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Suresh V. Ambudkar, Ph.D.

Selected Publications

1)  Ambudkar SV, Lelong IH, Zhang J, Cardarelli CO, Gottesman MM, Pastan I.
Partial purification and reconstitution of the human multidrug-resistance pump: characterization of the drug-stimulatable ATP hydrolysis.
Proc. Natl. Acad. Sci. U.S.A. 89: 8472-6, 1992.
2)  Ambudkar SV, Cardarelli CO, Pashinsky I, Stein WD.
Relation between the turnover number for vinblastine transport and for vinblastine-stimulated ATP hydrolysis by human P-glycoprotein.
J. Biol. Chem. 272: 21160-6, 1997.
3)  Sauna ZE, Ambudkar SV.
Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein.
Proc Natl Acad Sci U S A. 97: 2515-20, 2000.
4)  Chufan EE, Kapoor K, Sim HM, Singh S, Talele TT, Durell SR, Ambudkar SV.
Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1).
PLoS ONE. 8: e82463, 2013.
5)  Shukla S, Chufan EE, Singh S, Skoumbourdis AP, Kapoor K, Boxer MB, Duveau DY, Thomas CJ, Talele TT, Ambudkar SV.
Elucidation of the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna) with the human ABC drug transporter P-glycoprotein.
Leukemia. 28: 961-4, 2014.
6)  Singh S, Prasad NR, Chufan EE, Patel BA, Wang YJ, Chen ZS, Ambudkar SV, Talele TT.
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.
J. Med. Chem. 57: 4058-72, 2014.
7)  Wang D, Patel A, Shukla S, Zhang Y, Wang Y, Kathawala RJ, Robey RW, Zhang L, Yang D, Talele TT, Bates SE, Ambudkar SV, Xu R, Chen Z.
Icotinib antagonizes ABCG2-mediated multidrug resistance, but not the pemetrexed resistance mediated by thymidylate synthase and ABCG2.
Oncotarget. 5: 4529-4542, 2014.
8)  Shukla S, Kouanda A, Silverton L, Talele TT, Ambudkar SV.
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.
Mol. Pharm. 2014.
9)  Prasad B, Evers R, Gupta A, Hop CE, Salphati L, Shukla S, Ambudkar SV, Unadkat JD.
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.
Drug Metab. Dispos. 42: 78-88, 2014.
10)  Kapoor K, Bhatnagar J, Chufan EE, Ambudkar SV.
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.
J. Biol. Chem. 288: 32622-36, 2013.
11)  Fung KL, Pan J, Ohnuma S, Lund PE, Pixley JN, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.
MDR1 synonymous polymorphisms alter transporter specificity and protein stability in a stable epithelial monolayer.
Cancer Res. 74: 598-608, 2014.
12)  Zhang H, Kathawala RJ, Wang Y, Zhang Y, Patel A, Shukla S, Robey RW, Talele TT, Ashby CR, Ambudkar SV, Bates SE, Fu L, Chen Z.
Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance.
Int. J. Biochem. Cell Biol. [Epub ahead of print], 2014.
13)  Wang YJ, Kathawala RJ, Zhang YK, Patel A, Kumar P, Shukla S, Fung KL, Ambudkar SV, Talele TT, Chen ZS.
Motesanib (AMG706), a potent multikinase inhibitor, antagonizes multidrug resistance by inhibiting the efflux activity of the ABCB1.
Biochem. Pharmacol. 2014.
14)  Wu C, Ambudkar SV.
The pharmacological impact of ATP-binding cassette drug transporters on vemurafenib-based therapy.
Acta Pharmaceutica Sinica B. 4: 104-111, 2014.
15)  Zhang H, Zhang YK, Wang YJ, Kathawala RJ, Patel A, Zhu H, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Fu LW.
WHI-P154 Enhances the Chemotherapeutic Effect of Anticancer Agents in ABCG2-overexpressing Cells.
Cancer Sci. 2014.
16)  Bakhsheshian J, Wei B, Chang K, Shukla S, Ambudkar SV, Simpson RM, Gottesman MM, Hall MD.
Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2.
Proc. Natl. Acad. Sci. U.S.A. 110: 20801-6, 2013.
17)  Sim HM, Bhatnagar J, Chufan EE, Kapoor K, Ambudkar SV.
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.
Biochemistry. 52: 7327-38, 2013.
18)  Singh S, Prasad NR, Kapoor K, Chufan EE, Patel BA, Ambudkar SV, Talele TT.
Design, Synthesis, and Biological Evaluation of (S)-Valine Thiazole-Derived Cyclic and Noncyclic Peptidomimetic Oligomers as Modulators of Human P-Glycoprotein (ABCB1).
Chembiochem. 15: 157-69, 2013.
19)  Kapoor K, Sim H, Ambudkar S.
Bonavida B, eds.
Multidrug resistance in cancer: A tale of ABC drug transporters. In: Resistance to Targeted Anti-cancer Therapeutics. Volume 1.
New York: Springer; 2013. p. 1-34 [Book Chapter]
20)  Wang DS, Patel A, Sim HM, Zhang YK, Wang YJ, Kathawala RJ, Zhang H, Talele TT, Ambudkar SV, Xu RH, Chen ZS.
