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Items: 1 to 50 of 58

1.

Insights into kinetic mechanism of Janus kinase 3 and its inhibition by tofacitinib.

Hekmatnejad M, Conwell S, Lok SM, Kutach A, Shaw D, Fang E, Swinney DC.

Arch Biochem Biophys. 2016 Dec 15;612:22-34. doi: 10.1016/j.abb.2016.08.012. Epub 2016 Aug 20.

PMID:
27555492
2.

Glycogen Synthase Kinase 3β Promotes the Endocytosis of Transferrin in the African Trypanosome.

Guyett PJ, Xia S, Swinney DC, Pollastri MP, Mensa-Wilmot K.

ACS Infect Dis. 2016 Jul 8;2(7):518-28. doi: 10.1021/acsinfecdis.6b00077. Epub 2016 Jun 16.

3.

Challenges and Hurdles to Business as Usual in Drug Development for Treatment of Rare Diseases.

Swinney DC.

Clin Pharmacol Ther. 2016 Oct;100(4):339-41. doi: 10.1002/cpt.422. Epub 2016 Aug 16.

PMID:
27393380
4.

Correction: Intrahepatic Transcriptional Signature Associated with Response to Interferon-α Treatment in the Woodchuck Model of Chronic Hepatitis B.

Fletcher SP, Chin DJ, Gruenbaum L, Bitter H, Rasmussen E, Ravindran P, Swinney DC, Birzele F, Schmucki R, Lorenz SH, Kopetzki E, Carter J, Triyatni M, Thampi LM, Yang J, AlDeghaither D, Murreddu MG, Cote P, Menne S.

PLoS Pathog. 2016 Mar 29;12(3):e1005541. doi: 10.1371/journal.ppat.1005541. eCollection 2016 Mar. No abstract available.

5.

A Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3β.

Swinney ZT, Haubrich BA, Xia S, Ramesha C, Gomez SR, Guyett P, Mensa-Wilmot K, Swinney DC.

PLoS Negl Trop Dis. 2016 Mar 4;10(3):e0004506. doi: 10.1371/journal.pntd.0004506. eCollection 2016 Mar.

6.

On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targets.

Vauquelin G, Van Liefde I, Swinney DC.

Br J Pharmacol. 2016 Apr;173(8):1268-85. doi: 10.1111/bph.13445. Epub 2016 Mar 15. Review.

7.

Enzyme Activity Assays for Protein Kinases: Strategies to Identify Active Substrates.

Haubrich BA, Swinney DC.

Curr Drug Discov Technol. 2016;13(1):2-15. Review.

8.

Radioligand binding to intact cells as a tool for extended drug screening in a representative physiological context.

Vauquelin G, Van Liefde I, Swinney DC.

Drug Discov Today Technol. 2015 Oct;17:28-34. doi: 10.1016/j.ddtec.2015.09.001. Epub 2015 Oct 23. Review.

PMID:
26724334
9.

Intrahepatic Transcriptional Signature Associated with Response to Interferon-α Treatment in the Woodchuck Model of Chronic Hepatitis B.

Fletcher SP, Chin DJ, Gruenbaum L, Bitter H, Rasmussen E, Ravindran P, Swinney DC, Birzele F, Schmucki R, Lorenz SH, Kopetzki E, Carter J, Triyatni M, Thampi LM, Yang J, AlDeghaither D, Murreddu MG, Cote P, Menne S.

PLoS Pathog. 2015 Sep 9;11(9):e1005103. doi: 10.1371/journal.ppat.1005103. eCollection 2015 Sep. Erratum in: PLoS Pathog. 2016 Mar;12(3):e1005541. Murredu, Marta G [corrected to Murreddu, Marta G].

10.

The Role of Binding Kinetics in GPCR Drug Discovery.

Swinney DC, Haubrich BA, Van Liefde I, Vauquelin G.

Curr Top Med Chem. 2015;15(24):2504-22. Review.

PMID:
26126905
11.

Collaboration for rare disease drug discovery research.

