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Items: 1 to 50 of 89

1.

Development and Characterisation of a Human Hepatocyte Low Intrinsic Clearance Assay for Use in Drug Discovery.

Lancett P, Williamson B, Barton P, Riley RJ.

Drug Metab Dispos. 2018 Jun 7. pii: dmd.118.081596. doi: 10.1124/dmd.118.081596. [Epub ahead of print]

PMID:
29880630
2.

The pharmacokinetics and metabolism of diclofenac in chimeric humanized and murinized FRG mice.

Wilson CE, Dickie AP, Schreiter K, Wehr R, Wilson EM, Bial J, Scheer N, Wilson ID, Riley RJ.

Arch Toxicol. 2018 Jun;92(6):1953-1967. doi: 10.1007/s00204-018-2212-1. Epub 2018 May 2.

PMID:
29721588
3.

Hepatic transporter drug-drug interactions: an evaluation of approaches and methodologies.

Williamson B, Riley RJ.

Expert Opin Drug Metab Toxicol. 2017 Dec;13(12):1237-1250. doi: 10.1080/17425255.2017.1404028. Epub 2017 Nov 23. Review.

PMID:
29121476
4.

The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice.

Dickie AP, Wilson CE, Schreiter K, Wehr R, Wilson EM, Bial J, Scheer N, Wilson ID, Riley RJ.

Biochem Pharmacol. 2017 Jul 1;135:139-150. doi: 10.1016/j.bcp.2017.03.015. Epub 2017 Mar 27.

PMID:
28351678
5.

Harmonised high throughput microsomal stability assay.

Williamson B, Wilson C, Dagnell G, Riley RJ.

J Pharmacol Toxicol Methods. 2017 Mar - Apr;84:31-36. doi: 10.1016/j.vascn.2016.10.006. Epub 2016 Oct 20.

PMID:
27773845
6.

Evaluation of a novel PXR-knockout in HepaRG cells.

Williamson B, Lorbeer M, Mitchell MD, Brayman TG, Riley RJ.

Pharmacol Res Perspect. 2016 Sep 21;4(5):e00264. eCollection 2016 Oct.

7.

Hepatic drug transporters: the journey so far.

Riley RJ, Foley SA, Barton P, Soars MG, Williamson B.

Expert Opin Drug Metab Toxicol. 2016;12(2):201-16. doi: 10.1517/17425255.2016.1132308. Epub 2016 Jan 8. Review.

PMID:
26670591
8.

A new paradigm for navigating compound property related drug attrition.

Barton P, Riley RJ.

Drug Discov Today. 2016 Jan;21(1):72-81. doi: 10.1016/j.drudis.2015.09.010. Epub 2015 Sep 25. Review.

PMID:
26404453
9.

Cytochrome P450 time-dependent inhibition and induction: advances in assays, risk analysis and modelling.

Riley RJ, Wilson CE.

Expert Opin Drug Metab Toxicol. 2015 Apr;11(4):557-72. doi: 10.1517/17425255.2015.1013095. Epub 2015 Feb 8. Review.

PMID:
25659570
10.

Anxiety and stigma in dementia: a threat to aging in place.

Riley RJ, Burgener S, Buckwalter KC.

Nurs Clin North Am. 2014 Jun;49(2):213-31. doi: 10.1016/j.cnur.2014.02.008.

11.

Application of an in vitro OAT assay in drug design and optimization of renal clearance.

Soars MG, Barton P, Elkin LL, Mosure KW, Sproston JL, Riley RJ.

Xenobiotica. 2014 Jul;44(7):657-65. doi: 10.3109/00498254.2013.879625. Epub 2014 Jan 13.

PMID:
24417751
12.

Dissecting the relative contribution of OATP1B1-mediated uptake of xenobiotics into human hepatocytes using siRNA.

Williamson B, Soars AC, Owen A, White P, Riley RJ, Soars MG.

Xenobiotica. 2013 Oct;43(10):920-31. doi: 10.3109/00498254.2013.776194. Epub 2013 Mar 6.

PMID:
23461378
13.

The discovery of CCR3/H1 dual antagonists with reduced hERG risk.

Bahl A, Barton P, Bowers K, Brough S, Evans R, Luckhurst CA, Mochel T, Perry MW, Rigby A, Riley RJ, Sanganee H, Sisson A, Springthorpe B.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6688-93. doi: 10.1016/j.bmcl.2012.08.124. Epub 2012 Sep 15.

PMID:
23031591
14.

Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.

Bahl A, Barton P, Bowers K, Caffrey MV, Denton R, Gilmour P, Hawley S, Linannen T, Luckhurst CA, Mochel T, Perry MW, Riley RJ, Roe E, Springthorpe B, Stein L, Webborn P.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6694-9. doi: 10.1016/j.bmcl.2012.08.103. Epub 2012 Sep 11.

