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Items: 1 to 50 of 112

1.

P-glycoprotein (MDR1/ABCB1) restricts brain accumulation and cytochrome P450-3A (CYP3A) limits oral availability of the novel ALK/ROS1 inhibitor lorlatinib.

Li W, Sparidans RW, Wang Y, Lebre MC, Wagenaar E, Beijnen JH, Schinkel AH.

Int J Cancer. 2018 May 9. doi: 10.1002/ijc.31582. [Epub ahead of print]

PMID:
29744867
2.

P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) affect brain accumulation and intestinal disposition of encorafenib in mice.

Wang J, Gan C, Sparidans RW, Wagenaar E, van Hoppe S, Beijnen JH, Schinkel AH.

Pharmacol Res. 2018 Mar;129:414-423. doi: 10.1016/j.phrs.2017.11.006. Epub 2017 Nov 14.

PMID:
29155017
3.

Brain Accumulation of Ponatinib and Its Active Metabolite, N-Desmethyl Ponatinib, Is Limited by P-Glycoprotein (P-GP/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2).

Kort A, van Hoppe S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharm. 2017 Oct 2;14(10):3258-3268. doi: 10.1021/acs.molpharmaceut.7b00257. Epub 2017 Sep 19.

PMID:
28880088
4.

Ochratoxin A transport by the human breast cancer resistance protein (BCRP), multidrug resistance protein 2 (MRP2), and organic anion-transporting polypeptides 1A2, 1B1 and 2B1.

Qi X, Wagenaar E, Xu W, Huang K, Schinkel AH.

Toxicol Appl Pharmacol. 2017 Aug 15;329:18-25. doi: 10.1016/j.taap.2017.05.022. Epub 2017 May 19.

PMID:
28532671
5.

Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation.

van Hoppe S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharmacol Res. 2017 Jun;120:43-50. doi: 10.1016/j.phrs.2017.01.035. Epub 2017 Mar 10.

PMID:
28288939
6.

[A blood culture containing coagulase-negative staphylococci: not always due to contamination].

Wagenaar EC, van Wijngaarden P, Verduin CM, Beelen D, van Etten RW.

Ned Tijdschr Geneeskd. 2016;160:A9336. Dutch.

PMID:
27781969
7.

Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo.

Durmus S, Lozano-Mena G, van Esch A, Wagenaar E, van Tellingen O, Schinkel AH.

Mol Pharm. 2015 Dec 7;12(12):4259-69. doi: 10.1021/acs.molpharmaceut.5b00453. Epub 2015 Oct 29.

PMID:
26474710
8.

WD repeat-containing protein 5 (WDR5) localizes to the midbody and regulates abscission.

Bailey JK, Fields AT, Cheng K, Lee A, Wagenaar E, Lagrois R, Schmidt B, Xia B, Ma D.

J Biol Chem. 2015 Sep 11;290(37):22447. doi: 10.1074/jbc.A114.623611. No abstract available.

9.

Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2).

Kort A, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharmacol Res. 2015 Dec;102:200-7. doi: 10.1016/j.phrs.2015.09.003. Epub 2015 Sep 8.

PMID:
26361725
10.

P-glycoprotein, CYP3A, and Plasma Carboxylesterase Determine Brain Disposition and Oral Availability of the Novel Taxane Cabazitaxel (Jevtana) in Mice.

Tang SC, Kort A, Cheung KL, Rosing H, Fukami T, Durmus S, Wagenaar E, Hendrikx JJ, Nakajima M, van Vlijmen BJ, Beijnen JH, Schinkel AH.

Mol Pharm. 2015 Oct 5;12(10):3714-23. doi: 10.1021/acs.molpharmaceut.5b00470. Epub 2015 Sep 15.

PMID:
26317243
11.

Hepatocellular Shuttling and Recirculation of Sorafenib-Glucuronide Is Dependent on Abcc2, Abcc3, and Oatp1a/1b.

Vasilyeva A, Durmus S, Li L, Wagenaar E, Hu S, Gibson AA, Panetta JC, Mani S, Sparreboom A, Baker SD, Schinkel AH.

Cancer Res. 2015 Jul 1;75(13):2729-36. doi: 10.1158/0008-5472.CAN-15-0280. Epub 2015 May 7.

12.

WD repeat-containing protein 5 (WDR5) localizes to the midbody and regulates abscission.

Bailey JK, Fields AT, Cheng K, Lee A, Wagenaar E, Lagrois R, Schmidt B, Xia B, Ma D.

J Biol Chem. 2015 Apr 3;290(14):8987-9001. doi: 10.1074/jbc.M114.623611. Epub 2015 Feb 9. Erratum in: J Biol Chem. 2015 Sep 11;290(37):22447.

13.

Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1).

Kort A, Durmus S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jul;32(7):2205-16. doi: 10.1007/s11095-014-1609-7. Epub 2015 Jan 8.

