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Tivantinib, A c-Met Inhibitor in Clinical Trials, Is Susceptible to ABCG2-Mediated Drug Resistance.

Wu ZX, Yang Y, Teng QX, Wang JQ, Lei ZN, Wang JQ, Lusvarghi S, Ambudkar SV, Yang DH, Chen ZS.

Cancers (Basel). 2020 Jan 12;12(1). pii: E186. doi: 10.3390/cancers12010186.


The Selective Class IIa Histone Deacetylase Inhibitor TMP195 Resensitizes ABCB1- and ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Cytotoxic Anticancer Drugs.

Wu CP, Lusvarghi S, Wang JC, Hsiao SH, Huang YH, Hung TH, Ambudkar SV.

Int J Mol Sci. 2019 Dec 29;21(1). pii: E238. doi: 10.3390/ijms21010238.


ATP-dependent thermostabilization of human P-glycoprotein (ABCB1) is blocked by modulators.

Lusvarghi S, Ambudkar SV.

Biochem J. 2019 Dec 19;476(24):3737-3750. doi: 10.1042/BCJ20190736.


Nonsynonymous Mutations in Linker-2 of the Pdr5 Multidrug Transporter Identify a New RNA Stability Element.

Rahman H, Rudrow A, Carneglia J, Joly SSP, Nicotera D, Naldrett M, Choy J, Ambudkar SV, Golin J.

G3 (Bethesda). 2020 Jan 7;10(1):357-369. doi: 10.1534/g3.119.400863.


ABC Transporter-Mediated Multidrug-Resistant Cancer.

Amawi H, Sim HM, Tiwari AK, Ambudkar SV, Shukla S.

Adv Exp Med Biol. 2019;1141:549-580. doi: 10.1007/978-981-13-7647-4_12. Review.


ABC-transporter upregulation mediates resistance to the CDK7 inhibitors THZ1 and ICEC0942.

Sava GP, Fan H, Fisher RA, Lusvarghi S, Pancholi S, Ambudkar SV, Martin LA, Charles Coombes R, Buluwela L, Ali S.

Oncogene. 2020 Jan;39(3):651-663. doi: 10.1038/s41388-019-1008-y. Epub 2019 Sep 17.


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.


Synthesis and Characterization of Bodipy-FL-Cyclosporine A as a Substrate for Multidrug Resistance-Linked P-Glycoprotein (ABCB1).

Sajid A, Raju N, Lusvarghi S, Vahedi S, Swenson RE, Ambudkar SV.

Drug Metab Dispos. 2019 Oct;47(10):1013-1023. doi: 10.1124/dmd.119.087734. Epub 2019 Aug 1.


An A666G mutation in transmembrane helix 5 of the yeast multidrug transporter Pdr5 increases drug efflux by enhancing cooperativity between transport sites.

Arya N, Rahman H, Rudrow A, Wagner M, Schmitt L, Ambudkar SV, Golin J.

Mol Microbiol. 2019 Oct;112(4):1131-1144. doi: 10.1111/mmi.14351. Epub 2019 Jul 23.


Evidence for the Interaction of A3 Adenosine Receptor Agonists at the Drug-Binding Site(s) of Human P-glycoprotein (ABCB1).

Abel B, Tosh DK, Durell SR, Murakami M, Vahedi S, Jacobson KA, Ambudkar SV.

Mol Pharmacol. 2019 Aug;96(2):180-192. doi: 10.1124/mol.118.115295. Epub 2019 May 24.


Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-Mediated Multidrug Resistance in Cancer Cell Lines.

Wu CP, Lusvarghi S, Wang JC, Hsiao SH, Huang YH, Hung TH, Ambudkar SV.

Mol Pharm. 2019 Jul 1;16(7):3040-3052. doi: 10.1021/acs.molpharmaceut.9b00274. Epub 2019 Jun 4.


Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated Multidrug Resistance in Cancer Cells.

Cui Q, Cai CY, Gao HL, Ren L, Ji N, Gupta P, Yang Y, Shukla S, Ambudkar SV, Yang DH, Chen ZS.

Front Oncol. 2019 Apr 25;9:313. doi: 10.3389/fonc.2019.00313. eCollection 2019.


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.


Exome Sequencing of ABCB5 Identifies Recurrent Melanoma Mutations that Result in Increased Proliferative and Invasive Capacities.

Sana G, Madigan JP, Gartner JJ, Fourrez M, Lin J, Qutob N, Narayan J, Shukla S, Ambudkar SV, Xia D, Rosenberg SA, Gottesman MM, Samuels Y, Gillet JP.

J Invest Dermatol. 2019 Sep;139(9):1985-1992.e10. doi: 10.1016/j.jid.2019.01.036. Epub 2019 Mar 21.


Large-scale purification of functional human P-glycoprotein (ABCB1).