PMID:
23021991
15.

The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.

Soars MG, Barton P, Ismair M, Jupp R, Riley RJ.

Drug Metab Dispos. 2012 Aug;40(8):1641-8. doi: 10.1124/dmd.111.042382. Epub 2012 May 15.

16.

Hepatic uptake in the dog: comparison of uptake in hepatocytes and human embryonic kidney cells expressing dog organic anion-transporting polypeptide 1B4.

Wilby AJ, Maeda K, Courtney PF, Debori Y, Webborn PJ, Kitamura Y, Kusuhara H, Riley RJ, Sugiyama Y.

Drug Metab Dispos. 2011 Dec;39(12):2361-9. doi: 10.1124/dmd.111.041814. Epub 2011 Sep 22.

17.

Coronary artery endothelial transcriptome in vivo: identification of endoplasmic reticulum stress and enhanced reactive oxygen species by gene connectivity network analysis.

Civelek M, Manduchi E, Riley RJ, Stoeckert CJ Jr, Davies PF.

Circ Cardiovasc Genet. 2011 Jun;4(3):243-52. doi: 10.1161/CIRCGENETICS.110.958926. Epub 2011 Apr 14.

18.

Prediction of human renal clearance from preclinical species for a diverse set of drugs that exhibit both active secretion and net reabsorption.

Paine SW, Ménochet K, Denton R, McGinnity DF, Riley RJ.

Drug Metab Dispos. 2011 Jun;39(6):1008-13. doi: 10.1124/dmd.110.037267. Epub 2011 Feb 28.

20.

Prelesional arterial endothelial phenotypes in hypercholesterolemia: universal ABCA1 upregulation contrasts with region-specific gene expression in vivo.

Civelek M, Grant GR, Irolla CR, Shi C, Riley RJ, Chiesa OA, Stoeckert CJ Jr, Karanian JW, Pritchard WF, Davies PF.

Am J Physiol Heart Circ Physiol. 2010 Jan;298(1):H163-70. doi: 10.1152/ajpheart.00652.2009. Epub 2009 Nov 6.

21.

Chronic endoplasmic reticulum stress activates unfolded protein response in arterial endothelium in regions of susceptibility to atherosclerosis.

Civelek M, Manduchi E, Riley RJ, Stoeckert CJ Jr, Davies PF.

Circ Res. 2009 Aug 28;105(5):453-61. doi: 10.1161/CIRCRESAHA.109.203711. Epub 2009 Aug 6.

22.
23.

Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells.

McGinnity DF, Zhang G, Kenny JR, Hamilton GA, Otmani S, Stams KR, Haney S, Brassil P, Stresser DM, Riley RJ.

Drug Metab Dispos. 2009 Jun;37(6):1259-68. doi: 10.1124/dmd.109.026526. Epub 2009 Mar 23.

24.

Mechanism-based inhibition of cytochrome P450 enzymes: an evaluation of early decision making in vitro approaches and drug-drug interaction prediction methods.

Grime KH, Bird J, Ferguson D, Riley RJ.

Eur J Pharm Sci. 2009 Feb 15;36(2-3):175-91. doi: 10.1016/j.ejps.2008.10.002. Epub 2008 Nov 1. Review.

PMID:
19013237
25.

Functional consequences of active hepatic uptake on cytochrome P450 inhibition in rat and human hepatocytes.

Grime K, Webborn PJ, Riley RJ.

Drug Metab Dispos. 2008 Aug;36(8):1670-8. doi: 10.1124/dmd.108.021055. Epub 2008 May 12.

26.

Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes.

Paine SW, Parker AJ, Gardiner P, Webborn PJ, Riley RJ.

Drug Metab Dispos. 2008 Jul;36(7):1365-74. doi: 10.1124/dmd.107.019455. Epub 2008 Apr 21.

27.

Integrated in vitro analysis for the in vivo prediction of cytochrome P450-mediated drug-drug interactions.

McGinnity DF, Waters NJ, Tucker J, Riley RJ.

Drug Metab Dispos. 2008 Jun;36(6):1126-34. doi: 10.1124/dmd.108.020446. Epub 2008 Mar 20.

28.

In vitro-in vivo extrapolation of hepatic clearance involving active uptake: theoretical and experimental aspects.

Webborn PJ, Parker AJ, Denton RL, Riley RJ.

Xenobiotica. 2007 Oct-Nov;37(10-11):1090-109. Review.

PMID:
17968738
29.

Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.