ARRY-334543 Reverses Multidrug Resistance by Antagonizing the Activity of ATP-Binding Cassette Subfamily G Member 2.
J. Cell. Biochem. 115: 1381-91, 2014.
21)  Wu C, Hsiao S, Sim H, Luo S, Tuo W, Cheng H, Li Y, Huang Y, Ambudkar SV.
Human ABCB1 (P-glycoprotein) and ABCG2 Mediate Resistance to BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1.
Biochem. Pharmacol. 86: 904-13, 2013.
22)  Fukuda Y, Takenaka K, Sparreboom A, Cheepala SB, Wu CP, Ekins S, Ambudkar SV, Schuetz JD.
Human immunodeficiency virus protease inhibitors interact with ATP binding cassette transporter 4/multidrug resistance protein 4: a basis for unanticipated enhanced cytotoxicity.
Mol. Pharmacol. 84: 361-71, 2013.
23)  Wu CP, Sim HM, Huang YH, Liu YC, Hsiao SH, Cheng HW, Li YQ, Ambudkar SV, Hsu SC.
Overexpression of ATP-binding cassette transporter ABCG2 as a potential mechanism of acquired resistance to vemurafenib in BRAF(V600E) mutant cancer cells.
Biochem. Pharmacol. 85: 325-34, 2013.
24)  Patel A, Tiwari AK, Chufan EE, Sodani K, Anreddy N, Singh S, Ambudkar SV, Stephani R, Chen ZS.
PD173074, a selective FGFR inhibitor, reverses ABCB1-mediated drug resistance in cancer cells.
Cancer Chemother. Pharmacol. 72: 189-99, 2013.
25)  Liu K, He J, Su X, Sim H, Xie J, Chen X, Wang F, Liang Y, Singh S, Sodani K, Talele TT, Ambudkar SV, Chen Z, Wu H, Fu L.
Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo.
Int J Cancer. 132: 224-35, 2013.
26)  Ansbro MR, Shukla S, Ambudkar SV, Yuspa SH, Li L.
Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference.
PLoS ONE. 8: e60334, 2013.
27)  Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ.
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
Bioorg. Med. Chem. Lett. 23: 682-6, 2013.
28)  Zhao XQ, Dai CL, Ohnuma S, Liang YJ, Deng W, Chen JJ, Zeng MS, Ambudkar SV, Chen ZS, Fu LW.
Tandutinib (MLN518/CT53518) targeted to stem-like cells by inhibiting the function of ATP-binding cassette subfamily G member 2.
Eur J Pharm Sci. 49: 441-50, 2013.
29)  Furman C, Mehla J, Ananthaswamy N, Arya N, Kulesh B, Kovach I, Ambudkar SV, Golin J.
The deviant ATP-binding site of the multidrug efflux pump Pdr5 plays an active role in the transport cycle.
J. Biol. Chem. 288: 30420-31, 2013.
30)  Bhullar J, Natarajan K, Shukla S, Mathias TJ, Sadowska M, Ambudkar SV, Baer MR.
The FLT3 Inhibitor Quizartinib Inhibits ABCG2 at Pharmacologically Relevant Concentrations, with Implications for Both Chemosensitization and Adverse Drug Interactions.
PLoS ONE. 8: e71266, 2013.
31)  Sen R, Natarajan K, Bhullar J, Shukla S, Fang H, Cai L, Chen Z, Ambudkar SV, Baer MR.
The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the multidrug resistance-associated ATP-binding cassette transporter ABCG2.
Mol Cancer Ther. 11:: 2033-44, 2013.
32)  Natarajan K, Bhullar J, Shukla S, Burcu M, Chen ZS, Ambudkar SV, Baer MR.
The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms.
Biochem. Pharmacol. 85: 514-24, 2013.
33)  Downes MT, Mehla J, Ananthaswamy N, Wakschlag A, Lamonde M, Dine E, Ambudkar SV, Golin J.
The transmission interface of the Saccharomyces cerevisiae multidrug transporter Pdr5: Val-656 located in intracellular loop 2 plays a major role in drug resistance.
Antimicrob. Agents Chemother. 57: 1025-34, 2013.
34)  Yang D, Kathawala RJ, Chufan EE, Patel A, Ambudkar SV, Chen Z, Chen X.
Tivozanib reverses multidrug resistance mediated by ABCB1 (P-glycoprotein) and ABCG2 (BCRP).
Future Oncol. [Epub ahead of print], 2013.
35)  Zhang DM, Shu C, Chen JJ, Sodani K, Wang J, Bhatnagar J, Lan P, Ruan ZX, Xiao ZJ, Ambudkar SV, Chen WM, Chen ZS, Ye WC.
BBA, a derivative of 23-hydroxybetulinic acid, potently reverses ABCB1-mediated drug resistance in vitro and in vivo.
Mol. Pharm. 9: 3147-59, 2012.
36)  Gupta V, Bhinge KN, Hosain SB, Xiong K, Gu X, Shi R, Ho MY, Khoo KH, Li SC, Li YT, Ambudkar SV, Jazwinski SM, Liu YY.
Ceramide glycosylation by glucosylceramide synthase selectively maintains the properties of breast cancer stem cells.
J. Biol. Chem. 287: 37195-205, 2012.
37)  Gillet JP, Calcagno AM, Varma S, Davidson B, Bunkholt Elstrand M, Ganapathi R, Kamat AA, Sood AK, Ambudkar SV, Seiden MV, Rueda BR, Gottesman MM.
