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Items: 1 to 50 of 224

1.

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.

PMID:
29251928
2.

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.

3.

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.

PMID:
28893612
4.
5.

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.

PMID:
28641010
6.

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.

PMID:
28597653
7.

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.

8.

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.

9.

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.

10.

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.

PMID:
28242251
11.

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.

12.

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.

13.

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.

14.

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.

15.

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.

16.

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.

17.

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.

18.

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.

PMID:
26708291
19.

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.

20.

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.

21.

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.

22.

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.

23.

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.

24.

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.

25.

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.

26.

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.

27.

ATP-binding cassette subfamily B member 1 (ABCB1) and subfamily C member 10 (ABCC10) are not primary resistance factors for cabazitaxel.

Kathawala RJ, Wang YJ, Shukla S, Zhang YK, Alqahtani S, Kaddoumi A, Ambudkar SV, Ashby CR Jr, Chen ZS.

Chin J Cancer. 2015 Mar 5;34(3):115-20. doi: 10.1186/s40880-015-0003-0.

28.
29.

Molecular basis of the polyspecificity of P-glycoprotein (ABCB1): recent biochemical and structural studies.

Chufan EE, Sim HM, Ambudkar SV.

Adv Cancer Res. 2015;125:71-96. doi: 10.1016/bs.acr.2014.10.003. Epub 2015 Jan 8. Review.

PMID:
25640267
30.

The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.

Mathias TJ, Natarajan K, Shukla S, Doshi KA, Singh ZN, Ambudkar SV, Baer MR.

Invest New Drugs. 2015 Apr;33(2):300-9. doi: 10.1007/s10637-015-0205-y. Epub 2015 Jan 20.

PMID:
25597754
31.

Hydrogel-assisted functional reconstitution of human P-glycoprotein (ABCB1) in giant liposomes.

Horger KS, Liu H, Rao DK, Shukla S, Sept D, Ambudkar SV, Mayer M.

Biochim Biophys Acta. 2015 Feb;1848(2):643-53. doi: 10.1016/j.bbamem.2014.10.023. Epub 2014 Nov 4.

32.

A combination of curcumin with either gramicidin or ouabain selectively kills cells that express the multidrug resistance-linked ABCG2 transporter.

Rao DK, Liu H, Ambudkar SV, Mayer M.

J Biol Chem. 2014 Nov 7;289(45):31397-410. doi: 10.1074/jbc.M114.576819. Epub 2014 Sep 24.

33.

Evidence for a molecular diode-based mechanism in a multispecific ATP-binding cassette (ABC) exporter: SER-1368 as a gatekeeping residue in the yeast multidrug transporter Pdr5.

Mehla J, Ernst R, Moore R, Wakschlag A, Marquis MK, Ambudkar SV, Golin J.

J Biol Chem. 2014 Sep 19;289(38):26597-606. doi: 10.1074/jbc.M114.586032. Epub 2014 Aug 11.

34.

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.

35.

ARRY-334543 reverses multidrug resistance by antagonizing the activity of ATP-binding cassette subfamily G member 2.

Wang DS, Patel A, Sim HM, Zhang YK, Wang YJ, Kathawala RJ, Zhang H, Talele TT, Ambudkar SV, Xu RH, Chen ZS.

J Cell Biochem. 2014 Aug;115(8):1381-91. doi: 10.1002/jcb.24787.

36.

Motesanib (AMG706), a potent multikinase inhibitor, antagonizes multidrug resistance by inhibiting the efflux activity of the ABCB1.

Wang YJ, Kathawala RJ, Zhang YK, Patel A, Kumar P, Shukla S, Fung KL, Ambudkar SV, Talele TT, Chen ZS.

Biochem Pharmacol. 2014 Aug 15;90(4):367-78. doi: 10.1016/j.bcp.2014.06.006. Epub 2014 Jun 14.

37.

WHI-P154 enhances the chemotherapeutic effect of anticancer agents in ABCG2-overexpressing cells.

Zhang H, Zhang YK, Wang YJ, Kathawala RJ, Patel A, Zhu H, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Fu LW.

Cancer Sci. 2014 Aug;105(8):1071-8. doi: 10.1111/cas.12462. Epub 2014 Aug 21.

38.

Pharmacophore modeling of nilotinib as an inhibitor of ATP-binding cassette drug transporters and BCR-ABL kinase using a three-dimensional quantitative structure-activity relationship approach.

Shukla S, Kouanda A, Silverton L, Talele TT, Ambudkar SV.