Furber M, Alcaraz L, Bent JE, Beyerbach A, Bowers K, Braddock M, Caffrey MV, Cladingboel D, Collington J, Donald DK, Fagura M, Ince F, Kinchin EC, Laurent C, Lawson M, Luker TJ, Mortimore MM, Pimm AD, Riley RJ, Roberts N, Robertson M, Theaker J, Thorne PV, Weaver R, Webborn P, Willis P.

J Med Chem. 2007 Nov 29;50(24):5882-5. Epub 2007 Oct 27.

PMID:
17963373
30.

From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.

Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. Epub 2007 Aug 19.

PMID:
17827008
31.

Evaluation of human pharmacokinetics, therapeutic dose and exposure predictions using marketed oral drugs.

McGinnity DF, Collington J, Austin RP, Riley RJ.

Curr Drug Metab. 2007 Jun;8(5):463-79.

PMID:
17584017
32.

Use of hepatocytes to assess the contribution of hepatic uptake to clearance in vivo.

Soars MG, Grime K, Sproston JL, Webborn PJ, Riley RJ.

Drug Metab Dispos. 2007 Jun;35(6):859-65. Epub 2007 Mar 7.

33.

Time-dependent CYP inhibition.

Riley RJ, Grime K, Weaver R.

Expert Opin Drug Metab Toxicol. 2007 Feb;3(1):51-66. Review.

PMID:
17269894
34.

The pivotal role of hepatocytes in drug discovery.

Soars MG, McGinnity DF, Grime K, Riley RJ.

Chem Biol Interact. 2007 May 20;168(1):2-15. Epub 2006 Nov 18. Review.

PMID:
17208208
35.

The development of a cocktail CYP2B6, CYP2C8, and CYP3A5 inhibition assay and a preliminary assessment of utility in a drug discovery setting.

O'Donnell CJ, Grime K, Courtney P, Slee D, Riley RJ.

Drug Metab Dispos. 2007 Mar;35(3):381-5. Epub 2006 Dec 1.

36.
37.

Which hydroxy? Evidence for species differences in the regioselectivity of glucuronidation in rat, dog, and human in vitro systems and dog in vivo.

Martin IJ, Lewis RJ, Bernstein MA, Beattie IG, Martin CA, Riley RJ, Springthorpe B.

Drug Metab Dispos. 2006 Sep;34(9):1502-7. Epub 2006 Jun 8.

38.

Comparative analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5.

Soars MG, Grime K, Riley RJ.

Xenobiotica. 2006 Apr;36(4):287-99.

PMID:
16684709
39.

Evaluation of time-dependent cytochrome P450 inhibition using cultured human hepatocytes.

McGinnity DF, Berry AJ, Kenny JR, Grime K, Riley RJ.

Drug Metab Dispos. 2006 Aug;34(8):1291-300. Epub 2006 May 5.

40.
41.

Prediction of CYP2C9-mediated drug-drug interactions: a comparison using data from recombinant enzymes and human hepatocytes.

McGinnity DF, Tucker J, Trigg S, Riley RJ.

Drug Metab Dispos. 2005 Nov;33(11):1700-7. Epub 2005 Aug 4.

42.

A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes.

Riley RJ, McGinnity DF, Austin RP.

Drug Metab Dispos. 2005 Sep;33(9):1304-11. Epub 2005 Jun 2.

43.

The binding of drugs to hepatocytes and its relationship to physicochemical properties.

Austin RP, Barton P, Mohmed S, Riley RJ.

Drug Metab Dispos. 2005 Mar;33(3):419-25. Epub 2004 Dec 22.

44.

Metabolic screening in vitro: metabolic stability, CYP inhibition and induction.

Riley RJ, Grime K.

Drug Discov Today Technol. 2004 Dec;1(4):365-72. doi: 10.1016/j.ddtec.2004.10.008.

PMID:
24981616
45.

Predictive ADMET studies, the challenges and the opportunities.

Davis AM, Riley RJ.

Curr Opin Chem Biol. 2004 Aug;8(4):378-86. Review.

PMID:
15288247
46.

Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance.

McGinnity DF, Soars MG, Urbanowicz RA, Riley RJ.

Drug Metab Dispos. 2004 Nov;32(11):1247-53. Epub 2004 Jul 30.

47.

Cellular models for ADMET predictions and evaluation of drug-drug interactions.

Riley RJ, Kenna JG.

Curr Opin Drug Discov Devel. 2004 Jan;7(1):86-99. Review.

PMID:
14982152
48.
49.

Cloning and characterisation of the first drug-metabolising canine UDP-glucuronosyltransferase of the 2B subfamily.

Soars MG, Fettes M, O'Sullivan AC, Riley RJ, Ethell BT, Burchell B.

Biochem Pharmacol. 2003 Apr 15;65(8):1251-9.

PMID:
12694866
50.

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