Litterman NK, Rhee M, Swinney DC, Ekins S.

F1000Res. 2014 Oct 31;3:261. doi: 10.12688/f1000research.5564.1. eCollection 2014.

12.

The biopharmaceutics risk assessment roadmap for optimizing clinical drug product performance.

Selen A, Dickinson PA, Müllertz A, Crison JR, Mistry HB, Cruañes MT, Martinez MN, Lennernäs H, Wigal TL, Swinney DC, Polli JE, Serajuddin ATM, Cook JA, Dressman JB.

J Pharm Sci. 2014 Nov;103(11):3377-3397. doi: 10.1002/jps.24162. Epub 2014 Sep 24. Review.

PMID:
25256402
13.

The value of translational biomarkers to phenotypic assays.

Swinney DC.

Front Pharmacol. 2014 Jul 15;5:171. doi: 10.3389/fphar.2014.00171. eCollection 2014.

14.

The discovery of medicines for rare diseases.

Swinney DC, Xia S.

Future Med Chem. 2014 Jun;6(9):987-1002. doi: 10.4155/fmc.14.65.

15.

A study of the molecular mechanism of binding kinetics and long residence times of human CCR5 receptor small molecule allosteric ligands.

Swinney DC, Beavis P, Chuang KT, Zheng Y, Lee I, Gee P, Deval J, Rotstein DM, Dioszegi M, Ravendran P, Zhang J, Sankuratri S, Kondru R, Vauquelin G.

Br J Pharmacol. 2014 Jul;171(14):3364-75. doi: 10.1111/bph.12683.

16.

The contribution of mechanistic understanding to phenotypic screening for first-in-class medicines.

Swinney DC.

J Biomol Screen. 2013 Dec;18(10):1186-92. doi: 10.1177/1087057113501199. Epub 2013 Aug 27.

PMID:
23983234
17.

Phenotypic vs. target-based drug discovery for first-in-class medicines.

Swinney DC.

Clin Pharmacol Ther. 2013 Apr;93(4):299-301. doi: 10.1038/clpt.2012.236.

PMID:
23511784
18.

Contrasting roles of mitogen-activated protein kinases in cellular entry and replication of hepatitis C virus: MKNK1 facilitates cell entry.

Kim S, Ishida H, Yamane D, Yi M, Swinney DC, Foung S, Lemon SM.

J Virol. 2013 Apr;87(8):4214-24. doi: 10.1128/JVI.00954-12. Epub 2013 Jan 30.

19.

Transcriptomic analysis of the woodchuck model of chronic hepatitis B.

Fletcher SP, Chin DJ, Ji Y, Iniguez AL, Taillon B, Swinney DC, Ravindran P, Cheng DT, Bitter H, Lopatin U, Ma H, Klumpp K, Menne S.

Hepatology. 2012 Sep;56(3):820-30. doi: 10.1002/hep.25730. Epub 2012 Jul 12.

20.

How were new medicines discovered?

Swinney DC, Anthony J.

Nat Rev Drug Discov. 2011 Jun 24;10(7):507-19. doi: 10.1038/nrd3480. Review.

PMID:
21701501
21.

3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: design and development to a highly selective lead.

Soth M, Abbot S, Abubakari A, Arora N, Arzeno H, Billedeau R, Dewdney N, Durkin K, Frauchiger S, Ghate M, Goldstein DM, Hill RJ, Kuglstatter A, Li F, Loe B, McCaleb K, McIntosh J, Papp E, Park J, Stahl M, Sung ML, Suttman R, Swinney DC, Weller P, Wong B, Zecic H, Gabriel T.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3452-6. doi: 10.1016/j.bmcl.2011.03.098. Epub 2011 Apr 1.

PMID:
21515047
22.

Characterization of the elongation complex of dengue virus RNA polymerase: assembly, kinetics of nucleotide incorporation, and fidelity.

Jin Z, Deval J, Johnson KA, Swinney DC.