PMID:
25563977
14.

Young adult psychological outcome after puberty suppression and gender reassignment.

de Vries AL, McGuire JK, Steensma TD, Wagenaar EC, Doreleijers TA, Cohen-Kettenis PT.

Pediatrics. 2014 Oct;134(4):696-704. doi: 10.1542/peds.2013-2958. Epub 2014 Sep 8.

15.

Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) restrict oral availability and brain accumulation of the PARP inhibitor rucaparib (AG-014699).

Durmus S, Sparidans RW, van Esch A, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jan;32(1):37-46. doi: 10.1007/s11095-014-1442-z. Epub 2014 Jun 25.

PMID:
24962512
16.

Human OATP1B1, OATP1B3 and OATP1A2 can mediate the in vivo uptake and clearance of docetaxel.

Iusuf D, Hendrikx JJ, van Esch A, van de Steeg E, Wagenaar E, Rosing H, Beijnen JH, Schinkel AH.

Int J Cancer. 2015 Jan 1;136(1):225-33. doi: 10.1002/ijc.28970. Epub 2014 Jun 3.

17.

Oral co-administration of elacridar and ritonavir enhances plasma levels of oral paclitaxel and docetaxel without affecting relative brain accumulation.

Hendrikx JJ, Lagas JS, Wagenaar E, Rosing H, Schellens JH, Beijnen JH, Schinkel AH.

Br J Cancer. 2014 May 27;110(11):2669-76. doi: 10.1038/bjc.2014.222. Epub 2014 Apr 29.

18.

P-glycoprotein, CYP3A, and plasma carboxylesterase determine brain and blood disposition of the mTOR Inhibitor everolimus (Afinitor) in mice.

Tang SC, Sparidans RW, Cheung KL, Fukami T, Durmus S, Wagenaar E, Yokoi T, van Vlijmen BJ, Beijnen JH, Schinkel AH.

Clin Cancer Res. 2014 Jun 15;20(12):3133-45. doi: 10.1158/1078-0432.CCR-13-1759. Epub 2014 Apr 11.

19.

In vivo disposition of doxorubicin is affected by mouse Oatp1a/1b and human OATP1A/1B transporters.

Durmus S, Naik J, Buil L, Wagenaar E, van Tellingen O, Schinkel AH.

Int J Cancer. 2014 Oct 1;135(7):1700-10. doi: 10.1002/ijc.28797. Epub 2014 Mar 4.

20.

Bcrp1;Mdr1a/b;Mrp2 combination knockout mice: altered disposition of the dietary carcinogen PhIP (2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine) and its genotoxic metabolites.

Vlaming ML, Teunissen SF, van de Steeg E, van Esch A, Wagenaar E, Brunsveld L, de Greef TF, Rosing H, Schellens JH, Beijnen JH, Schinkel AH.

Mol Pharmacol. 2014 Mar;85(3):520-30. doi: 10.1124/mol.113.088823. Epub 2013 Dec 13.

21.

OATP1A/1B transporters affect irinotecan and SN-38 pharmacokinetics and carboxylesterase expression in knockout and humanized transgenic mice.

Iusuf D, Ludwig M, Elbatsh A, van Esch A, van de Steeg E, Wagenaar E, van der Valk M, Lin F, van Tellingen O, Schinkel AH.

Mol Cancer Ther. 2014 Feb;13(2):492-503. doi: 10.1158/1535-7163.MCT-13-0541. Epub 2013 Nov 5.

22.

Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar.

Tang SC, Nguyen LN, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Int J Cancer. 2014 Mar 15;134(6):1484-94. doi: 10.1002/ijc.28475. Epub 2013 Oct 3.

23.

Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) gene dosage on plasma pharmacokinetics and brain accumulation of dasatinib, sorafenib, and sunitinib.

Tang SC, de Vries N, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

J Pharmacol Exp Ther. 2013 Sep;346(3):486-94. doi: 10.1124/jpet.113.205583. Epub 2013 Jul 10.

24.

P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387.

Durmus S, Xu N, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharmacol Res. 2013 Oct;76:9-16. doi: 10.1016/j.phrs.2013.06.009. Epub 2013 Jul 1.

PMID:
23827160
25.

Murine Oatp1a/1b uptake transporters control rosuvastatin systemic exposure without affecting its apparent liver exposure.

Iusuf D, van Esch A, Hobbs M, Taylor M, Kenworthy KE, van de Steeg E, Wagenaar E, Schinkel AH.

Mol Pharmacol. 2013 May;83(5):919-29. doi: 10.1124/mol.112.081927. Epub 2013 Feb 19.

26.

Influence of human OATP1B1, OATP1B3, and OATP1A2 on the pharmacokinetics of methotrexate and paclitaxel in humanized transgenic mice.

van de Steeg E, van Esch A, Wagenaar E, Kenworthy KE, Schinkel AH.