Multidrug resistance-linked gene signature predicts overall survival of patients with primary ovarian serous carcinoma.
Clin. Cancer Res. 18: 3197-206, 2012.
38)  Zhao X, Xie J, Chen X, Sim HM, Zhang X, Liang Y, Singh S, Talele TT, Sun Y, Ambudkar SV, Chen Z, Fu L.
Neratinib (HKI-272) Reverses ABCB1-Mediated Chemotherapeutic Drug Resistance in Vitro, in Vivo and ex Vivo.
Mol Pharmacol. 82:: 47-58, 2012.
39)  Kuang Y, Patel JP, Sodani K, Wu C, Liao L, Patel A, Tiwari AK, Dai C, Chen X, Fu L, Ambudkar SV, Korlipara VL, Chen Z.
OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance.
Biochem Pharmacol. 84: 766-74, 2012.
40)  Shukla S, Chen Z, Ambudkar SV.
Tyrosine kinase inhibitors as modulators of ABC transporter-mediated drug resistance.
Drug Resist Updat. 15: 70-80, 2012.
41)  Shukla S, Schwartz C, Kapoor K, Kouanda A, Ambudkar SV.
Use of Baculovirus BacMam Vectors for Expression of ABC Drug Transporters in Mammalian Cells.
Drug Metab. Dispos. 40: 304-12, 2012.
42)  Chanmahasathien W, Ohnuma S, Ambudkar SV, Limtrakul P.
Biochemical Mechanism of Modulation of Human P-glycoprotein by Stemofoline.
Planta Medica. 77: 1990-1995, 2011.
43)  Gillet J, Wang J, Calcagno AM, Green LJ, Varma S, Bunkholt Elstrand M, Trope CG, Ambudkar SV, Davidson B, Gottesman MM.
Clinical Relevance of Multidrug Resistance Gene Expression in Ovarian Serous Carcinoma Effusions.
Mol. Pharmaceutics. 8: 2080-2088, 2011.
44)  Wu C, Ohnuma S, Ambudkar S.
Discovering natural product modulators to overcome multidrug resistance in cancer chemotherapy.
Curr. Pharmaceut. Biotechnol. 12: 609-620, 2011.
45)  Shukla S, Ohnuma S, Ambudkar S.
Improving cancer chemotherapy with modulators of ABC drug transporters.
Curr. Drug Targets. 12: 621-630, 2011.
46)  Sim HM, Wu CP, Ambudkar SV, Go ML.
In vitro and in vivo modulation of ABCG2 by functionalized aurones and structurally related analogs.
Biochem. Pharmacol. 82: 1562-71, 2011.
47)  Ohnuma S, Chufan EE, Nandigama K, Miller Jenkins LM, Durell SR, Appella E, Sauna ZE, Ambudkar SV.
Inhibition of Multidrug Resistance-Linked P-Glycoprotein (ABCB1) Function by 5'-Fluorosulfonylbenzoyl 5'-Adenosine: Evidence for an ATP Analog That Interacts With Both Drug-Substrate- and Nucleotide-Binding Sites.
Biochemistry. 50: 3724-3735, 2011.
48)  Pitchakarn P, Ohnuma S, Pintha K, Pompimon W, Ambudkar SV, Limtrakul P.
Kuguacin J isolated from Momordica charantia leaves inhibits P-glycoprotein (ABCB1)-mediated multidrug resistance.
J. Nutritional Biochem. 23: 76-84, 2011.
49)  Gillet JP, Calcagno AM, Varma S, Marino M, Green LJ, Vora MI, Patel C, Orina JN, Eliseeva TA, Singal V, Padmanabhan R, Davidson B, Ganapathi R, Sood AK, Rueda BR, Ambudkar SV, Gottesman MM.
Redefining the relevance of established cancer cell lines to the study of mechanisms of clinical anti-cancer drug resistance.
Proc. Natl. Acad. Sci. U.S.A. 108: 18708-13, 2011.
50)  Shi Z, Tiwari AK, Shukla S, Robey RW, Singh S, Kim I, Bates SE, Peng X, Abraham I, Ambudkar SV, Talele TT, Fu L, Chen Z.
Sildenafil Reverses ABCB1- and ABCG2-Mediated Chemotherapeutic Drug Resistance.
Cancer Res. 71: 3029-3041, 2011.
51)  Shukla S, Skoumbourdis AP, Walsh MJ, Hartz AM, Fung KL, Wu C, Gottesman MM, Bauer B, Thomas CJ, Ambudkar SV.
Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna® (Nilotinib): Evidence for transport of Tasigna® and its fluorescent derivative by ABC drug transporters.
Mol. Pharmaceutics. 8: 1292-1302, 2011.
52)  Ding PR, Tiwari AK, Ohnuma S, Lee JW, An X, Dai CL, Lu QS, Singh S, Yang DH, Talele TT, Ambudkar SV, Chen ZS.
The Phosphodiesterase-5 Inhibitor Vardenafil Is a Potent Inhibitor of ABCB1/P-Glycoprotein Transporter.
PLoS ONE. 6: e19329, 2011.
53)  Kannan P, Telu S, Shukla S, Ambudkar S, Pike V, Halldin C, Gottesman M, Innis R, Hall M.