Nandigama K, Lusvarghi S, Shukla S, Ambudkar SV.

Protein Expr Purif. 2019 Jul;159:60-68. doi: 10.1016/j.pep.2019.03.002. Epub 2019 Mar 6.


The FLT3 inhibitor midostaurin selectively resensitizes ABCB1-overexpressing multidrug-resistant cancer cells to conventional chemotherapeutic agents.

Hsiao SH, Lusvarghi S, Huang YH, Ambudkar SV, Hsu SC, Wu CP.

Cancer Lett. 2019 Mar 31;445:34-44. doi: 10.1016/j.canlet.2019.01.001. Epub 2019 Jan 11.


Regorafenib antagonizes BCRP-mediated multidrug resistance in colon cancer.

Zhang YK, Wang YJ, Lei ZN, Zhang GN, Zhang XY, Wang DS, Al-Rihani SB, Shukla S, Ambudkar SV, Kaddoumi A, Shi Z, Chen ZS.

Cancer Lett. 2019 Feb 1;442:104-112. doi: 10.1016/j.canlet.2018.10.032. Epub 2018 Oct 28.


Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells.

Ji N, Yang Y, Cai CY, Lei ZN, Wang JQ, Gupta P, Shukla S, Ambudkar SV, Kong D, Chen ZS.

Cancer Lett. 2019 Jan;440-441:82-93. doi: 10.1016/j.canlet.2018.10.007. Epub 2018 Oct 10.


Evidence for the critical role of transmembrane helices 1 and 7 in substrate transport by human P-glycoprotein (ABCB1).

Sajid A, Lusvarghi S, Chufan EE, Ambudkar SV.

PLoS One. 2018 Sep 28;13(9):e0204693. doi: 10.1371/journal.pone.0204693. eCollection 2018.


Mapping discontinuous epitopes for MRK-16, UIC2 and 4E3 antibodies to extracellular loops 1 and 4 of human P-glycoprotein.

Vahedi S, Lusvarghi S, Pluchino K, Shafrir Y, Durell SR, Gottesman MM, Ambudkar SV.

Sci Rep. 2018 Aug 24;8(1):12716. doi: 10.1038/s41598-018-30984-8.


Novel Potent ABCB1 Modulator, Phenethylisoquinoline Alkaloid, Reverses Multidrug Resistance in Cancer Cell.

Sugisawa N, Ohnuma S, Ueda H, Murakami M, Sugiyama K, Ohsawa K, Kano K, Tokuyama H, Doi T, Aoki J, Ishida M, Kudoh K, Naitoh T, Ambudkar SV, Unno M.

Mol Pharm. 2018 Sep 4;15(9):4021-4030. doi: 10.1021/acs.molpharmaceut.8b00457. Epub 2018 Aug 13.


The positive inotropic agent DPI-201106 selectively reverses ABCB1-mediated multidrug resistance in cancer cell lines.

Hsiao SH, Murakami M, Yeh N, Li YQ, Hung TH, Wu YS, Ambudkar SV, Wu CP.

Cancer Lett. 2018 Oct 10;434:81-90. doi: 10.1016/j.canlet.2018.07.022. Epub 2018 Jul 18.


Human ATP-binding cassette transporters ABCB1 and ABCG2 confer resistance to histone deacetylase 6 inhibitor ricolinostat (ACY-1215) in cancer cell lines.

Wu CP, Hsieh YJ, Murakami M, Vahedi S, Hsiao SH, Yeh N, Chou AW, Li YQ, Wu YS, Yu JS, Ambudkar SV.

Biochem Pharmacol. 2018 Sep;155:316-325. doi: 10.1016/j.bcp.2018.07.018. Epub 2018 Jul 17.


SIS3, a specific inhibitor of Smad3 reverses ABCB1- and ABCG2-mediated multidrug resistance in cancer cell lines.

Wu CP, Murakami M, Hsiao SH, Liu TC, Yeh N, Li YQ, Hung TH, Wu YS, Ambudkar SV.

Cancer Lett. 2018 Oct 1;433:259-272. doi: 10.1016/j.canlet.2018.07.004. Epub 2018 Jul 6.


Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.

Patel BA, Abel B, Barbuti AM, Velagapudi UK, Chen ZS, Ambudkar SV, Talele TT.

J Med Chem. 2018 Feb 8;61(3):834-864. doi: 10.1021/acs.jmedchem.7b01340. Epub 2018 Jan 23.


Synthetic Analogs of Curcumin Modulate the Function of Multidrug Resistance-Linked ATP-Binding Cassette Transporter ABCG2.

Murakami M, Ohnuma S, Fukuda M, Chufan EE, Kudoh K, Kanehara K, Sugisawa N, Ishida M, Naitoh T, Shibata H, Iwabuchi Y, Ambudkar SV, Unno M.

