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Items: 1 to 50 of 114


Mechanistic Insights of Phenobarbital-Mediated Activation of Human but Not Mouse Pregnane X Receptor.

Li L, Welch MA, Li Z, Mackowiak B, Heyward S, Swaan PW, Wang H.

Mol Pharmacol. 2019 Sep;96(3):345-354. doi: 10.1124/mol.119.116616. Epub 2019 Jul 10.


Tyrosine Phosphorylation Regulates Plasma Membrane Expression and Stability of the Human Bile Acid Transporter ASBT (SLC10A2).

Chothe PP, Czuba LC, Ayewoh EN, Swaan PW.

Mol Pharm. 2019 Aug 5;16(8):3569-3576. doi: 10.1021/acs.molpharmaceut.9b00426. Epub 2019 Jul 8.


Molecular Modeling of Drug-Transporter Interactions-An International Transporter Consortium Perspective.

Schlessinger A, Welch MA, van Vlijmen H, Korzekwa K, Swaan PW, Matsson P.

Clin Pharmacol Ther. 2018 Nov;104(5):818-835. doi: 10.1002/cpt.1174. Epub 2018 Aug 30. Review.


Post-translational modifications of transporters.

Czuba LC, Hillgren KM, Swaan PW.

Pharmacol Ther. 2018 Dec;192:88-99. doi: 10.1016/j.pharmthera.2018.06.013. Epub 2018 Jun 30. Review.


Human bile acid transporter ASBT (SLC10A2) forms functional non-covalent homodimers and higher order oligomers.

Chothe PP, Czuba LC, Moore RH, Swaan PW.

Biochim Biophys Acta Biomembr. 2018 Mar;1860(3):645-653. doi: 10.1016/j.bbamem.2017.11.016. Epub 2017 Dec 1.


Planar bile acids in health and disease.

Shiffka SJ, Kane MA, Swaan PW.

Biochim Biophys Acta Biomembr. 2017 Nov;1859(11):2269-2276. doi: 10.1016/j.bbamem.2017.08.019. Epub 2017 Sep 6. Review.


Molecular Basis of Metabolism-Mediated Conversion of PK11195 from an Antagonist to an Agonist of the Constitutive Androstane Receptor.

Mackowiak B, Li L, Welch MA, Li D, Jones JW, Heyward S, Kane MA, Swaan PW, Wang H.

Mol Pharmacol. 2017 Jul;92(1):75-87. doi: 10.1124/mol.117.108621. Epub 2017 Apr 25.


Identification of novel MRP3 inhibitors based on computational models and validation using an in vitro membrane vesicle assay.

Ali I, Welch MA, Lu Y, Swaan PW, Brouwer KLR.

Eur J Pharm Sci. 2017 May 30;103:52-59. doi: 10.1016/j.ejps.2017.02.011. Epub 2017 Feb 24.


Potent and Selective Inhibition of Plasma Membrane Monoamine Transporter by HIV Protease Inhibitors.

Duan H, Hu T, Foti RS, Pan Y, Swaan PW, Wang J.

Drug Metab Dispos. 2015 Nov;43(11):1773-80. doi: 10.1124/dmd.115.064824. Epub 2015 Aug 18.


Obituary: Paul M. Bummer (1955 - 2015).

Swaan PW.

Pharm Res. 2015 Sep;32(9):2813. doi: 10.1007/s11095-015-1757-4. No abstract available.


Internalization and Subcellular Trafficking of Poly-l-lysine Dendrimers Are Impacted by the Site of Fluorophore Conjugation.

Avaritt BR, Swaan PW.

Mol Pharm. 2015 Jun 1;12(6):1961-9. doi: 10.1021/mp500765e. Epub 2015 May 19.


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.


Activation of the constitutive androstane receptor inhibits gluconeogenesis without affecting lipogenesis or fatty acid synthesis in human hepatocytes.