The Specific P-Glycoprotein Inhibitor Tariquidar Is Also a Substrate and an Inhibitor for Breast Cancer Resistance Protein (BCRP/ABCG2).
ACS Chem. Neurosci. 2: 82-89, 2011.
54)  Calcagno AM, Ambudkar SV.
Analysis of expression of drug resistance-linked ABC transporters in cancer cells by quantitative RT-PCR.
Methods Mol. Biol. 637: 121-32, 2010.
55)  Mi YJ, Liang YJ, Huang HB, Zhao HY, Wu CP, Wang F, Tao LY, Zhang CZ, Dai CL, Tiwari AK, Ma XX, To KK, Ambudkar SV, Chen ZS, Fu LW.
Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters.
Cancer Res. 70: 7981-91, 2010.
56)  Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE.
Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib.
Drug Metab. Dispos. 38: 1371-80, 2010.
57)  Kucka M, Kretschmannova K, Murano T, Wu CP, Zemkova H, Ambudkar SV, Stojilkovic SS.
Dependence of multidrug resistance protein-mediated cyclic nucleotide efflux on the background sodium conductance.
Mol. Pharmacol. 77: 270-9, 2010.
58)  Kumar A, Shukla S, Mandal A, Shukla S, Ambudkar SV, Prasad R.
Divergent signature motifs of nucleotide binding domains of ABC multidrug transporter, CaCdr1p of pathogenic Candida albicans, are functionally asymmetric and noninterchangeable.
Biochim. Biophys. Acta. 1798: 1757-1766, 2010.
59)  Abraham I, Jain S, Wu C, Khanfar MA, Kuang Y, Dai C, Shi Z, Chen X, Fu L, Ambudkar SV, Sayed KE, Chen Z.
Marine sponge-derived sipholane triterpenoids reverse P-glycoprotein (ABCB1)-mediated multidrug resistance in cancer cells.
Biochem. Pharmacol. 80: 1497-1506, 2010.
60)  Calcagno AM, Ambudkar SV.
Molecular mechanisms of drug resistance in single-step and multi-step drug-selected cancer cells.
Methods Mol. Biol. 596: 77-93, 2010.
61)  Tam J, Vemuri VK, Liu J, Bátkai S, Mukhopadhyay B, Godlewski G, Osei-Hyiaman D, Ohnuma S, Ambudkar SV, Pickel J, Makriyannis A, Kunos G.
Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.
J. Clin. Invest. 120: 2953-66, 2010.
62)  Calcagno AM, Salcido CD, Gillet JP, Wu CP, Fostel JM, Mumau MD, Gottesman MM, Varticovski L, Ambudkar SV.
Prolonged drug selection of breast cancer cells and enrichment of cancer stem cell characteristics.
J. Natl. Cancer Inst. 102: 1637-52, 2010.
63)  Ananthaswamy N, Rutledge R, Sauna ZE, Ambudkar SV, Dine E, Nelson E, Xia D, Golin J.
The Signaling Interface of the Yeast Multidrug Transporter Pdr5 Adopts a Cis Conformation, and There Are Functional Overlap and Equivalence of the Deviant and Canonical Q-Loop Residues.
Biochemistry. 49: 4440-4449, 2010.
64)  Li L, Shukla S, Lee A, Garfield SH, Maloney DJ, Ambudkar SV, Yuspa SH.
The Skin Cancer Chemotherapeutic Agent Ingenol-3-Angelate (PEP005) Is a Substrate for the Epidermal Multidrug Transporter (ABCB1) and Targets Tumor Vasculature.
Cancer Res. 70: 4509-4519, 2010.
65)  Robey RW, Obrzut T, Shukla S, Polgar O, Macalou S, Bahr JC, Di Pietro A, Ambudkar SV, Bates SE.
Becatecarin (rebeccamycin analog, NSC 655649) is a transport substrate and induces expression of the ATP-binding cassette transporter, ABCG2, in lung carcinoma cells.
Cancer Chemother. Pharmacol. 2009.
66)  Henrich CJ, Robey RW, Takada K, Bokesch HR, Bates SE, Shukla S, Ambudkar SV, McMahon JB, Gustafson KR.
Botryllamides: Natural Product Inhibitors of ABCG2.
ACS Chem. Biol. 4: 637-47, 2009.
67)  Shukla S, Zaher H, Hartz A, Bauer B, Ware JA, Ambudkar SV.
Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice.
Pharm. Res. 26: 480-7, 2009.
68)  Sharma M, Manoharlal R, Shukla S, Puri N, Prasad T, Ambudkar SV, Prasad R.
Curcumin Modulates Efflux Mediated By Yeast ABC Multidrug Transporters And Is Synergistic To Antifungals.
Antimicrob. Agents Chemother. 2009.
69)  Orina JN, Calcagno AM, Wu C, Varma S, Shih J, Lin M, Eichler G, Weinstein JN, Pommier Y, Ambudkar SV, Gottesman MM, Gillet J.
Evaluation of current methods used to analyze the expression profiles of ATP-binding cassette transporters yields an improved drug-discovery database.
Mol. Cancer Ther. 8: 2057-66, 2009.
