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Items: 36

1.

Expression of cytochrome P450 mRNAs in Type II alveolar cells from subjects with chronic obstructive pulmonary disease.

Kamata S, Fujino N, Yamada M, Grime K, Suzuki S, Ota C, Tando Y, Okada Y, Sakurada A, Noda M, Matsuda Y, Sugiura H, Ichinose M.

Pharmacol Res Perspect. 2018 May 21;6(3):e00405. doi: 10.1002/prp2.405. eCollection 2018 Jun.

2.

Translational model to predict pulmonary pharmacokinetics and efficacy in man for inhaled bronchodilators.

Hendrickx R, Lamm Bergström E, Janzén DLI, Fridén M, Eriksson U, Grime K, Ferguson D.

CPT Pharmacometrics Syst Pharmacol. 2018 Mar;7(3):147-157. doi: 10.1002/psp4.12270. Epub 2017 Dec 27.

3.

Benchmarking of Human Dose Prediction for Inhaled Medicines from Preclinical In Vivo Data.

Ericsson T, Fridén M, Kärrman-Mårdh C, Dainty I, Grime K.

Pharm Res. 2017 Dec;34(12):2557-2567. doi: 10.1007/s11095-017-2218-z. Epub 2017 Jul 6.

PMID:
28685298
4.

Intrinsic Clearance Assay Incubational Binding: A Method Comparison.

Chen S, Prieto Garcia L, Bergström F, Nordell P, Grime K.

Drug Metab Dispos. 2017 Apr;45(4):342-345. doi: 10.1124/dmd.116.074138. Epub 2017 Jan 25.

5.

An S-warfarin and AZD1981 interaction: in vitro and clinical pilot data suggest the N-deacetylated amino acid metabolite as the primary perpetrator.

Grime K, Pehrson R, Nordell P, Gillen M, Kühn W, Mant T, Brännström M, Svanberg P, Jones B, Brealey C.

Br J Clin Pharmacol. 2017 Feb;83(2):381-392. doi: 10.1111/bcp.13102. Epub 2016 Oct 13.

6.

Determination of Human Hepatocyte Intrinsic Clearance for Slowly Metabolized Compounds: Comparison of a Primary Hepatocyte/Stromal Cell Co-culture with Plated Primary Hepatocytes and HepaRG.

Bonn B, Svanberg P, Janefeldt A, Hultman Ia, Grime K.

Drug Metab Dispos. 2016 Apr;44(4):527-33. doi: 10.1124/dmd.115.067769. Epub 2016 Feb 5.

7.

Montelukast Disposition: No Indication of Transporter-Mediated Uptake in OATP2B1 and OATP1B1 Expressing HEK293 Cells.

Brännström M, Nordell P, Bonn B, Davis AM, Palmgren AP, Hilgendorf C, Rubin K, Grime K.

Pharmaceutics. 2015 Dec 15;7(4):554-64. doi: 10.3390/pharmaceutics7040554.

8.

Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists.

Austin RP, Bennion C, Bonnert RV, Cheema L, Cook AR, Cox RJ, Ebden MR, Gaw A, Grime K, Meghani P, Nicholls D, Phillips C, Smith N, Steele J, Stonehouse JP.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1616-20. doi: 10.1016/j.bmcl.2015.01.067. Epub 2015 Feb 3.

PMID:
25708618
9.

HepaRG cells as human-relevant in vitro model to study the effects of inflammatory stimuli on cytochrome P450 isoenzymes.

Rubin K, Janefeldt A, Andersson L, Berke Z, Grime K, Andersson TB.

Drug Metab Dispos. 2015 Jan;43(1):119-25. doi: 10.1124/dmd.114.059246. Epub 2014 Nov 4.

10.

Exploring concepts of in vitro time-dependent CYP inhibition assays.

Stresser DM, Mao J, Kenny JR, Jones BC, Grime K.

Expert Opin Drug Metab Toxicol. 2014 Feb;10(2):157-74. doi: 10.1517/17425255.2014.856882. Epub 2013 Nov 21. Review.

PMID:
24256452
11.

The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.

Mete A, Bowers K, Bull RJ, Coope H, Donald DK, Escott KJ, Ford R, Grime K, Mather A, Ray NC, Russell V.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6248-53. doi: 10.1016/j.bmcl.2013.09.092. Epub 2013 Oct 4.

