for Drug-Induced Liver Injury (DILI) Using Mechanistic in vitro Assays.

Shah F, Leung L, Barton HA, Will Y, Rodrigues AD, Greene N, Aleo MD.

Toxicol Sci. 2015 Oct;147(2):500-14. doi: 10.1093/toxsci/kfv152. Epub 2015 Jul 23.


Minimizing DILI risk in drug discovery - A screening tool for drug candidates.

Schadt S, Simon S, Kustermann S, Boess F, McGinnis C, Brink A, Lieven R, Fowler S, Youdim K, Ullah M, Marschmann M, Zihlmann C, Siegrist YM, Cascais AC, Di Lenarda E, Durr E, Schaub N, Ang X, Starke V, Singer T, Alvarez-Sanchez R, Roth AB, Schuler F, Funk C.

Toxicol In Vitro. 2015 Dec 25;30(1 Pt B):429-37. doi: 10.1016/j.tiv.2015.09.019. Epub 2015 Sep 25.


The role of bile salt export pump gene repression in drug-induced cholestatic liver toxicity.

Garzel B, Yang H, Zhang L, Huang SM, Polli JE, Wang H.

Drug Metab Dispos. 2014 Mar;42(3):318-22. doi: 10.1124/dmd.113.054189. Epub 2013 Dec 12.


Inhibition of bile salt transport by drugs associated with liver injury in primary hepatocytes from human, monkey, dog, rat, and mouse.

Zhang J, He K, Cai L, Chen YC, Yang Y, Shi Q, Woolf TF, Ge W, Guo L, Borlak J, Tong W.

Chem Biol Interact. 2016 Aug 5;255:45-54. doi: 10.1016/j.cbi.2016.03.019. Epub 2016 Mar 19.


The feline bile salt export pump: a structural and functional comparison with canine and human Bsep/BSEP.

van Beusekom CD, van den Heuvel JJ, Koenderink JB, Schrickx JA, Russel FG.

BMC Vet Res. 2013 Dec 20;9:259. doi: 10.1186/1746-6148-9-259.


Exploring BSEP inhibition-mediated toxicity with a mechanistic model of drug-induced liver injury.

Woodhead JL, Yang K, Siler SQ, Watkins PB, Brouwer KL, Barton HA, Howell BA.

Front Pharmacol. 2014 Nov 7;5:240. doi: 10.3389/fphar.2014.00240. eCollection 2014.

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