Drug Metab Dispos. 2017 Nov;45(11):1166-1177. doi: 10.1124/dmd.117.076000. Epub 2017 Sep 13.


Tyrphostin RG14620 selectively reverses ABCG2-mediated multidrug resistance in cancer cell lines.

Wu CP, Hsiao SH, Murakami M, Lu MJ, Li YQ, Hsieh CH, Ambudkar SV, Wu YS.

Cancer Lett. 2017 Nov 28;409:56-65. doi: 10.1016/j.canlet.2017.08.035. Epub 2017 Sep 8.


Alpha-Mangostin Reverses Multidrug Resistance by Attenuating the Function of the Multidrug Resistance-Linked ABCG2 Transporter.

Wu CP, Hsiao SH, Murakami M, Lu YJ, Li YQ, Huang YH, Hung TH, Ambudkar SV, Wu YS.

Mol Pharm. 2017 Aug 7;14(8):2805-2814. doi: 10.1021/acs.molpharmaceut.7b00334. Epub 2017 Jul 5.


Overexpression of ATP-Binding Cassette Subfamily G Member 2 Confers Resistance to Phosphatidylinositol 3-Kinase Inhibitor PF-4989216 in Cancer Cells.

Wu CP, Murakami M, Hsiao SH, Chou AW, Li YQ, Huang YH, Hung TH, Ambudkar SV.

Mol Pharm. 2017 Jul 3;14(7):2368-2377. doi: 10.1021/acs.molpharmaceut.7b00277. Epub 2017 Jun 20.


Regorafenib overcomes chemotherapeutic multidrug resistance mediated by ABCB1 transporter in colorectal cancer: In vitro and in vivo study.

Wang YJ, Zhang YK, Zhang GN, Al Rihani SB, Wei MN, Gupta P, Zhang XY, Shukla S, Ambudkar SV, Kaddoumi A, Shi Z, Chen ZS.

Cancer Lett. 2017 Jun 28;396:145-154. doi: 10.1016/j.canlet.2017.03.011. Epub 2017 Mar 14.


Effects of a detergent micelle environment on P-glycoprotein (ABCB1)-ligand interactions.

Shukla S, Abel B, Chufan EE, Ambudkar SV.

J Biol Chem. 2017 Apr 28;292(17):7066-7076. doi: 10.1074/jbc.M116.771634. Epub 2017 Mar 10.


The BTK Inhibitor Ibrutinib (PCI-32765) Overcomes Paclitaxel Resistance in ABCB1- and ABCC10-Overexpressing Cells and Tumors.

Zhang H, Patel A, Wang YJ, Zhang YK, Kathawala RJ, Qiu LH, Patel BA, Huang LH, Shukla S, Yang DH, Ambudkar SV, Fu LW, Chen ZS.

Mol Cancer Ther. 2017 Jun;16(6):1021-1030. doi: 10.1158/1535-7163.MCT-16-0511. Epub 2017 Mar 6.


Selective reversal of BCRP-mediated MDR by VEGFR-2 inhibitor ZM323881.

Zhang YK, Zhang XY, Zhang GN, Wang YJ, Xu H, Zhang D, Shukla S, Liu L, Yang DH, Ambudkar SV, Chen ZS.

Biochem Pharmacol. 2017 May 15;132:29-37. doi: 10.1016/j.bcp.2017.02.019. Epub 2017 Feb 27.


Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCB1.

Wang YJ, Patel BA, Anreddy N, Zhang YK, Zhang GN, Alqahtani S, Singh S, Shukla S, Kaddoumi A, Ambudkar SV, Talele TT, Chen ZS.

Sci Rep. 2017 Feb 9;7:42106. doi: 10.1038/srep42106.


Structures of the Multidrug Transporter P-glycoprotein Reveal Asymmetric ATP Binding and the Mechanism of Polyspecificity.

Esser L, Zhou F, Pluchino KM, Shiloach J, Ma J, Tang WK, Gutierrez C, Zhang A, Shukla S, Madigan JP, Zhou T, Kwong PD, Ambudkar SV, Gottesman MM, Xia D.

J Biol Chem. 2017 Jan 13;292(2):446-461. doi: 10.1074/jbc.M116.755884. Epub 2016 Nov 18.


Crystal structure of the antigen-binding fragment of a monoclonal antibody specific for the multidrug-resistance-linked ABC transporter human P-glycoprotein.

Esser L, Shukla S, Zhou F, Ambudkar SV, Xia D.

Acta Crystallogr F Struct Biol Commun. 2016 Aug;72(Pt 8):636-41. doi: 10.1107/S2053230X16009778. Epub 2016 Jul 27.


Screening dietary flavonoids for the reversal of P-glycoprotein-mediated multidrug resistance in cancer.

