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Items: 22

1.

In Vitro Evaluation of the Drug Interaction Potential of Doravirine.

Bleasby K, Fillgrove KL, Houle R, Lu B, Palamanda J, Newton DJ, Lin M, Chan GH, Sanchez RI.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02492-18. doi: 10.1128/AAC.02492-18. Print 2019 Apr.

PMID:
30745395
2.

Transporters affecting biochemical test results: Creatinine-drug interactions.

Chu X, Bleasby K, Chan GH, Nunes I, Evers R.

Clin Pharmacol Ther. 2016 Nov;100(5):437-440. doi: 10.1002/cpt.445. Epub 2016 Sep 15. Review.

PMID:
27509262
3.

The Complexities of Interpreting Reversible Elevated Serum Creatinine Levels in Drug Development: Does a Correlation with Inhibition of Renal Transporters Exist?

Chu X, Bleasby K, Chan GH, Nunes I, Evers R.

Drug Metab Dispos. 2016 Sep;44(9):1498-509. doi: 10.1124/dmd.115.067694. Epub 2016 Jan 29. Review.

PMID:
26825641
4.

Species differences in drug transporters and implications for translating preclinical findings to humans.

Chu X, Bleasby K, Evers R.

Expert Opin Drug Metab Toxicol. 2013 Mar;9(3):237-52. doi: 10.1517/17425255.2013.741589. Epub 2012 Dec 21. Review.

PMID:
23256482
5.

QSAR Prediction of Passive Permeability in the LLC-PK1 Cell Line: Trends in Molecular Properties and Cross-Prediction of Caco-2 Permeabilities.

Sherer EC, Verras A, Madeira M, Hagmann WK, Sheridan RP, Roberts D, Bleasby K, Cornell WD.

Mol Inform. 2012 Apr;31(3-4):231-45. doi: 10.1002/minf.201100157. Epub 2012 Mar 12.

PMID:
27477094
6.

A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.

Graham TH, Liu W, Verras A, Reibarkh M, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xie D, Xu S, Xiao J, Hale JJ, Pinto S, Shen DM.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2818-22. doi: 10.1016/j.bmcl.2012.02.077. Epub 2012 Mar 1.

PMID:
22444685
7.

A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2811-7. doi: 10.1016/j.bmcl.2012.02.075. Epub 2012 Mar 1.

PMID:
22444683
8.

Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Wu Z, Yang C, Graham TH, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Shen Z, Chen Q, Bleasby K, Sinharoy R, Hale JJ, Tata JR, Pinto S, Colletti SL, Shen DM.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1727-30. doi: 10.1016/j.bmcl.2011.12.098. Epub 2012 Jan 8.

PMID:
22290078
9.

The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.

Graham TH, Shen HC, Liu W, Xiong Y, Verras A, Bleasby K, Bhatt UR, Chabin RM, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Lassman ME, Shen Z, Tong X, Tung EC, Xie D, Xu S, Colletti SL, Tata JR, Hale JJ, Pinto S, Shen DM.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):658-65. doi: 10.1016/j.bmcl.2011.10.060. Epub 2011 Oct 24.

PMID:
22079761
10.

Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy.

Powell DA, Black WC, Bleasby K, Chan CC, Deschenes D, Gagnon M, Gordon R, Guay J, Guiral S, Hafey MJ, Huang Z, Isabel E, Leblanc Y, Styhler A, Xu LJ, Zhang L, Oballa RM.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7281-6. doi: 10.1016/j.bmcl.2011.10.040. Epub 2011 Oct 18.

PMID:
22047692
11.

Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.

Lévesque JF, Bleasby K, Chefson A, Chen A, Dubé D, Ducharme Y, Fournier PA, Gagné S, Gallant M, Grimm E, Hafey M, Han Y, Houle R, Lacombe P, Laliberté S, MacDonald D, Mackay B, Papp R, Tschirret-Guth R.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5547-51. doi: 10.1016/j.bmcl.2011.06.095. Epub 2011 Jun 28.

PMID:
21784634
12.

Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.

Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L.

J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28.

PMID:
21661758
13.

The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease.

Monteagudo E, Fonsi M, Chu X, Bleasby K, Evers R, Pucci V, Orsale MV, Cianetti S, Ferrara M, Harper S, Laufer R, Rowley M, Summa V.

Xenobiotica. 2010 Dec;40(12):826-39. doi: 10.3109/00498254.2010.519061. Epub 2010 Oct 7.

PMID:
20925584
14.

Utility of unbound plasma drug levels and P-glycoprotein transport data in prediction of central nervous system exposure.

He H, Lyons KA, Shen X, Yao Z, Bleasby K, Chan G, Hafey M, Li X, Xu S, Salituro GM, Cohen LH, Tang W.

Xenobiotica. 2009 Sep;39(9):687-93. doi: 10.1080/00498250903015402.

PMID:
19569734
15.

Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.

Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, Hafey M, Evers R, Dean DC, Magriotis PA, Lanza TJ, Lin LS, Hagmann WK, Baillie TA.

Xenobiotica. 2008 Feb;38(2):223-37. doi: 10.1080/00498250701744682 .

PMID:
18197560
16.

Madin-Darby canine kidney II cells: a pharmacologically validated system for NPC1L1-mediated cholesterol uptake.

Weinglass AB, Köhler MG, Nketiah EO, Liu J, Schmalhofer W, Thomas A, Williams B, Beers L, Smith L, Hafey M, Bleasby K, Leone J, Tang YS, Braun M, Ujjainwalla F, McCann ME, Kaczorowski GJ, Garcia ML.

Mol Pharmacol. 2008 Apr;73(4):1072-84. doi: 10.1124/mol.107.043844. Epub 2008 Jan 10.

PMID:
18187582
17.

Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein.

Chu XY, Bleasby K, Yabut J, Cai X, Chan GH, Hafey MJ, Xu S, Bergman AJ, Braun MP, Dean DC, Evers R.

J Pharmacol Exp Ther. 2007 May;321(2):673-83. Epub 2007 Feb 21.

PMID:
17314201
18.

Expression profiles of 50 xenobiotic transporter genes in humans and pre-clinical species: a resource for investigations into drug disposition.

Bleasby K, Castle JC, Roberts CJ, Cheng C, Bailey WJ, Sina JF, Kulkarni AV, Hafey MJ, Evers R, Johnson JM, Ulrich RG, Slatter JG.

Xenobiotica. 2006 Oct-Nov;36(10-11):963-88.

PMID:
17118916
19.

The flounder organic anion transporter fOat has sequence, function, and substrate specificity similarity to both mammalian Oat1 and Oat3.

Aslamkhan AG, Thompson DM, Perry JL, Bleasby K, Wolff NA, Barros S, Miller DS, Pritchard JB.

Am J Physiol Regul Integr Comp Physiol. 2006 Dec;291(6):R1773-80. Epub 2006 Jul 20.

20.

Functional consequences of single nucleotide polymorphisms in the human organic anion transporter hOAT1 (SLC22A6).

Bleasby K, Hall LA, Perry JL, Mohrenweiser HW, Pritchard JB.

J Pharmacol Exp Ther. 2005 Aug;314(2):923-31. Epub 2005 May 24.

PMID:
15914676

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