PMID:
24144851
12.

Evaluation of various static in vitro-in vivo extrapolation models for risk assessment of the CYP3A inhibition potential of an investigational drug.

Vieira ML, Kirby B, Ragueneau-Majlessi I, Galetin A, Chien JY, Einolf HJ, Fahmi OA, Fischer V, Fretland A, Grime K, Hall SD, Higgs R, Plowchalk D, Riley R, Seibert E, Skordos K, Snoeys J, Venkatakrishnan K, Waterhouse T, Obach RS, Berglund EG, Zhang L, Zhao P, Reynolds KS, Huang SM.

Clin Pharmacol Ther. 2014 Feb;95(2):189-98. doi: 10.1038/clpt.2013.187. Epub 2013 Sep 18.

PMID:
24048277
13.

Predicting metabolic clearance for drugs that are actively transported into hepatocytes: incubational binding as a consequence of in vitro hepatocyte concentration is a key factor.

Nordell P, Svanberg P, Bird J, Grime K.

Drug Metab Dispos. 2013 Apr;41(4):836-43. doi: 10.1124/dmd.112.050377. Epub 2013 Jan 30.

14.

Application of in silico, in vitro and preclinical pharmacokinetic data for the effective and efficient prediction of human pharmacokinetics.

Grime KH, Barton P, McGinnity DF.

Mol Pharm. 2013 Apr 1;10(4):1191-206. doi: 10.1021/mp300476z. Epub 2013 Jan 29.

PMID:
23253040
15.

Species differences in biliary clearance and possible relevance of hepatic uptake and efflux transporters involvement.

Grime K, Paine SW.

Drug Metab Dispos. 2013 Feb;41(2):372-8. doi: 10.1124/dmd.112.049312. Epub 2012 Nov 8.

16.

A novel matrix for the short-term storage of cells: utility in drug metabolism and drug transporter studies with rat, dog and human hepatocytes.

Palmgren AP, Fihn BM, Bird J, Courtney P, Grime K.

Xenobiotica. 2013 Jun;43(6):487-97. doi: 10.3109/00498254.2012.738316. Epub 2012 Nov 9.

PMID:
23137276
17.

Optimisation of DMPK by the inhaled route: challenges and approaches.

Cooper AE, Ferguson D, Grime K.

Curr Drug Metab. 2012 May 1;13(4):457-73. Review.

PMID:
22299825
18.

Lead optimisation of pyrazoles as novel FPR1 antagonists.

Morley AD, King S, Roberts B, Lever S, Teobald B, Fisher A, Cook T, Parker B, Wenlock M, Phillips C, Grime K.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):532-6. doi: 10.1016/j.bmcl.2011.10.090. Epub 2011 Nov 4.

PMID:
22094028
19.

The discovery of AZD9164, a novel muscarinic M3 antagonist.

Mete A, Bowers K, Chevalier E, Donald DK, Edwards H, Escott KJ, Ford R, Grime K, Millichip I, Teobald B, Russell V.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7440-6. doi: 10.1016/j.bmcl.2011.10.002. Epub 2011 Oct 8.

PMID:
22047691
21.

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
22.
23.

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.

24.

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.

25.

Time-dependent CYP inhibition.

Riley RJ, Grime K, Weaver R.

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

PMID:
17269894
26.

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
27.

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.

28.
29.

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
30.

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.

31.

Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.

Cumming JG, Brown SJ, Cooper AE, Faull AW, Flynn AP, Grime K, Oldfield J, Shaw JS, Shepherd E, Tucker H, Whittaker D.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3533-6. Epub 2006 May 2.

PMID:
16631366
32.
33.

Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.

Cumming JG, Cooper AE, Grime K, Logan CJ, McLaughlin S, Oldfield J, Shaw JS, Tucker H, Winter J, Whittaker D.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5012-5.

PMID:
16154744
34.
35.

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
36.

Rapid high-performance liquid chromatographic method for the separation of hydroxylated testosterone metabolites.

Whalley PM, Bakes D, Grime K, Weaver RJ.

J Chromatogr B Biomed Sci Appl. 2001 Sep 5;760(2):281-8.

PMID:
11530987

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