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Multidrug transporters: recent insights from cryo-electron microscopy-derived atomic structures and animal models.

Lusvarghi S, Robey RW, Gottesman MM, Ambudkar SV.

F1000Res. 2020 Jan 13;9. pii: F1000 Faculty Rev-17. doi: 10.12688/f1000research.21295.1. eCollection 2020. Review.


A role for ceramide glycosylation in resistance to oxaliplatin in colorectal cancer.

Madigan JP, Robey RW, Poprawski JE, Huang H, Clarke CJ, Gottesman MM, Cabot MC, Rosenberg DW.

Exp Cell Res. 2020 Mar 15;388(2):111860. doi: 10.1016/j.yexcr.2020.111860. Epub 2020 Jan 20.


Mycoplasma Infection Mediates Sensitivity of Multidrug-Resistant Cell Lines to Tiopronin: A Cautionary Tale.

Huff LM, Horibata S, Robey RW, Hall MD, Gottesman MM.

J Med Chem. 2020 Feb 13;63(3):1434-1439. doi: 10.1021/acs.jmedchem.9b00484. Epub 2020 Feb 4.


A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.

Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD.

Mol Pharmacol. 2019 Nov;96(5):629-640. doi: 10.1124/mol.119.115964. Epub 2019 Sep 12.


Model systems for studying the blood-brain barrier: Applications and challenges.

Jackson S, Meeks C, Vézina A, Robey RW, Tanner K, Gottesman MM.

Biomaterials. 2019 Sep;214:119217. doi: 10.1016/j.biomaterials.2019.05.028. Epub 2019 May 18. Review.


Porphyrin-lipid assemblies and nanovesicles overcome ABC transporter-mediated photodynamic therapy resistance in cancer cells.

Baglo Y, Liang BJ, Robey RW, Ambudkar SV, Gottesman MM, Huang HC.

Cancer Lett. 2019 Aug 10;457:110-118. doi: 10.1016/j.canlet.2019.04.037. Epub 2019 May 6.


Coexpression of ABCB1 and ABCG2 in a Cell Line Model Reveals Both Independent and Additive Transporter Function.

Robinson AN, Tebase BG, Francone SC, Huff LM, Kozlowski H, Cossari D, Lee JM, Esposito D, Robey RW, Gottesman MM.

Drug Metab Dispos. 2019 Jul;47(7):715-723. doi: 10.1124/dmd.118.086181. Epub 2019 May 2.


Spatial control of oxygen delivery to three-dimensional cultures alters cancer cell growth and gene expression.

Wulftange WJ, Rose MA, Garmendia-Cedillos M, da Silva D, Poprawski JE, Srinivasachar D, Sullivan T, Lim L, Bliskovsky VV, Hall MD, Pohida TJ, Robey RW, Morgan NY, Gottesman MM.

J Cell Physiol. 2019 Nov;234(11):20608-20622. doi: 10.1002/jcp.28665. Epub 2019 Apr 22.


Targeting mitochondrial hexokinases increases efficacy of histone deacetylase inhibitors in solid tumor models.

McDonald AJ, Curt KM, Patel RP, Kozlowski H, Sackett DL, Robey RW, Gottesman MM, Bates SE.

Exp Cell Res. 2019 Feb 15;375(2):106-112. doi: 10.1016/j.yexcr.2018.12.012. Epub 2018 Dec 21.


Bax/Tubulin/Epithelial-Mesenchymal Pathways Determine the Efficacy of Silybin Analog HM015k in Colorectal Cancer Cell Growth and Metastasis.

Amawi H, Hussein NA, Ashby CR Jr, Alnafisah R, Sanglard LM, Manivannan E, Karthikeyan C, Trivedi P, Eisenmann KM, Robey RW, Tiwari AK.

Front Pharmacol. 2018 May 23;9:520. doi: 10.3389/fphar.2018.00520. eCollection 2018.


Revisiting the role of ABC transporters in multidrug-resistant cancer.

Robey RW, Pluchino KM, Hall MD, Fojo AT, Bates SE, Gottesman MM.

Nat Rev Cancer. 2018 Jul;18(7):452-464. doi: 10.1038/s41568-018-0005-8. Review.


Pancreatic Cancer: "A Riddle Wrapped in a Mystery inside an Enigma".

Borazanci E, Dang CV, Robey RW, Bates SE, Chabot JA, Von Hoff DD.

Clin Cancer Res. 2017 Apr 1;23(7):1629-1637. doi: 10.1158/1078-0432.CCR-16-2070. Review.


Blocking downstream signaling pathways in the context of HDAC inhibition promotes apoptosis preferentially in cells harboring mutant Ras.