70)  Deeken JF, Robey RW, Shukla S, Steadman K, Chakraborty A, Poonkuzhali B, Schuetz EG, Holbeck S, Ambudkar SV, Bates SE.
Identification of compounds that correlate with ABCG2 transporter function in the National Cancer Institute Anticancer Drug Screen.
Mol. Pharmacol. 76: 946-56, 2009.
71)  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.
Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478.
Biochem. Pharmacol. 77: 781-93, 2009.
72)  Dai CL, Liang YJ, Chen LM, Zhang X, Deng WJ, Su XD, Shi Z, Wu CP, Ashby CR, Akiyama SI, Ambudkar SV, Chen ZS, Fu LW.
Sensitization of ABCB1 overexpressing cells to chemotherapeutic agents by FG020326 via binding to ABCB1 and inhibiting its function.
Biochem. Pharmacol. 2009.
73)  Hunt R, Sauna ZE, Ambudkar SV, Gottesman MM, Kimchi-Sarfaty C.
Silent (synonymous) SNPs: should we care about them?.
Methods Mol. Biol. 578: 23-39, 2009.
74)  Gottesman MM, Ambudkar SV, Xia D.
Structure of a multidrug transporter.
Nat. Biotechnol. 27: 546-7, 2009.
75)  Shukla S, Robey RW, Bates SE, Ambudkar SV.
Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2.
Drug Metab. Dispos. 37: 359-65, 2009.
76)  Puri N, Gaur M, Sharma M, Shukla S, Ambudkar SV, Prasad R.
The amino acid residues of transmembrane helix 5 of multidrug resistance protein CaCdr1p of Candida albicans are involved in substrate specificity and drug transport.
Biochim. Biophys. Acta. 2009.
77)  Gardner ER, Ahlers CM, Shukla S, Sissung TM, Ockers SB, Price DK, Hamada A, Robey RW, Steinberg SM, Ambudkar SV, Dahut WL, Figg WD.
Association of the ABCG2 C421A polymorphism with prostate cancer risk and survival.
BJU Int. 2008.
78)  Wright MH, Calcagno AM, Salcido CD, Carlson MD, Ambudkar SV, Varticovski L.
Brca1 breast tumors contain distinct CD44+/CD24- and CD133+ cells with cancer stem cell characteristics.
Breast Cancer Res. 10: R10, 2008.
79)  Shukla S, Wu CP, Ambudkar SV.
Development of inhibitors of ATP-binding cassette drug transporters: present status and challenges.
Expert opinion on drug metabolism & toxicology. 4: 205-23, 2008.
80)  Shukla S, Sauna ZE, Ambudkar SV.
Evidence for the interaction of imatinib at the transport-substrate site(s) of the multidrug-resistance-linked ABC drug transporters ABCB1 (P-glycoprotein) and ABCG2.
Leukemia. 22: 445-447, 2008.
81)  Robey RW, Shukla S, Finley EM, Oldham RK, Barnett D, Ambudkar SV, Fojo T, Bates SE.
Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).
Biochem. Pharmacol. 75: 1302-1312, 2008.
82)  Dai CL, Tiwari AK, Wu CP, Su XD, Wang SR, Liu DG, Ashby CR, Huang Y, Robey RW, Liang YJ, Chen LM, Shi CJ, Ambudkar SV, Chen ZS, Fu LW.
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.
Cancer Res. 68: 7905-14, 2008.
83)  Sauna ZE, Bohn SS, Rutledge R, Dougherty MP, Cronin S, May L, Xia D, Ambudkar SV, Golin J.
Mutations define cross-talk between the N-terminal nucleotide-binding domain and transmembrane helix-2 of the yeast multidrug transporter Pdr5: possible conservation of a signaling interface for coupling ATP hydrolysis to drug transport.
J. Biol. Chem. 283: 35010-22, 2008.
84)  Kim IW, Booth-Genthe C, Ambudkar SV.
Relationship Between Drugs and Functional Activity of Various Mammalian P-Glycoproteins (ABCB1).
Mini reviews in medicinal chemistry. 8: 193-200, 2008.
85)  Wu C, Calcagno AM, Ambudkar SV.
Reversal of ABC drug transporter-mediated multidrug resistance in cancer cells: Evaluation of current strategies.
Current Mol Pharmacol. 1: 93-105, 2008.
86)  Calcagno AM, Fostel JM, To KK, Salcido CD, Martin SE, Chewning KJ, Wu CP, Varticovski L, Bates SE, Caplen NJ, Ambudkar SV.
Single-step doxorubicin-selected cancer cells overexpress the ABCG2 drug transporter through epigenetic changes.
Br. J. Cancer. 98: 1515-24, 2008.
87)  Tsai CJ, Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM, Nussinov R.
Synonymous Mutations and Ribosome Stalling Can Lead to Altered Folding Pathways and Distinct Minima.
J. Mol. Biol. 2008.
88)  Chen SY, Pan CJ, Nandigama K, Mansfield BC, Ambudkar SV, Chou JY.
The glucose-6-phosphate transporter is a phosphate-linked antiporter deficient in glycogen storage disease type Ib and Ic.
FASEB J. 2008.
89)  Kimchi-Sarfaty C, Oh JM, Kim IW, Sauna ZE, Calcagno AM, Ambudkar SV, Gottesman MM.
Science. 315: 525-8, 2007.