Mol Pharm. 2014 Jul 7;11(7):2313-22. doi: 10.1021/mp400762h. Epub 2014 Jun 5.

39.

Design and synthesis of human ABCB1 (P-glycoprotein) inhibitors by peptide coupling of diverse chemical scaffolds on carboxyl and amino termini of (S)-valine-derived thiazole amino acid.

Singh S, Prasad NR, Chufan EE, Patel BA, Wang YJ, Chen ZS, Ambudkar SV, Talele TT.

J Med Chem. 2014 May 22;57(10):4058-72. doi: 10.1021/jm401966m. Epub 2014 May 7.

40.

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.

PMID:
24726739
41.

Elucidation of the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna) with the human ABC drug transporter P-glycoprotein.

Shukla S, Chufan EE, Singh S, Skoumbourdis AP, Kapoor K, Boxer MB, Duveau DY, Thomas CJ, Talele TT, Ambudkar SV.

Leukemia. 2014 Apr;28(4):961-4. doi: 10.1038/leu.2014.21. Epub 2014 Jan 14. No abstract available.

42.

Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1).

Chufan EE, Kapoor K, Sim HM, Singh S, Talele TT, Durell SR, Ambudkar SV.

PLoS One. 2013 Dec 5;8(12):e82463. doi: 10.1371/journal.pone.0082463. eCollection 2013.

43.

MDR1 synonymous polymorphisms alter transporter specificity and protein stability in a stable epithelial monolayer.

Fung KL, Pan J, Ohnuma S, Lund PE, Pixley JN, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.

Cancer Res. 2014 Jan 15;74(2):598-608. doi: 10.1158/0008-5472.CAN-13-2064. Epub 2013 Dec 4.

44.

Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2.

Bakhsheshian J, Wei BR, Chang KE, Shukla S, Ambudkar SV, Simpson RM, Gottesman MM, Hall MD.

Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):20801-6. doi: 10.1073/pnas.1312159110. Epub 2013 Dec 2.

45.

Tivozanib reverses multidrug resistance mediated by ABCB1 (P-glycoprotein) and ABCG2 (BCRP).

Yang D, Kathawala RJ, Chufan EE, Patel A, Ambudkar SV, Chen ZS, Chen X.

Future Oncol. 2014 Aug;10(11):1827-41. doi: 10.2217/fon.13.253. Epub 2013 Dec 3.

PMID:
24295377
46.

Design, synthesis, and biological evaluation of (S)-valine thiazole-derived cyclic and noncyclic peptidomimetic oligomers as modulators of human P-glycoprotein (ABCB1).

Singh S, Prasad NR, Kapoor K, Chufan EE, Patel BA, Ambudkar SV, Talele TT.

Chembiochem. 2014 Jan 3;15(1):157-69. doi: 10.1002/cbic.201300565. Epub 2013 Nov 29.

47.

Interindividual variability in hepatic organic anion-transporting polypeptides and P-glycoprotein (ABCB1) protein expression: quantification by liquid chromatography tandem mass spectroscopy and influence of genotype, age, and sex.

Prasad B, Evers R, Gupta A, Hop CE, Salphati L, Shukla S, Ambudkar SV, Unadkat JD.

Drug Metab Dispos. 2014 Jan;42(1):78-88. doi: 10.1124/dmd.113.053819. Epub 2013 Oct 11.

48.

Mutations in intracellular loops 1 and 3 lead to misfolding of human P-glycoprotein (ABCB1) that can be rescued by cyclosporine A, which reduces its association with chaperone Hsp70.

Kapoor K, Bhatnagar J, Chufan EE, Ambudkar SV.

J Biol Chem. 2013 Nov 8;288(45):32622-36. doi: 10.1074/jbc.M113.498980. Epub 2013 Sep 24.

49.

Conserved Walker A cysteines 431 and 1074 in human P-glycoprotein are accessible to thiol-specific agents in the apo and ADP-vanadate trapped conformations.

Sim HM, Bhatnagar J, Chufan EE, Kapoor K, Ambudkar SV.

Biochemistry. 2013 Oct 15;52(41):7327-38. doi: 10.1021/bi4007786. Epub 2013 Oct 4.

50.

The deviant ATP-binding site of the multidrug efflux pump Pdr5 plays an active role in the transport cycle.

Furman C, Mehla J, Ananthaswamy N, Arya N, Kulesh B, Kovach I, Ambudkar SV, Golin J.

J Biol Chem. 2013 Oct 18;288(42):30420-31. doi: 10.1074/jbc.M113.494682. Epub 2013 Sep 9.

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