Bahr JC, Robey RW, Luchenko V, Basseville A, Chakraborty AR, Kozlowski H, Pauly GT, Patel P, Schneider JP, Gottesman MM, Bates SE.

Oncotarget. 2016 Oct 25;7(43):69804-69815. doi: 10.18632/oncotarget.12001.


The linker region of breast cancer resistance protein ABCG2 is critical for coupling of ATP-dependent drug transport.

Macalou S, Robey RW, Jabor Gozzi G, Shukla S, Grosjean I, Hegedus T, Ambudkar SV, Bates SE, Di Pietro A.

Cell Mol Life Sci. 2016 May;73(9):1927-37. doi: 10.1007/s00018-015-2118-5. Epub 2015 Dec 26.


CCR 20th Anniversary Commentary: Expanding the Epigenetic Therapeutic Portfolio.

Bates SE, Robey RW, Piekarz RL.

Clin Cancer Res. 2015 May 15;21(10):2195-7. doi: 10.1158/1078-0432.CCR-14-2555.


Icotinib antagonizes ABCG2-mediated multidrug resistance, but not the pemetrexed resistance mediated by thymidylate synthase and ABCG2.

Wang DS, Patel A, Shukla S, Zhang YK, Wang YJ, Kathawala RJ, Robey RW, Zhang L, Yang DH, Talele TT, Bates SE, Ambudkar SV, Xu RH, Chen ZS.

Oncotarget. 2014 Jun 30;5(12):4529-42.


Histone deacetylase inhibitor-mediated cell death is distinct from its global effect on chromatin.

Luchenko VL, Litman T, Chakraborty AR, Heffner A, Devor C, Wilkerson J, Stein W, Robey RW, Bangiolo L, Levens D, Bates SE.

Mol Oncol. 2014 Dec;8(8):1379-92. doi: 10.1016/j.molonc.2014.05.001. Epub 2014 May 28.


Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance.

Zhang H, Kathawala RJ, Wang YJ, Zhang YK, Patel A, Shukla S, Robey RW, Talele TT, Ashby CR Jr, Ambudkar SV, Bates SE, Fu LW, Chen ZS.

Int J Biochem Cell Biol. 2014 Jun;51:111-9. doi: 10.1016/j.biocel.2014.03.026. Epub 2014 Apr 12.


Assessment of drug transporter function using fluorescent cell imaging.

Bircsak KM, Gibson CJ, Robey RW, Aleksunes LM.

Curr Protoc Toxicol. 2013 Sep 23;57:Unit 23.6.. doi: 10.1002/0471140856.tx2306s57.


Loss of the proteins Bak and Bax prevents apoptosis mediated by histone deacetylase inhibitors.

Ierano C, Chakraborty AR, Nicolae A, Bahr JC, Zhan Z, Pittaluga S, Bates SE, Robey RW.

Cell Cycle. 2013 Sep 1;12(17):2829-38. doi: 10.4161/cc.25914. Epub 2013 Aug 7.


Overlapping substrate and inhibitor specificity of human and murine ABCG2.

Bakhsheshian J, Hall MD, Robey RW, Herrmann MA, Chen JQ, Bates SE, Gottesman MM.

Drug Metab Dispos. 2013 Oct;41(10):1805-12. doi: 10.1124/dmd.113.053140. Epub 2013 Jul 18.


MAPK pathway activation leads to Bim loss and histone deacetylase inhibitor resistance: rationale to combine romidepsin with an MEK inhibitor.

Chakraborty AR, Robey RW, Luchenko VL, Zhan Z, Piekarz RL, Gillet JP, Kossenkov AV, Wilkerson J, Showe LC, Gottesman MM, Collie NL, Bates SE.

Blood. 2013 May 16;121(20):4115-25. doi: 10.1182/blood-2012-08-449140. Epub 2013 Mar 26.


Histone deacetylase inhibitors induce CXCR4 mRNA but antagonize CXCR4 migration.

Ierano C, Basseville A, To KK, Zhan Z, Robey RW, Wilkerson J, Bates SE, Scala S.

Cancer Biol Ther. 2013 Feb;14(2):175-83. doi: 10.4161/cbt.22957. Epub 2012 Nov 28.


HG-829 is a potent noncompetitive inhibitor of the ATP-binding cassette multidrug resistance transporter ABCB1.

Caceres G, Robey RW, Sokol L, McGraw KL, Clark J, Lawrence NJ, Sebti SM, Wiese M, List AF.

Cancer Res. 2012 Aug 15;72(16):4204-13. doi: 10.1158/0008-5472.CAN-12-0743. Epub 2012 Jul 3.