90)  Calcagno AM, Kim IW, Wu CP, Shukla S, Ambudkar SV.
ABC drug transporters as molecular targets for the prevention of multidrug resistance and drug-drug interactions.
Current drug delivery. 4: 324-33, 2007.
91)  Sauna ZE, Ambudkar SV.
About a switch: how P-glycoprotein (ABCB1) harnesses the energy of ATP binding and hydrolysis to do mechanical work.
Mol. Cancer Ther. 6: 13-23, 2007.
92)  Sauna ZE, Kim IW, Nandigama K, Kopp S, Chiba P, Ambudkar SV.
Catalytic Cycle of ATP Hydrolysis by P-Glycoprotein: Evidence for Formation of the E.S Reaction Intermediate with ATP-gamma-S, a Nonhydrolyzable Analogue of ATP.
Biochemistry. 46: 13787-13799, 2007.
93)  Golin J, Kon ZN, Wu CP, Martello J, Hanson L, Supernavage S, Ambudkar SV, Sauna ZE.
Complete inhibition of the Pdr5p multidrug efflux pump ATPase activity by its transport substrate clotrimazole suggests that GTP as Well as ATP may be used as an energy source.
Biochemistry. 46: 13109-19, 2007.
94)  Shi Z, Peng XX, Kim IW, Shukla S, Si QS, Robey RW, Bates SE, Shen T, Ashby CR, Fu LW, Ambudkar SV, Chen ZS.
Erlotinib (Tarceva, OSI-774) antagonizes ATP-binding cassette subfamily B member 1 and ATP-binding cassette subfamily G member 2-mediated drug resistance.
Cancer Res. 67: 11012-20, 2007.
95)  Wu CP, Shukla S, Calcagno AM, Hall MD, Gottesman MM, Ambudkar SV.
Evidence for dual mode of action of a thiosemicarbazone, NSC73306: a potent substrate of the multidrug resistance linked ABCG2 transporter.
Mol. Cancer Ther. 6: 3287-96, 2007.
96)  Sauna ZE, Kim IW, Ambudkar SV.
Genomics and the mechanism of P-glycoprotein (ABCB1).
J Bioenerg Biomembr. 2007.
97)  Paterson JK, Shukla S, Black CM, Tachiwada T, Garfield S, Wincovitch S, Ernst DN, Agadir A, Li X, Ambudkar SV, Szakacs G, Akiyama SI, Gottesman MM.
Human ABCB6 Localizes to Both the Outer Mitochondrial Membrane and the Plasma Membrane.
Biochemistry. 2007.
98)  Brendel C, Scharenberg C, Dohse M, Robey RW, Bates SE, Shukla S, Ambudkar SV, Wang Y, Wennemuth G, Burchert A, Boudriot U, Neubauer A.
Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells.
Leukemia. 21: 1267-75, 2007.
99)  Robey RW, Shukla S, Steadman K, Obrzut T, Finley EM, Ambudkar SV, Bates SE.
Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure.
Mol. Cancer Ther. 6: 1877-85, 2007.
100)  Henrich CJ, Robey RW, Bokesch HR, Bates SE, Shukla S, Ambudkar SV, Dean M, McMahon JB.
New inhibitors of ABCG2 identified by high-throughput screening.
Mol. Cancer Ther. 6: 3271-8, 2007.
101)  Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.
Silent polymorphisms speak: how they affect pharmacogenomics and the treatment of cancer.
Cancer Res. 67: 9609-12, 2007.
102)  Shi Z, Jain S, Kim IW, Peng XX, Abraham I, Youssef DT, Fu LW, El Sayed K, Ambudkar SV, Chen ZS.
Sipholenol A, a marine-derived sipholane triterpene, potently reverses P-glycoprotein (ABCB1)-mediated multidrug resistance in cancer cells.
Cancer Sci. 98: 1373-80, 2007.
103)  Shukla S, Wu CP, Nandigama K, Ambudkar SV.
The naphthoquinones, vitamin K3 and its structural analogue plumbagin, are substrates of the multidrug resistance linked ATP binding cassette drug transporter ABCG2.
Mol. Cancer Ther. 6: 3279-86, 2007.
104)  Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.
The sounds of silence: synonymous mutations affect function.
Pharmacogenomics. 8: 527-532, 2007.
105)  Golin J, Ambudkar SV, May L.
The yeast Pdr5p multidrug transporter: how does it recognize so many substrates?.
Biochem. Biophys. Res. Commun. 356: 1-5, 2007.
106)  Calcagno AM, Ludwig JA, Fostel JM, Gottesman MM, Ambudkar SV.
Comparison of drug transporter levels in normal colon, colon cancer, and Caco-2 cells: impact on drug disposition and discovery.
Mol. Pharm. 3: 87-93, 2006.
107)  Rai V, Gaur M, Shukla S, Shukla S, Ambudkar SV, Komath SS, Prasad R.
Conserved Asp327 of walker B motif in the N-terminal nucleotide binding domain (NBD-1) of Cdr1p of Candida albicans has acquired a new role in ATP hydrolysis.
Biochemistry. 45: 14726-39, 2006.
108)  Pawarode A, Shukla S, Minderman H, Fricke SM, Pinder EM, O'loughlin KL, Ambudkar SV, Baer MR.
Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins.
Cancer Chemother Pharmacol. 2006.