Clin Cancer Res. 2013 Feb 15;19(4):821-32. doi: 10.1158/1078-0432.CCR-12-2080. Epub 2012 Dec 14.

27.

Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar.

Durmus S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharm. 2012 Nov 5;9(11):3236-45. doi: 10.1021/mp3003144. Epub 2012 Oct 18.

PMID:
23020847
28.

Organic anion-transporting polypeptides 1a/1b control the hepatic uptake of pravastatin in mice.

Iusuf D, Sparidans RW, van Esch A, Hobbs M, Kenworthy KE, van de Steeg E, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharm. 2012 Sep 4;9(9):2497-504. doi: 10.1021/mp300108c. Epub 2012 Aug 3.

PMID:
22812517
29.

Proof of concept for low-dose molecular breast imaging with a dual-head CZT gamma camera. Part II. Evaluation in patients.

Hruska CB, Weinmann AL, Tello Skjerseth CM, Wagenaar EM, Conners AL, Tortorelli CL, Maxwell RW, Rhodes DJ, O'Connor MK.

Med Phys. 2012 Jun;39(6):3476-83. doi: 10.1118/1.4719959.

30.

P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib.

Tang SC, Lankheet NA, Poller B, Wagenaar E, Beijnen JH, Schinkel AH.

J Pharmacol Exp Ther. 2012 Apr;341(1):164-73. doi: 10.1124/jpet.111.186908. Epub 2012 Jan 11.

31.

Complete OATP1B1 and OATP1B3 deficiency causes human Rotor syndrome by interrupting conjugated bilirubin reuptake into the liver.

van de Steeg E, Stránecký V, Hartmannová H, Nosková L, Hřebíček M, Wagenaar E, van Esch A, de Waart DR, Oude Elferink RP, Kenworthy KE, Sticová E, al-Edreesi M, Knisely AS, Kmoch S, Jirsa M, Schinkel AH.

J Clin Invest. 2012 Feb;122(2):519-28. doi: 10.1172/JCI59526. Epub 2012 Jan 9.

32.

Impact of abcc2 [multidrug resistance-associated protein (MRP) 2], abcc3 (MRP3), and abcg2 (breast cancer resistance protein) on the oral pharmacokinetics of methotrexate and its main metabolite 7-hydroxymethotrexate.

Vlaming ML, van Esch A, van de Steeg E, Pala Z, Wagenaar E, van Tellingen O, Schinkel AH.

Drug Metab Dispos. 2011 Aug;39(8):1338-44. doi: 10.1124/dmd.111.038794. Epub 2011 May 12.

33.

P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration.

Iusuf D, Teunissen SF, Wagenaar E, Rosing H, Beijnen JH, Schinkel AH.

J Pharmacol Exp Ther. 2011 Jun;337(3):710-7. doi: 10.1124/jpet.110.178301. Epub 2011 Mar 4.

34.

Individual and combined roles of CYP3A, P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) in the pharmacokinetics of docetaxel.

van Waterschoot RA, Lagas JS, Wagenaar E, Rosing H, Beijnen JH, Schinkel AH.

Int J Cancer. 2010 Dec 15;127(12):2959-64. doi: 10.1002/ijc.25279.

35.

Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier.

Poller B, Wagenaar E, Tang SC, Schinkel AH.

Mol Pharm. 2011 Apr 4;8(2):571-82. doi: 10.1021/mp1003898. Epub 2011 Mar 4.

PMID:
21309545
36.

Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics.

Poller B, Iusuf D, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Drug Metab Dispos. 2011 May;39(5):729-35. doi: 10.1124/dmd.110.037317. Epub 2011 Jan 31.

37.

High impact of Oatp1a/1b transporters on in vivo disposition of the hydrophobic anticancer drug paclitaxel.

van de Steeg E, van Esch A, Wagenaar E, van der Kruijssen CM, van Tellingen O, Kenworthy KE, Schinkel AH.

Clin Cancer Res. 2011 Jan 15;17(2):294-301. doi: 10.1158/1078-0432.CCR-10-1980. Epub 2010 Nov 19.

38.

Organic anion transporting polypeptide 1a/1b-knockout mice provide insights into hepatic handling of bilirubin, bile acids, and drugs.

van de Steeg E, Wagenaar E, van der Kruijssen CM, Burggraaff JE, de Waart DR, Elferink RP, Kenworthy KE, Schinkel AH.

J Clin Invest. 2010 Aug;120(8):2942-52. doi: 10.1172/JCI42168. Epub 2010 Jul 19.

39.

Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir.

van Waterschoot RA, ter Heine R, Wagenaar E, van der Kruijssen CM, Rooswinkel RW, Huitema AD, Beijnen JH, Schinkel AH.