Lynch C, Pan Y, Li L, Heyward S, Moeller T, Swaan PW, Wang H.

Toxicol Appl Pharmacol. 2014 Aug 15;279(1):33-42. doi: 10.1016/j.taap.2014.05.009. Epub 2014 May 27.


Intracellular Ca2+ release mediates cationic but not anionic poly(amidoamine) (PAMAM) dendrimer-induced tight junction modulation.

Avaritt BR, Swaan PW.

Pharm Res. 2014 Sep;31(9):2429-38. doi: 10.1007/s11095-014-1338-y. Epub 2014 Mar 20.


The role of transporters in toxicity and disease.

Schuetz JD, Swaan PW, Tweedie DJ.

Drug Metab Dispos. 2014 Apr;42(4):541-5. doi: 10.1124/dmd.114.057539. Review.


Resveratrol promotes degradation of the human bile acid transporter ASBT (SLC10A2).

Chothe PP, Swaan PW.

Biochem J. 2014 Apr 15;459(2):301-12. doi: 10.1042/BJ20131428.


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.


Microfluidic preparation of liposomes to determine particle size influence on cellular uptake mechanisms.

Andar AU, Hood RR, Vreeland WN, Devoe DL, Swaan PW.

Pharm Res. 2014 Feb;31(2):401-13. doi: 10.1007/s11095-013-1171-8. Epub 2013 Oct 3.


Transmembrane domain II of the human bile acid transporter SLC10A2 coordinates sodium translocation.

Sabit H, Mallajosyula SS, MacKerell AD Jr, Swaan PW.

J Biol Chem. 2013 Nov 8;288(45):32394-404. doi: 10.1074/jbc.M113.518555. Epub 2013 Sep 17.


Transmembrane domain V plays a stabilizing role in the function of human bile acid transporter SLC10A2.

Moore RH, Chothe P, Swaan PW.

Biochemistry. 2013 Jul 30;52(30):5117-24. doi: 10.1021/bi400028q. Epub 2013 Jul 16.


ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans.

Zamek-Gliszczynski MJ, Lee CA, Poirier A, Bentz J, Chu X, Ellens H, Ishikawa T, Jamei M, Kalvass JC, Nagar S, Pang KS, Korzekwa K, Swaan PW, Taub ME, Zhao P, Galetin A; International Transporter Consortium.

Clin Pharmacol Ther. 2013 Jul;94(1):64-79. doi: 10.1038/clpt.2013.45. Epub 2013 Feb 25. Review.


Riboflavin-targeted polymer conjugates for breast tumor delivery.

Bareford LM, Avaritt BR, Ghandehari H, Nan A, Swaan PW.

Pharm Res. 2013 Jul;30(7):1799-812. doi: 10.1007/s11095-013-1024-5. Epub 2013 Apr 9.


The solute carrier family 10 (SLC10): beyond bile acid transport.

Claro da Silva T, Polli JE, Swaan PW.

Mol Aspects Med. 2013 Apr-Jun;34(2-3):252-69. doi: 10.1016/j.mam.2012.07.004. Review.


Identification of novel breast cancer resistance protein (BCRP) inhibitors by virtual screening.

Pan Y, Chothe PP, Swaan PW.

Mol Pharm. 2013 Apr 1;10(4):1236-48. doi: 10.1021/mp300547h. Epub 2013 Mar 21.


Identification of novel activators of constitutive androstane receptor from FDA-approved drugs by integrated computational and biological approaches.

Lynch C, Pan Y, Li L, Ferguson SS, Xia M, Swaan PW, Wang H.

Pharm Res. 2013 Feb;30(2):489-501. doi: 10.1007/s11095-012-0895-1. Epub 2012 Oct 23.


Computational modeling to accelerate the identification of substrates and inhibitors for transporters that affect drug disposition.

Ekins S, Polli JE, Swaan PW, Wright SH.