109)  Sauna ZE, Nandigama K, Ambudkar SV.
Exploiting reaction intermediates of the ATPase reaction to elucidate the mechanism of transport by P-glycoprotein (ABCB1).
J. Biol. Chem. 281: 26501-11, 2006.
110)  Limtrakul P, Chearwae W, Shukla S, Phisalphong C, Ambudkar SV.
Modulation of function of three ABC drug transporters, P-glycoprotein (ABCB1), mitoxantrone resistance protein (ABCG2) and multidrug resistance protein 1 (ABCC1) by tetrahydrocurcumin, a major metabolite of curcumin.
Mol Cell Biochem. 2006.
111)  Chearwae W, Shukla S, Limtrakul P, Ambudkar SV.
Modulation of the function of the multidrug resistance-linked ATP-binding cassette transporter ABCG2 by the cancer chemopreventive agent curcumin.
Mol. Cancer Ther. 5: 1995-2006, 2006.
112)  Calcagno AM, Chewning KJ, Wu CP, Ambudkar SV.
Plasma membrane calcium ATPase (PMCA4): A housekeeper for RT-PCR relative quantification of polytopic membrane proteins.
BMC Mol Biol. 7: 29, 2006.
113)  Seamon JA, Rugg CA, Emanuel S, Calcagno AM, Ambudkar SV, Middleton SA, Butler J, Borowski V, Greenberger LM.
Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.
Mol. Cancer Ther. 5: 2459-67, 2006.
114)  Ludwig JA, Szakács G, Martin SE, Chu BF, Cardarelli C, Sauna ZE, Caplen NJ, Fales HM, Ambudkar SV, Weinstein JN, Gottesman MM.
Selective toxicity of NSC73306 in MDR1-positive cells as a new strategy to circumvent multidrug resistance in cancer.
Cancer Res. 66: 4808-15, 2006.
115)  Ambudkar SV, Kim IW, Xia D, Sauna ZE.
The A-loop, a novel conserved aromatic acid subdomain upstream of the Walker A motif in ABC transporters, is critical for ATP binding.
FEBS Lett. 580: 1049-55, 2006.
116)  Shukla S, Robey RW, Bates SE, Ambudkar SV.
The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2.
Biochemistry. 45: 8940-51, 2006.
117)  Kim IW, Peng XH, Sauna ZE, Fitzgerald PC, Xia D, Müller M, Nandigama K, Ambudkar SV.
The Conserved Tyrosine Residues 401 and 1044 in ATP Sites of Human P-Glycoprotein Are Critical for ATP Binding and Hydrolysis: Evidence for a Conserved Subdomain, the A-Loop in the ATP-Binding Cassette.
Biochemistry. 45: 7605-16, 2006.
118)  Ambudkar SV, Kim IW, Sauna ZE.
The power of the pump: mechanisms of action of P-glycoprotein (ABCB1).
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 27: 392-400, 2006.
119)  Ambudkar SV, Sauna ZE, Gottesman MM, Szakacs G.
A novel way to spread drug resistance in tumor cells: functional intercellular transfer of P-glycoprotein (ABCB1).
Trends Pharmacol Sci. 2005.
120)  Chearwae W, Wu CP, Chu HY, Lee TR, Ambudkar SV, Limtrakul P.
Curcuminoids purified from turmeric powder modulate the function of human multidrug resistance protein 1 (ABCC1).
Cancer Chemother Pharmacol. 1-13, 2005.
121)  Sauna ZE, Shukla S, Ambudkar SV.
Disulfiram, an old drug with new potential therapeutic uses for human cancers and fungal infections.
Mol Biosyst. 1: 127-34, 2005.
122)  Wu CP, Klokouzas A, Hladky SB, Ambudkar SV, Barrand MA.
Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes.
Biochem Pharmacol. 70: 500-10, 2005.
123)  Wu CP, Calcagno AM, Hladky SB, Ambudkar SV, Barrand MA.
Modulatory effects of plant phenols on human multidrug-resistance proteins 1, 4 and 5 (ABCC1, 4 and 5).
FEBS J. 272: 4725-40, 2005.
124)  Jiang Y, Bhattacharjee H, Zhou T, Rosen BP, Ambudkar SV, Sauna ZE.
Nonequivalence of the nucleotide binding domains of the ArsA ATPase.
J Biol Chem. 280: 9921-6, 2005.
125)  Hanson L, May L, Tuma P, Keeven J, Mehl P, Ferenz M, Ambudkar SV, Golin J.
The role of hydrogen bond acceptor groups in the interaction of substrates with Pdr5p, a major yeast drug transporter.
Biochemistry. 44: 9703-13, 2005.
126)  Sauna ZE, Andrus MB, Turner TM, Ambudkar SV.
Biochemical basis of polyvalency as a strategy for enhancing the efficacy of P-glycoprotein (ABCB1) modulators: stipiamide homodimers separated with defined-length spacers reverse drug efflux with greater efficacy.
Biochemistry. 43: 2262-71, 2004.
127)  Chearwae W, Anuchapreeda S, Nandigama K, Ambudkar SV, Limtrakul P.
Biochemical mechanism of modulation of human P-glycoprotein (ABCB1) by curcumin I, II, and III purified from Turmeric powder.
Biochem Pharmacol. 68: 2043-52, 2004.
