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Items: 43

1.

Application of in vitro CYP and transporter assays to predict clinical drug-drug interactions.

Volpe DA, Balimane PV.

Bioanalysis. 2018 May 1;10(9):619-623. doi: 10.4155/bio-2017-0266. Epub 2018 May 16. No abstract available.

2.

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.

Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7.

PMID:
28002964
3.

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.

Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG.

J Med Chem. 2016 Nov 10;59(21):9837-9854. Epub 2016 Oct 20.

PMID:
27726358
4.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
5.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1.

PMID:
27055941
6.

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

ACS Med Chem Lett. 2016 Jan 19;7(3):283-8. doi: 10.1021/acsmedchemlett.5b00448. eCollection 2016 Mar 10.

7.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10.

PMID:
26924461
8.

Development of novel, 384-well high-throughput assay panels for human drug transporters: drug interaction and safety assessment in support of discovery research.

Tang H, Shen DR, Han YH, Kong Y, Balimane P, Marino A, Gao M, Wu S, Xie D, Soars MG, O'Connell JC, Rodrigues AD, Zhang L, Cvijic ME.

J Biomol Screen. 2013 Oct;18(9):1072-83. doi: 10.1177/1087057113494807.

PMID:
24062352
9.

International Transporter Consortium commentary on clinically important transporter polymorphisms.

Giacomini KM, Balimane PV, Cho SK, Eadon M, Edeki T, Hillgren KM, Huang SM, Sugiyama Y, Weitz D, Wen Y, Xia CQ, Yee SW, Zimdahl H, Niemi M; International Transporter Consortium.

Clin Pharmacol Ther. 2013 Jul;94(1):23-6. doi: 10.1038/clpt.2013.12.

PMID:
23778707
10.

Application of receiver operating characteristic analysis to refine the prediction of potential digoxin drug interactions.

Ellens H, Deng S, Coleman J, Bentz J, Taub ME, Ragueneau-Majlessi I, Chung SP, Herédi-Szabó K, Neuhoff S, Palm J, Balimane P, Zhang L, Jamei M, Hanna I, O'Connor M, Bednarczyk D, Forsgard M, Chu X, Funk C, Guo A, Hillgren KM, Li L, Pak AY, Perloff ES, Rajaraman G, Salphati L, Taur JS, Weitz D, Wortelboer HM, Xia CQ, Xiao G, Yamagata T, Lee CA.

Drug Metab Dispos. 2013 Jul;41(7):1367-74. doi: 10.1124/dmd.112.050542. Epub 2013 Apr 25.

11.

Variability in P-glycoprotein inhibitory potency (IC₅₀) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria.

Bentz J, O'Connor MP, Bednarczyk D, Coleman J, Lee C, Palm J, Pak YA, Perloff ES, Reyner E, Balimane P, Brännström M, Chu X, Funk C, Guo A, Hanna I, Herédi-Szabó K, Hillgren K, Li L, Hollnack-Pusch E, Jamei M, Lin X, Mason AK, Neuhoff S, Patel A, Podila L, Plise E, Rajaraman G, Salphati L, Sands E, Taub ME, Taur JS, Weitz D, Wortelboer HM, Xia CQ, Xiao G, Yabut J, Yamagata T, Zhang L, Ellens H.

Drug Metab Dispos. 2013 Jul;41(7):1347-66. doi: 10.1124/dmd.112.050500. Epub 2013 Apr 25.

12.

Characterization of efflux transporters involved in distribution and disposition of apixaban.

Zhang D, He K, Herbst JJ, Kolb J, Shou W, Wang L, Balimane PV, Han YH, Gan J, Frost CE, Humphreys WG.

Drug Metab Dispos. 2013 Apr;41(4):827-35. doi: 10.1124/dmd.112.050260. Epub 2013 Feb 4.

PMID:
23382458
13.

Cynomolgus monkey as a potential model to assess drug interactions involving hepatic organic anion transporting polypeptides: in vitro, in vivo, and in vitro-to-in vivo extrapolation.