Br J Pharmacol. 2010 Jul;160(5):1224-33. doi: 10.1111/j.1476-5381.2010.00759.x.

40.

Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation.

Lagas JS, van Waterschoot RA, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Cancer Ther. 2010 Feb;9(2):319-26. doi: 10.1158/1535-7163.MCT-09-0663. Epub 2010 Jan 26.

41.

Hepatic clearance of reactive glucuronide metabolites of diclofenac in the mouse is dependent on multiple ATP-binding cassette efflux transporters.

Lagas JS, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharmacol. 2010 Apr;77(4):687-94. doi: 10.1124/mol.109.062364. Epub 2010 Jan 19.

42.

P-glycoprotein (P-gp/Abcb1), Abcc2, and Abcc3 determine the pharmacokinetics of etoposide.

Lagas JS, Fan L, Wagenaar E, Vlaming ML, van Tellingen O, Beijnen JH, Schinkel AH.

Clin Cancer Res. 2010 Jan 1;16(1):130-40. doi: 10.1158/1078-0432.CCR-09-1321. Epub 2009 Dec 22.

43.

Abcc2 (Mrp2), Abcc3 (Mrp3), and Abcg2 (Bcrp1) are the main determinants for rapid elimination of methotrexate and its toxic metabolite 7-hydroxymethotrexate in vivo.

Vlaming ML, van Esch A, Pala Z, Wagenaar E, van de Wetering K, van Tellingen O, Schinkel AH.

Mol Cancer Ther. 2009 Dec;8(12):3350-9. doi: 10.1158/1535-7163.MCT-09-0668.

44.

ABCC2, ABCC3, and ABCB1, but not CYP3A, Protect against Trabectedin-Mediated Hepatotoxicity.

van Waterschoot RA, Eman RM, Wagenaar E, van der Kruijssen CM, Rosing H, Beijnen JH, Schinkel AH.

Clin Cancer Res. 2009 Dec 15;15(24):7616-7623.

45.

Absence of both cytochrome P450 3A and P-glycoprotein dramatically increases docetaxel oral bioavailability and risk of intestinal toxicity.

van Waterschoot RA, Lagas JS, Wagenaar E, van der Kruijssen CM, van Herwaarden AE, Song JY, Rooswinkel RW, van Tellingen O, Rosing H, Beijnen JH, Schinkel AH.

Cancer Res. 2009 Dec 1;69(23):8996-9002. doi: 10.1158/0008-5472.CAN-09-2915. Epub 2009 Nov 17.

46.

Functionally overlapping roles of Abcg2 (Bcrp1) and Abcc2 (Mrp2) in the elimination of methotrexate and its main toxic metabolite 7-hydroxymethotrexate in vivo.

Vlaming ML, Pala Z, van Esch A, Wagenaar E, de Waart DR, van de Wetering K, van der Kruijssen CM, Oude Elferink RP, van Tellingen O, Schinkel AH.

Clin Cancer Res. 2009 May 1;15(9):3084-93. doi: 10.1158/1078-0432.CCR-08-2940. Epub 2009 Apr 21.

47.

Impact of Abcc2 (Mrp2) and Abcc3 (Mrp3) on the in vivo elimination of methotrexate and its main toxic metabolite 7-hydroxymethotrexate.

Vlaming ML, Pala Z, van Esch A, Wagenaar E, van Tellingen O, de Waart DR, Oude Elferink RP, van de Wetering K, Schinkel AH.

Clin Cancer Res. 2008 Dec 15;14(24):8152-60. doi: 10.1158/1078-0432.CCR-08-1609.

48.

Methotrexate pharmacokinetics in transgenic mice with liver-specific expression of human organic anion-transporting polypeptide 1B1 (SLCO1B1).

van de Steeg E, van der Kruijssen CM, Wagenaar E, Burggraaff JE, Mesman E, Kenworthy KE, Schinkel AH.

Drug Metab Dispos. 2009 Feb;37(2):277-81. doi: 10.1124/dmd.108.024315. Epub 2008 Nov 20.

49.

Intestinal cytochrome P450 3A plays an important role in the regulation of detoxifying systems in the liver.

van Waterschoot RA, Rooswinkel RW, Wagenaar E, van der Kruijssen CM, van Herwaarden AE, Schinkel AH.

FASEB J. 2009 Jan;23(1):224-31. doi: 10.1096/fj.08-114876. Epub 2008 Sep 15.

PMID:
18794335
50.

P-glycoprotein limits oral availability, brain penetration, and toxicity of an anionic drug, the antibiotic salinomycin.

Lagas JS, Sparidans RW, van Waterschoot RA, Wagenaar E, Beijnen JH, Schinkel AH.

Antimicrob Agents Chemother. 2008 Mar;52(3):1034-9. doi: 10.1128/AAC.01041-07. Epub 2008 Jan 14.

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