128)  Shukla S, Sauna ZE, Prasad R, Ambudkar SV.
Disulfiram is a potent modulator of multidrug transporter Cdr1p of Candida albicans.
Biochem Biophys Res Commun. 322: 520-5, 2004.
129)  Sauna ZE, Nandigama K, Ambudkar SV.
Multidrug resistance protein 4 (MRP4/ABCC4)-mediated ATP hydrolysis: Effect of transport substrates and characterization of the post-hydrolysis transition state.
J Biol Chem. 2004.
130)  Polgar O, Robey RW, Morisaki K, Dean M, Michejda C, Sauna ZE, Ambudkar SV, Tarasova N, Bates SE.
Mutational analysis of ABCG2: role of the GXXXG motif.
Biochemistry. 43: 9448-56, 2004.
131)  Shukla S, Ambudkar SV, Prasad R.
Substitution of threonine-1351 in the multidrug transporter Cdr1p of Candida albicans results in hypersusceptibility to antifungal agents and threonine-1351 is essential for synergic effects of calcineurin inhibitor FK520.
J Antimicrob Chemother. 54: 38-45, 2004.
132)  Sauna ZE, Peng XH, Nandigama K, Tekle S, Ambudkar SV.
The molecular basis of the action of disulfiram as a modulator of the multidrug resistance-linked ATP binding cassette transporters MDR1 (ABCB1) and MRP1 (ABCC1).
Mol Pharmacol. 65: 675-84, 2004.
133)  Singh BB, Lockwich TP, Bandyopadhyay BC, Liu X, Bollimuntha S, Brazer SC, Combs C, Das S, Leenders AG, Sheng ZH, Knepper MA, Ambudkar SV, Ambudkar IS.
VAMP2-dependent exocytosis regulates plasma membrane insertion of TRPC3 channels and contributes to agonist-stimulated Ca2+ influx.
Mol Cell. 15: 635-46, 2004.
134)  Shukla S, Saini P, Smriti , Jha S, Ambudkar SV, Prasad R.
Functional characterization of Candida albicans ABC transporter Cdr1p.
Eukaryot Cell. 2: 1361-75, 2003.
135)  Ambudkar SV, Kimchi-Sarfaty C, Sauna ZE, Gottesman MM.
P-glycoprotein: from genomics to mechanism.
Oncogene. 22: 7468-85, 2003.
136)  Golin J, Ambudkar SV, Gottesman MM, Habib AD, Sczepanski J, Ziccardi W, May L.
Studies with novel Pdr5p substrates demonstrate a strong size dependence for xenobiotic efflux.
J Biol Chem. 278: 5963-9, 2003.
137)  Kozak L, Gopal G, Yoon JH, Sauna ZE, Ambudkar SV, Thakurta AG, Dhar R.
Elf1p, a member of the ABC class of ATPases, functions as a mRNA export factor in Schizosacchromyces pombe.
J Biol Chem. 277: 33580-9, 2002.
138)  Müller M, Yong M, Peng XH, Petre B, Arora S, Ambudkar SV.
Evidence for the role of glycosylation in accessibility of the extracellular domains of human MRP1 (ABCC1).
Biochemistry. 41: 10123-32, 2002.
139)  Sauna ZE, Müller M, Peng XH, Ambudkar SV.
Importance of the conserved Walker B glutamate residues, 556 and 1201, for the completion of the catalytic cycle of ATP hydrolysis by human P-glycoprotein (ABCB1).
Biochemistry. 41: 13989-4000, 2002.
140)  Anuchapreeda S, Leechanachai P, Smith MM, Ambudkar SV, Limtrakul PN.
Modulation of P-glycoprotein expression and function by curcumin in multidrug-resistant human KB cells.
Biochem Pharmacol. 64: 573-82, 2002.
141)  Kimchi-Sarfaty C, Kasir J, Ambudkar SV, Rahamimoff H.
Transport activity and surface expression of the Na+-Ca2+ exchanger NCX1 are inhibited by the immunosuppressive agent cyclosporin A and by the nonimmunosuppressive agent PSC833.
J Biol Chem. 277: 2505-10, 2002.
142)  Sauna ZE, Ambudkar SV.
Characterization of the catalytic cycle of ATP hydrolysis by human P-glycoprotein. The two ATP hydrolysis events in a single catalytic cycle are kinetically similar but affect different functional outcomes.
J Biol Chem. 276: 11653-61, 2001.
143)  Kerr KM, Sauna ZE, Ambudkar SV.
Correlation between steady-state ATP hydrolysis and vanadate-induced ADP trapping in Human P-glycoprotein. Evidence for ADP release as the rate-limiting step in the catalytic cycle and its modulation by substrates.
J Biol Chem. 276: 8657-64, 2001.
144)  Sauna ZE, Smith MM, Müller M, Kerr KM, Ambudkar SV.
The mechanism of action of multidrug-resistance-linked P-glycoprotein.
J Bioenerg Biomembr. 33: 481-91, 2001.
145)  Andrus MB, Turner TM, Sauna ZE, Ambudkar SV.
The synthesis and evaluation of a solution phase indexed combinatorial library of non-natural polyenes for reversal of P-glycoprotein mediated multidrug resistance.
J Org Chem. 65: 4973-83, 2000.
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