Histone deacetylase inhibitors influence chemotherapy transport by modulating expression and trafficking of a common polymorphic variant of the ABCG2 efflux transporter.

Basseville A, Tamaki A, Ierano C, Trostel S, Ward Y, Robey RW, Hegde RS, Bates SE.

Cancer Res. 2012 Jul 15;72(14):3642-51. doi: 10.1158/0008-5472.CAN-11-2008. Epub 2012 Apr 3.


A pharmacodynamic study of the P-glycoprotein antagonist CBT-1® in combination with paclitaxel in solid tumors.

Kelly RJ, Robey RW, Chen CC, Draper D, Luchenko V, Barnett D, Oldham RK, Caluag Z, Frye AR, Steinberg SM, Fojo T, Bates SE.

Oncologist. 2012;17(4):512. doi: 10.1634/theoncologist.2012-0080. Epub 2012 Mar 13.


The controversial role of ABC transporters in clinical oncology.

Tamaki A, Ierano C, Szakacs G, Robey RW, Bates SE.

Essays Biochem. 2011 Sep 7;50(1):209-32. doi: 10.1042/bse0500209. Review.


Histone deacetylase inhibitors: emerging mechanisms of resistance.

Robey RW, Chakraborty AR, Basseville A, Luchenko V, Bahr J, Zhan Z, Bates SE.

Mol Pharm. 2011 Dec 5;8(6):2021-31. doi: 10.1021/mp200329f. Epub 2011 Oct 7. Review.


Sildenafil reverses ABCB1- and ABCG2-mediated chemotherapeutic drug resistance.

Shi Z, Tiwari AK, Shukla S, Robey RW, Singh S, Kim IW, Bates SE, Peng X, Abraham I, Ambudkar SV, Talele TT, Fu LW, Chen ZS.

Cancer Res. 2011 Apr 15;71(8):3029-41. doi: 10.1158/0008-5472.CAN-10-3820. Epub 2011 Mar 14.


ABC transporters: unvalidated therapeutic targets in cancer and the CNS.

Robey RW, Massey PR, Amiri-Kordestani L, Bates SE.

Anticancer Agents Med Chem. 2010 Oct 1;10(8):625-33. Review.


The challenge of exploiting ABCG2 in the clinic.

Robey RW, Ierano C, Zhan Z, Bates SE.

Curr Pharm Biotechnol. 2011 Apr;12(4):595-608. Review.


Rapid detection of ABC transporter interaction: potential utility in pharmacology.

Robey RW, Lin B, Qiu J, Chan LL, Bates SE.

J Pharmacol Toxicol Methods. 2011 May-Jun;63(3):217-22. doi: 10.1016/j.vascn.2010.11.003. Epub 2010 Nov 25.


A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer.

Kelly RJ, Draper D, Chen CC, Robey RW, Figg WD, Piekarz RL, Chen X, Gardner ER, Balis FM, Venkatesan AM, Steinberg SM, Fojo T, Bates SE.

Clin Cancer Res. 2011 Feb 1;17(3):569-80. doi: 10.1158/1078-0432.CCR-10-1725. Epub 2010 Nov 16.


Romidepsin: a new therapy for cutaneous T-cell lymphoma and a potential therapy for solid tumors.

Grant C, Rahman F, Piekarz R, Peer C, Frye R, Robey RW, Gardner ER, Figg WD, Bates SE.

Expert Rev Anticancer Ther. 2010 Jul;10(7):997-1008. doi: 10.1586/era.10.88. Review. Erratum in: Expert Rev Anticancer Ther. 2011 Oct;11(10):1622.


Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib.

Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE.

Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27.


Mutational analysis of threonine 402 adjacent to the GXXXG dimerization motif in transmembrane segment 1 of ABCG2.

Polgar O, Ierano C, Tamaki A, Stanley B, Ward Y, Xia D, Tarasova N, Robey RW, Bates SE.

Biochemistry. 2010 Mar 16;49(10):2235-45. doi: 10.1021/bi902085q.


Laboratory correlates for a phase II trial of romidepsin in cutaneous and peripheral T-cell lymphoma.

Bates SE, Zhan Z, Steadman K, Obrzut T, Luchenko V, Frye R, Robey RW, Turner M, Gardner ER, Figg WD, Steinberg SM, Ling A, Fojo T, To KW, Piekarz RL.

Br J Haematol. 2010 Jan;148(2):256-67. doi: 10.1111/j.1365-2141.2009.07954.x. Epub 2009 Oct 28.


Escape from hsa-miR-519c enables drug-resistant cells to maintain high expression of ABCG2.

