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Items: 25

1.

Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors.

George DM, Huntley RJ, Cusack K, Duignan DB, Hoemann M, Loud J, Mario R, Melim T, Mullen K, Somal G, Wang L, Edmunds JJ.

PLoS One. 2018 Sep 7;13(9):e0203567. doi: 10.1371/journal.pone.0203567. eCollection 2018.

2.

Navigating tissue chips from development to dissemination: A pharmaceutical industry perspective.

Ewart L, Fabre K, Chakilam A, Dragan Y, Duignan DB, Eswaraka J, Gan J, Guzzie-Peck P, Otieno M, Jeong CG, Keller DA, de Morais SM, Phillips JA, Proctor W, Sura R, Van Vleet T, Watson D, Will Y, Tagle D, Berridge B.

Exp Biol Med (Maywood). 2017 Oct;242(16):1579-1585. doi: 10.1177/1535370217715441. Epub 2017 Jun 16.

3.

Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

Hoemann M, Wilson N, Argiriadi M, Banach D, Burchat A, Calderwood D, Clapham B, Cox P, Duignan DB, Konopacki D, Somal G, Vasudevan A.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5562-5567. doi: 10.1016/j.bmcl.2016.09.077. Epub 2016 Oct 11.

PMID:
27789138
4.

Sphingosine-1-Phosphate (S1P) Lyase Inhibition Causes Increased Cardiac S1P Levels and Bradycardia in Rats.

Harris CM, Mittelstadt S, Banfor P, Bousquet P, Duignan DB, Gintant G, Hart M, Kim Y, Segreti J.

J Pharmacol Exp Ther. 2016 Oct;359(1):151-8. doi: 10.1124/jpet.116.235002. Epub 2016 Aug 12.

PMID:
27519818
5.

Optimized protein kinase Cθ (PKCθ) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis.

George DM, Breinlinger EC, Argiriadi MA, Zhang Y, Wang J, Bansal-Pakala P, Duignan DB, Honore P, Lang Q, Mittelstadt S, Rundell L, Schwartz A, Sun J, Edmunds JJ.

J Med Chem. 2015 Jan 8;58(1):333-46. doi: 10.1021/jm5013006. Epub 2014 Oct 9.

PMID:
25254961
6.

Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit.

George DM, Breinlinger EC, Friedman M, Zhang Y, Wang J, Argiriadi M, Bansal-Pakala P, Barth M, Duignan DB, Honore P, Lang Q, Mittelstadt S, Potin D, Rundell L, Edmunds JJ.

J Med Chem. 2015 Jan 8;58(1):222-36. doi: 10.1021/jm500669m. Epub 2014 Jul 7.

PMID:
25000588
7.

Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.

Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP.

J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24.

PMID:
22196621
8.

pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1.

Varma MV, Rotter CJ, Chupka J, Whalen KM, Duignan DB, Feng B, Litchfield J, Goosen TC, El-Kattan AF.

Mol Pharm. 2011 Aug 1;8(4):1303-13. doi: 10.1021/mp200103h. Epub 2011 Jul 11.

PMID:
21710988
9.

Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.

Pfefferkorn JA, Litchfield J, Hutchings R, Cheng XM, Larsen SD, Auerbach B, Bush MR, Lee C, Erasga N, Bowles DM, Boyles DC, Lu G, Sekerke C, Askew V, Hanselman JC, Dillon L, Lin Z, Robertson A, Olsen K, Boustany C, Atkinson K, Goosen TC, Sahasrabudhe V, Chupka J, Duignan DB, Feng B, Scialis R, Kimoto E, Bi YA, Lai Y, El-Kattan A, Bakker-Arkema R, Barclay P, Kindt E, Le V, Mandema JW, Milad M, Tait BD, Kennedy R, Trivedi BK, Kowala M.

Bioorg Med Chem Lett. 2011 May 1;21(9):2725-31. doi: 10.1016/j.bmcl.2010.11.103. Epub 2010 Nov 26.

PMID:
21183342
10.

Characterization of digoxin uptake in sandwich-cultured human hepatocytes.

Kimoto E, Chupka J, Xiao Y, Bi YA, Duignan DB.

Drug Metab Dispos. 2011 Jan;39(1):47-53. doi: 10.1124/dmd.110.034298. Epub 2010 Oct 6.

PMID:
20926619
11.

Assessment of a micropatterned hepatocyte coculture system to generate major human excretory and circulating drug metabolites.

Wang WW, Khetani SR, Krzyzewski S, Duignan DB, Obach RS.