Shen H, Yang Z, Mintier G, Han YH, Chen C, Balimane P, Jemal M, Zhao W, Zhang R, Kallipatti S, Selvam S, Sukrutharaj S, Krishnamurthy P, Marathe P, Rodrigues AD.

J Pharmacol Exp Ther. 2013 Mar;344(3):673-85. doi: 10.1124/jpet.112.200691. Epub 2013 Jan 7.

PMID:
23297161
14.

Generation and characterization of a novel multidrug resistance protein 2 humanized mouse line.

Scheer N, Balimane P, Hayward MD, Buechel S, Kauselmann G, Wolf CR.

Drug Metab Dispos. 2012 Nov;40(11):2212-8. doi: 10.1124/dmd.112.047605. Epub 2012 Aug 23.

PMID:
22917771
15.

Validation of in vitro cell-based human blood-brain barrier model using clinical positron emission tomography radioligands to predict in vivo human brain penetration.

Mabondzo A, Bottlaender M, Guyot AC, Tsaouin K, Deverre JR, Balimane PV.

Mol Pharm. 2010 Oct 4;7(5):1805-15. doi: 10.1021/mp1002366. Epub 2010 Sep 15.

PMID:
20795735
16.

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.

J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u.

PMID:
20405922
17.

SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.

Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21.

PMID:
20153189
18.

Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.

Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM.

J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.

PMID:
19778024
19.

P-gp inhibition potential in cell-based models: which "calculation" method is the most accurate?

Balimane PV, Marino A, Chong S.

AAPS J. 2008 Dec;10(4):577-86. doi: 10.1208/s12248-008-9068-x. Epub 2008 Dec 11.

20.

Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.

Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D.

J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3.

PMID:
18763755
21.

Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.

Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Langley DR, Sang X, Frennesson D, Carboni J, Li A, Greer A, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Vyas D.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4075-80. doi: 10.1016/j.bmcl.2008.05.104. Epub 2008 Jun 21.

PMID:
18572407
22.

Augmentation of SIV DNA vaccine-induced cellular immunity by targeting the 4-1BB costimulatory molecule.

Calarota SA, Hokey DA, Dai A, Jure-Kunkel MN, Balimane P, Weiner DB.

Vaccine. 2008 Jun 13;26(25):3121-34. doi: 10.1016/j.vaccine.2008.02.017. Epub 2008 Feb 22.

PMID:
18336959
23.

2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.

Saulnier MG, Frennesson DB, Wittman MD, Zimmermann K, Velaparthi U, Langley DR, Struzynski C, Sang X, Carboni J, Li A, Greer A, Yang Z, Balimane P, Gottardis M, Attar R, Vyas D.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1702-7. doi: 10.1016/j.bmcl.2008.01.049. Epub 2008 Jan 18.

PMID:
18258427
24.

A novel design of artificial membrane for improving the PAMPA model.

Chen X, Murawski A, Patel K, Crespi CL, Balimane PV.

Pharm Res. 2008 Jul;25(7):1511-20. doi: 10.1007/s11095-007-9517-8. Epub 2008 Jan 10.

PMID:
18185985
25.

Development of an in silico model for predicting efflux substrates in Caco-2 cells.

Zhang L, Balimane PV, Johnson SR, Chong S.

Int J Pharm. 2007 Oct 1;343(1-2):98-105. Epub 2007 May 18.

PMID:
17583455
26.

Development of a quantitative LC-MS/MS analytical method coupled with turbulent flow chromatography for digoxin for the in vitro P-gp inhibition assay.

Smalley J, Marino AM, Xin B, Olah T, Balimane PV.

J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Jul 1;854(1-2):260-7. Epub 2007 May 1.

PMID:
17524973
27.

Peptide transporter substrate identification during permeability screening in drug discovery: comparison of transfected MDCK-hPepT1 cells to Caco-2 cells.

Balimane PV, Chong S, Patel K, Quan Y, Timoszyk J, Han YH, Wang B, Vig B, Faria TN.

Arch Pharm Res. 2007 Apr;30(4):507-18.