Clin Pharmacol Ther. 2012 Nov;92(5):661-5. doi: 10.1038/clpt.2012.164. Epub 2012 Sep 26. No abstract available.


Putative irreversible inhibitors of the human sodium-dependent bile acid transporter (hASBT; SLC10A2) support the role of transmembrane domain 7 in substrate binding/translocation.

González PM, Hussainzada N, Swaan PW, Mackerell AD Jr, Polli JE.

Pharm Res. 2012 Jul;29(7):1821-31. doi: 10.1007/s11095-012-0706-8. Epub 2012 Feb 22.


Molecular analysis and structure-activity relationship modeling of the substrate/inhibitor interaction site of plasma membrane monoamine transporter.

Ho HT, Pan Y, Cui Z, Duan H, Swaan PW, Wang J.

J Pharmacol Exp Ther. 2011 Nov;339(2):376-85. doi: 10.1124/jpet.111.184036. Epub 2011 Aug 4.


Transmembrane helix 1 contributes to substrate translocation and protein stability of bile acid transporter SLC10A2.

da Silva TC, Hussainzada N, Khantwal CM, Polli JE, Swaan PW.

J Biol Chem. 2011 Aug 5;286(31):27322-32. doi: 10.1074/jbc.M110.217802. Epub 2011 Jun 6.


ATP-binding cassette transporter expression in human placenta as a function of pregnancy condition.

Mason CW, Buhimschi IA, Buhimschi CS, Dong Y, Weiner CP, Swaan PW.

Drug Metab Dispos. 2011 Jun;39(6):1000-7. doi: 10.1124/dmd.111.038166. Epub 2011 Mar 23.


G3.5 PAMAM dendrimers enhance transepithelial transport of SN38 while minimizing gastrointestinal toxicity.

Goldberg DS, Vijayalakshmi N, Swaan PW, Ghandehari H.

J Control Release. 2011 Mar 30;150(3):318-25. doi: 10.1016/j.jconrel.2010.11.022. Epub 2010 Nov 27.


Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening.

Pan Y, Li L, Kim G, Ekins S, Wang H, Swaan PW.

Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10. Erratum in: Drug Metab Dispos. 2012 Sep;40(9):1868.


Structural requirements of the ASBT by 3D-QSAR analysis using aminopyridine conjugates of chenodeoxycholic acid.

Zheng X, Pan Y, Acharya C, Swaan PW, Polli JE.

Bioconjug Chem. 2010 Nov 17;21(11):2038-48. doi: 10.1021/bc100273w. Epub 2010 Oct 22.


Publication ethics--a guide for submitting manuscripts to Pharmaceutical Research.

Swaan PW.

Pharm Res. 2010 Sep;27(9):1757-8. doi: 10.1007/s11095-010-0188-5. Epub 2010 Jun 15. No abstract available.


Human effector/initiator gene sets that regulate myometrial contractility during term and preterm labor.

Weiner CP, Mason CW, Dong Y, Buhimschi IA, Swaan PW, Buhimschi CS.

Am J Obstet Gynecol. 2010 May;202(5):474.e1-20. doi: 10.1016/j.ajog.2010.02.034.


Targeting drug transporters - combining in silico and in vitro approaches to predict in vivo.

Bahadduri PM, Polli JE, Swaan PW, Ekins S.

Methods Mol Biol. 2010;637:65-103. doi: 10.1007/978-1-60761-700-6_4.


Cellular entry of G3.5 poly (amido amine) dendrimers by clathrin- and dynamin-dependent endocytosis promotes tight junctional opening in intestinal epithelia.

Goldberg DS, Ghandehari H, Swaan PW.

Pharm Res. 2010 Aug;27(8):1547-57. doi: 10.1007/s11095-010-0153-3. Epub 2010 Apr 22.


Membrane transporters in drug development.

International Transporter Consortium, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L.