Drug Metab Dispos. 2010 Oct;38(10):1900-5. doi: 10.1124/dmd.110.034876. Epub 2010 Jul 1.

PMID:
20595376
12.

Understanding the clinical pharmacokinetics of a GABAA partial agonist by application of in vitro tools.

Sawant AD, Miller EL, Duignan DB, Brodfuehrer J, Winter SM, Nelson FR, Kamel A, Obach RS, Vaz AD.

Xenobiotica. 2010 Jul;40(7):476-84. doi: 10.3109/00498254.2010.481057.

PMID:
20429841
13.

Prediction of biliary excretion in rats and humans using molecular weight and quantitative structure-pharmacokinetic relationships.

Yang X, Gandhi YA, Duignan DB, Morris ME.

AAPS J. 2009 Sep;11(3):511-25. doi: 10.1208/s12248-009-9124-1. Epub 2009 Jul 11.

14.

Quantitative expression profile of hepatobiliary transporters in sandwich cultured rat and human hepatocytes.

Li N, Bi YA, Duignan DB, Lai Y.

Mol Pharm. 2009 Jul-Aug;6(4):1180-9. doi: 10.1021/mp900044x.

PMID:
19545175
15.

Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714.

Feng B, Xu JJ, Bi YA, Mireles R, Davidson R, Duignan DB, Campbell S, Kostrubsky VE, Dunn MC, Smith AR, Wang HF.

Toxicol Sci. 2009 Apr;108(2):492-500. doi: 10.1093/toxsci/kfp033. Epub 2009 Feb 17.

PMID:
19223659
16.

The development and validation of a computational model to predict rat liver microsomal clearance.

Chang C, Duignan DB, Johnson KD, Lee PH, Cowan GS, Gifford EM, Stankovic CJ, Lepsy CS, Stoner CL.

J Pharm Sci. 2009 Aug;98(8):2857-67. doi: 10.1002/jps.21651.

PMID:
19116953
17.

High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.

Hop CE, Cole MJ, Davidson RE, Duignan DB, Federico J, Janiszewski JS, Jenkins K, Krueger S, Lebowitz R, Liston TE, Mitchell W, Snyder M, Steyn SJ, Soglia JR, Taylor C, Troutman MD, Umland J, West M, Whalen KM, Zelesky V, Zhao SX.

Curr Drug Metab. 2008 Nov;9(9):847-53. Review.

PMID:
18991580
18.

Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human.

Kalgutkar AS, Feng B, Nguyen HT, Frederick KS, Campbell SD, Hatch HL, Bi YA, Kazolias DC, Davidson RE, Mireles RJ, Duignan DB, Choo EF, Zhao SX.

Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8.

PMID:
17686907
19.

Use of cryopreserved human hepatocytes in sandwich culture to measure hepatobiliary transport.

Bi YA, Kazolias D, Duignan DB.

Drug Metab Dispos. 2006 Sep;34(9):1658-65. Epub 2006 Jun 16.

PMID:
16782767
20.

A 96-well efflux assay to identify ABCG2 substrates using a stably transfected MDCK II cell line.

Xiao Y, Davidson R, Smith A, Pereira D, Zhao S, Soglia J, Gebhard D, de Morais S, Duignan DB.

Mol Pharm. 2006 Jan-Feb;3(1):45-54.

PMID:
16686368
21.

Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.

Sanner MA, Chappie TA, Dunaiskis AR, Fliri AF, Desai KA, Zorn SH, Jackson ER, Johnson CG, Morrone JM, Seymour PA, Majchrzak MJ, Faraci WS, Collins JL, Duignan DB, Prete Di CC, Lee JS, Trozzi A.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30.

PMID:
9871530
22.

Expression and characterization of canine cytochrome P450 2D15.

Roussel F, Duignan DB, Lawton MP, Obach RS, Strick CA, Tweedie DJ.

Arch Biochem Biophys. 1998 Sep 1;357(1):27-36.

PMID:
9721180
23.

The metabolism of xenobiotics and endogenous compounds by the constitutive dog liver cytochrome P450 PBD-2.

Duignan DB, Sipes IG, Ciaccio PJ, Halpert JR.

Arch Biochem Biophys. 1988 Nov 15;267(1):294-304.

PMID:
3143308
24.

Selective inactivation by chloramphenicol of the major phenobarbital-inducible isozyme of dog liver cytochrome P-450.

Ciaccio PJ, Duignan DB, Halpert JR.

Drug Metab Dispos. 1987 Nov-Dec;15(6):852-6.

PMID:
2893713
25.

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