PMID:
17489369
28.

Pharmacokinetic drug interactions involving 17alpha-ethinylestradiol: a new look at an old drug.

Zhang H, Cui D, Wang B, Han YH, Balimane P, Yang Z, Sinz M, Rodrigues AD.

Clin Pharmacokinet. 2007;46(2):133-57. Review.

PMID:
17253885
29.

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

Potin D, Launay M, Monatlik F, Malabre P, Fabreguettes M, Fouquet A, Maillet M, Nicolai E, Dorgeret L, Chevallier F, Besse D, Dufort M, Caussade F, Ahmad SZ, Stetsko DK, Skala S, Davis PM, Balimane P, Patel K, Yang Z, Marathe P, Postelneck J, Townsend RM, Goldfarb V, Sheriff S, Einspahr H, Kish K, Malley MF, DiMarco JD, Gougoutas JZ, Kadiyala P, Cheney DL, Tejwani RW, Murphy DK, Mcintyre KW, Yang X, Chao S, Leith L, Xiao Z, Mathur A, Chen BC, Wu DR, Traeger SC, McKinnon M, Barrish JC, Robl JA, Iwanowicz EJ, Suchard SJ, Dhar TG.

J Med Chem. 2006 Nov 30;49(24):6946-9.

PMID:
17125246
30.

Current industrial practices of assessing permeability and P-glycoprotein interaction.

Balimane PV, Han YH, Chong S.

AAPS J. 2006 Jan 13;8(1):E1-13. Review.

31.

Development of an on-line extraction turbulent flow chromatography tandem mass spectrometry method for cassette analysis of Caco-2 cell based bi-directional assay samples.

Smalley J, Kadiyala P, Xin B, Balimane P, Olah T.

J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jan 18;830(2):270-7. Epub 2005 Nov 22.

PMID:
16307910
32.

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.

Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D.

J Med Chem. 2005 Sep 8;48(18):5639-43.

PMID:
16134929
33.
34.

A novel high-throughput automated chip-based nanoelectrospray tandem mass spectrometric method for PAMPA sample analysis.

Balimane PV, Pace E, Chong S, Zhu M, Jemal M, Pelt CK.

J Pharm Biomed Anal. 2005 Sep 1;39(1-2):8-16.

PMID:
15978768
35.

Validation of the 96 well Caco-2 cell culture model for high throughput permeability assessment of discovery compounds.

Marino AM, Yarde M, Patel H, Chong S, Balimane PV.

Int J Pharm. 2005 Jun 13;297(1-2):235-41. Epub 2005 Apr 11.

PMID:
15907606
36.

Cell culture-based models for intestinal permeability: a critique.

Balimane PV, Chong S.

Drug Discov Today. 2005 Mar 1;10(5):335-43. Review.

PMID:
15749282
37.

Utility of 96 well Caco-2 cell system for increased throughput of P-gp screening in drug discovery.

Balimane PV, Patel K, Marino A, Chong S.

Eur J Pharm Biopharm. 2004 Jul;58(1):99-105.

PMID:
15207543
38.

Current methodologies used for evaluation of intestinal permeability and absorption.

Balimane PV, Chong S, Morrison RA.

J Pharmacol Toxicol Methods. 2000 Jul-Aug;44(1):301-12. Review.

PMID:
11274897
39.
40.

Involvement of multiple transporters in the oral absorption of nucleoside analogues.

Balimane PV, Sinko PJ.

Adv Drug Deliv Rev. 1999 Oct 18;39(1-3):183-209.

PMID:
10837774
41.

Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.

Guo A, Hu P, Balimane PV, Leibach FH, Sinko PJ.

J Pharmacol Exp Ther. 1999 Apr;289(1):448-54.

PMID:
10087037
42.

Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.

Balimane PV, Tamai I, Guo A, Nakanishi T, Kitada H, Leibach FH, Tsuji A, Sinko PJ.

Biochem Biophys Res Commun. 1998 Sep 18;250(2):246-51.

PMID:
9753615

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