To KK, Robey RW, Knutsen T, Zhan Z, Ried T, Bates SE.

Mol Cancer Ther. 2009 Oct;8(10):2959-68. doi: 10.1158/1535-7163.MCT-09-0292.


Identification of compounds that correlate with ABCG2 transporter function in the National Cancer Institute Anticancer Drug Screen.

Deeken JF, Robey RW, Shukla S, Steadman K, Chakraborty AR, Poonkuzhali B, Schuetz EG, Holbeck S, Ambudkar SV, Bates SE.

Mol Pharmacol. 2009 Nov;76(5):946-56. doi: 10.1124/mol.109.056192. Epub 2009 Jul 24.


Botryllamides: natural product inhibitors of ABCG2.

Henrich CJ, Robey RW, Takada K, Bokesch HR, Bates SE, Shukla S, Ambudkar SV, McMahon JB, Gustafson KR.

ACS Chem Biol. 2009 Aug 21;4(8):637-47. doi: 10.1021/cb900134c.


Arginine 383 is a crucial residue in ABCG2 biogenesis.

Polgar O, Ediriwickrema LS, Robey RW, Sharma A, Hegde RS, Li Y, Xia D, Ward Y, Dean M, Ozvegy-Laczka C, Sarkadi B, Bates SE.

Biochim Biophys Acta. 2009 Jul;1788(7):1434-43. doi: 10.1016/j.bbamem.2009.04.016. Epub 2009 May 3.


The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance.

Shi Z, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS.

Oncol Rep. 2009 Feb;21(2):483-9.


ABCG2: a perspective.

Robey RW, To KK, Polgar O, Dohse M, Fetsch P, Dean M, Bates SE.

Adv Drug Deliv Rev. 2009 Jan 31;61(1):3-13. doi: 10.1016/j.addr.2008.11.003. Epub 2008 Dec 16. Review.


Becatecarin (rebeccamycin analog, NSC 655649) is a transport substrate and induces expression of the ATP-binding cassette transporter, ABCG2, in lung carcinoma cells.

Robey RW, Obrzut T, Shukla S, Polgar O, Macalou S, Bahr JC, Di Pietro A, Ambudkar SV, Bates SE.

Cancer Chemother Pharmacol. 2009 Aug;64(3):575-83. doi: 10.1007/s00280-008-0908-2. Epub 2009 Jan 9.


Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478.

Shi Z, Tiwari AK, Shukla S, Robey RW, Kim IW, Parmar S, Bates SE, Si QS, Goldblatt CS, Abraham I, Fu LW, Ambudkar SV, Chen ZS.

Biochem Pharmacol. 2009 Mar 1;77(5):781-93. doi: 10.1016/j.bcp.2008.11.007. Epub 2008 Nov 18.


ABCG2 is expressed in late spermatogenesis and is associated with the acrosome.

Scharenberg C, Mannowetz N, Robey RW, Brendel C, Repges P, Sahrhage T, Jähn T, Wennemuth G.

Biochem Biophys Res Commun. 2009 Jan 9;378(2):302-7. doi: 10.1016/j.bbrc.2008.11.058. Epub 2008 Nov 24.


The 315-316 deletion determines the BXP-21 antibody epitope but has no effect on the function of wild type ABCG2 or the Q141K variant.

Polgar O, Deeken JF, Ediriwickrema LS, Tamaki A, Steinberg SM, Robey RW, Bates SE.

Mol Cell Biochem. 2009 Feb;322(1-2):63-71. doi: 10.1007/s11010-008-9940-0. Epub 2008 Nov 11.


Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2.

Shukla S, Robey RW, Bates SE, Ambudkar SV.

Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29.


Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2.

Dai CL, Tiwari AK, Wu CP, Su XD, Wang SR, Liu DG, Ashby CR Jr, Huang Y, Robey RW, Liang YJ, Chen LM, Shi CJ, Ambudkar SV, Chen ZS, Fu LW.

Cancer Res. 2008 Oct 1;68(19):7905-14. doi: 10.1158/0008-5472.CAN-08-0499. Erratum in: Cancer Res. 2008 Dec 15;68(24):10387.


Association of the ABCG2 C421A polymorphism with prostate cancer risk and survival.

Gardner ER, Ahlers CM, Shukla S, Sissung TM, Ockers SB, Price DK, Hamada A, Robey RW, Steinberg SM, Ambudkar SV, Dahut WL, Figg WD.

BJU Int. 2008 Dec;102(11):1694-9. doi: 10.1111/j.1464-410X.2008.07913.x. Epub 2008 Aug 14.

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