Mohana S, Ganesan M, Agilan B, Karthikeyan R, Srithar G, Beaulah Mary R, Ananthakrishnan D, Velmurugan D, Rajendra Prasad N, Ambudkar SV.

Mol Biosyst. 2016 Jul 19;12(8):2458-70. doi: 10.1039/c6mb00187d.


Cryo-EM Analysis of the Conformational Landscape of Human P-glycoprotein (ABCB1) During its Catalytic Cycle.

Frank GA, Shukla S, Rao P, Borgnia MJ, Bartesaghi A, Merk A, Mobin A, Esser L, Earl LA, Gottesman MM, Xia D, Ambudkar SV, Subramaniam S.

Mol Pharmacol. 2016 Jul;90(1):35-41. doi: 10.1124/mol.116.104190. Epub 2016 May 11.


South Asian Medicinal Compounds as Modulators of Resistance to Chemotherapy and Radiotherapy.

Prasad NR, Muthusamy G, Shanmugam M, Ambudkar SV.

Cancers (Basel). 2016 Mar 5;8(3). pii: E32. doi: 10.3390/cancers8030032. Review.


Human-Mouse Chimeras with Normal Expression and Function Reveal That Major Domain Swapping Is Tolerated by P-Glycoprotein (ABCB1).

Pluchino KM, Hall MD, Moen JK, Chufan EE, Fetsch PA, Shukla S, Gill DR, Hyde SC, Xia D, Ambudkar SV, Gottesman MM.

Biochemistry. 2016 Feb 23;55(7):1010-23. doi: 10.1021/acs.biochem.5b01064. Epub 2016 Feb 10.


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.


Drug-protein hydrogen bonds govern the inhibition of the ATP hydrolysis of the multidrug transporter P-glycoprotein.

Chufan EE, Kapoor K, Ambudkar SV.

Biochem Pharmacol. 2016 Feb 1;101:40-53. doi: 10.1016/j.bcp.2015.12.007. Epub 2015 Dec 11.


A Gene Expression Signature Associated with Overall Survival in Patients with Hepatocellular Carcinoma Suggests a New Treatment Strategy.

Gillet JP, Andersen JB, Madigan JP, Varma S, Bagni RK, Powell K, Burgan WE, Wu CP, Calcagno AM, Ambudkar SV, Thorgeirsson SS, Gottesman MM.

Mol Pharmacol. 2016 Feb;89(2):263-72. doi: 10.1124/mol.115.101360. Epub 2015 Dec 14.


Using the BacMam Baculovirus System to Study Expression and Function of Recombinant Efflux Drug Transporters in Polarized Epithelial Cell Monolayers.

Fung KL, Kapoor K, Pixley JN, Talbert DJ, Kwit AD, Ambudkar SV, Gottesman MM.

Drug Metab Dispos. 2016 Feb;44(2):180-8. doi: 10.1124/dmd.115.066506. Epub 2015 Nov 30. Erratum in: Drug Metab Dispos. 2016 Apr;44(4):517.


A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo.

Anreddy N, Patel A, Zhang YK, Wang YJ, Shukla S, Kathawala RJ, Kumar P, Gupta P, Ambudkar SV, Wurpel JN, Chen ZS, Guo H.

Oncotarget. 2015 Nov 17;6(36):39276-91. doi: 10.18632/oncotarget.5747.


Identification of a Cryptic Bacterial Promoter in Mouse (mdr1a) P-Glycoprotein cDNA.

Pluchino KM, Esposito D, Moen JK, Hall MD, Madigan JP, Shukla S, Procter LV, Wall VE, Schneider TD, Pringle I, Ambudkar SV, Gill DR, Hyde SC, Gottesman MM.

PLoS One. 2015 Aug 26;10(8):e0136396. doi: 10.1371/journal.pone.0136396. eCollection 2015.


The Inhibitor Ko143 Is Not Specific for ABCG2.

Weidner LD, Zoghbi SS, Lu S, Shukla S, Ambudkar SV, Pike VW, Mulder J, Gottesman MM, Innis RB, Hall MD.

J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. doi: 10.1124/jpet.115.225482. Epub 2015 Jul 6.


Expression of the multidrug transporter P-glycoprotein is inversely related to that of apoptosis-associated endogenous TRAIL.

Souza PS, Madigan JP, Gillet JP, Kapoor K, Ambudkar SV, Maia RC, Gottesman MM, Fung KL.

Exp Cell Res. 2015 Aug 15;336(2):318-28. doi: 10.1016/j.yexcr.2015.06.005. Epub 2015 Jun 19.


Revealing the fate of cell surface human P-glycoprotein (ABCB1): The lysosomal degradation pathway.

Katayama K, Kapoor K, Ohnuma S, Patel A, Swaim W, Ambudkar IS, Ambudkar SV.

Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2361-70. doi: 10.1016/j.bbamcr.2015.06.001. Epub 2015 Jun 6.

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