Nat Rev Drug Discov. 2010 Mar;9(3):215-36. doi: 10.1038/nrd3028. Review.


The ethanol metabolite acetaldehyde increases paracellular drug permeability in vitro and oral bioavailability in vivo.

Fisher SJ, Swaan PW, Eddington ND.

J Pharmacol Exp Ther. 2010 Jan;332(1):326-33. doi: 10.1124/jpet.109.158642. Epub 2009 Oct 9.


The cytosolic half of helix III forms the substrate exit route during permeation events of the sodium/bile acid cotransporter ASBT.

Hussainzada N, Claro Da Silva T, Swaan PW.

Biochemistry. 2009 Sep 15;48(36):8528-39. doi: 10.1021/bi900616w.


Science beyond impact factors.

Swaan PW.

Pharm Res. 2009 Apr;26(4):743-5. doi: 10.1007/s11095-009-9856-8. Epub 2009 Feb 18. No abstract available.


Pharmaceutical research-looking ahead.

Swaan PW.

Pharm Res. 2009 Mar;26(3):491. doi: 10.1007/s11095-009-9836-z. Epub 2009 Jan 22. No abstract available.


Intracellular processing of riboflavin in human breast cancer cells.

Bareford LM, Phelps MA, Foraker AB, Swaan PW.

Mol Pharm. 2008 Sep-Oct;5(5):839-48. doi: 10.1021/mp800046m. Epub 2008 Aug 29.


Machine learning methods and docking for predicting human pregnane X receptor activation.

Khandelwal A, Krasowski MD, Reschly EJ, Sinz MW, Swaan PW, Ekins S.

Chem Res Toxicol. 2008 Jul;21(7):1457-67. doi: 10.1021/tx800102e. Epub 2008 Jun 12.


Conserved aspartic acid residues lining the extracellular loop 1 of sodium-coupled bile acid transporter ASBT Interact with Na+ and 7alpha-OH moieties on the ligand cholestane skeleton.

Hussainzada N, Da Silva TC, Zhang EY, Swaan PW.

J Biol Chem. 2008 Jul 25;283(30):20653-63. doi: 10.1074/jbc.M802885200. Epub 2008 May 28.


Bacterial peptide recognition and immune activation facilitated by human peptide transporter PEPT2.

Swaan PW, Bensman T, Bahadduri PM, Hall MW, Sarkar A, Bao S, Khantwal CM, Ekins S, Knoell DL.

Am J Respir Cell Mol Biol. 2008 Nov;39(5):536-42. doi: 10.1165/rcmb.2008-0059OC. Epub 2008 May 12.


Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1).

Bahadduri PM, Ray A, Khandelwal A, Swaan PW.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2555-7. doi: 10.1016/j.bmcl.2008.03.044. Epub 2008 Mar 20.


Cytosolic half of transmembrane domain IV of the human bile acid transporter hASBT (SLC10A2) forms part of the substrate translocation pathway.

Khantwal CM, Swaan PW.

Biochemistry. 2008 Mar 25;47(12):3606-14. doi: 10.1021/bi702498w. Epub 2008 Mar 1.


Design, synthesis, cytoselective toxicity, structure-activity relationships, and pharmacophore of thiazolidinone derivatives targeting drug-resistant lung cancer cells.

Zhou H, Wu S, Zhai S, Liu A, Sun Y, Li R, Zhang Y, Ekins S, Swaan PW, Fang B, Zhang B, Yan B.

J Med Chem. 2008 Mar 13;51(5):1242-51. doi: 10.1021/jm7012024. Epub 2008 Feb 8.


Multi-level analysis of organic anion transporters 1, 3, and 6 reveals major differences in structural determinants of antiviral discrimination.

Truong DM, Kaler G, Khandelwal A, Swaan PW, Nigam SK.

J Biol Chem. 2008 Mar 28;283(13):8654-63. doi: 10.1074/jbc.M708615200. Epub 2008 Jan 3.

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