J Biol Chem. 2011 Jan 21;286(3):2067-77. doi: 10.1074/jbc.M110.162685. Epub 2010 Nov 15.

23.

Biochemical characterization of the inhibition of the dengue virus RNA polymerase by beta-d-2'-ethynyl-7-deaza-adenosine triphosphate.

Latour DR, Jekle A, Javanbakht H, Henningsen R, Gee P, Lee I, Tran P, Ren S, Kutach AK, Harris SF, Wang SM, Lok SJ, Shaw D, Li J, Heilek G, Klumpp K, Swinney DC, Deval J.

Antiviral Res. 2010 Aug;87(2):213-22. doi: 10.1016/j.antiviral.2010.05.003. Epub 2010 May 12.

PMID:
20470829
24.

Steady-state kinetic characterization of kinase activity and requirements for Mg2+ of interleukin-1 receptor-associated kinase-4.

Hekmat-Nejad M, Cai T, Swinney DC.

Biochemistry. 2010 Feb 23;49(7):1495-506. doi: 10.1021/bi901609m.

PMID:
20104875
25.

The role of binding kinetics in therapeutically useful drug action.

Swinney DC.

Curr Opin Drug Discov Devel. 2009 Jan;12(1):31-9.

PMID:
19152211
26.

Essential role of the N-terminal domain in the regulation of RIG-I ATPase activity.

Gee P, Chua PK, Gevorkyan J, Klumpp K, Najera I, Swinney DC, Deval J.

J Biol Chem. 2008 Apr 4;283(14):9488-96. doi: 10.1074/jbc.M706777200. Epub 2008 Feb 11.

27.

Steady state kinetics of spleen tyrosine kinase investigated by a real time fluorescence assay.

Papp E, Tse JK, Ho H, Wang S, Shaw D, Lee S, Barnett J, Swinney DC, Bradshaw JM.

Biochemistry. 2007 Dec 25;46(51):15103-14. Epub 2007 Dec 1.

PMID:
18052078
28.

Kinetic characterization of human JNK2alpha2 reaction mechanism using substrate competitive inhibitors.

Niu L, Chang KC, Wilson S, Tran P, Zuo F, Swinney DC.

Biochemistry. 2007 Apr 24;46(16):4775-84. Epub 2007 Mar 31.

PMID:
17397142
29.

Activation mechanism and steady state kinetics of Bruton's tyrosine kinase.

Dinh M, Grunberger D, Ho H, Tsing SY, Shaw D, Lee S, Barnett J, Hill RJ, Swinney DC, Bradshaw JM.

J Biol Chem. 2007 Mar 23;282(12):8768-76. Epub 2007 Jan 30.

30.

Opportunities to minimise risk in drug discovery and development.

Swinney DC.

Expert Opin Drug Discov. 2006 Dec;1(7):627-33. doi: 10.1517/17460441.1.7.627.

PMID:
23495989
32.

Successful drug discovery.

Swinney DC.

Curr Top Med Chem. 2006;6(5):403-4. No abstract available.

PMID:
16719799
33.

Cigarette smoke synergistically enhances respiratory mucin induction by proinflammatory stimuli.

Baginski TK, Dabbagh K, Satjawatcharaphong C, Swinney DC.

Am J Respir Cell Mol Biol. 2006 Aug;35(2):165-74. Epub 2006 Mar 16.

PMID:
16543607
34.

Bi-substrate kinetic analysis of an E3-ligase-dependent ubiquitylation reaction.

Swinney DC, Rose MJ, Mak AY, Lee I, Scarafia L, Xu YZ.

Methods Enzymol. 2005;399:323-33.

PMID:
16338366
35.

Biochemical mechanisms of drug action: what does it take for success?

Swinney DC.

Nat Rev Drug Discov. 2004 Sep;3(9):801-8. Review.

PMID:
15340390
36.

A small molecule ubiquitination inhibitor blocks NF-kappa B-dependent cytokine expression in cells and rats.

Swinney DC, Xu YZ, Scarafia LE, Lee I, Mak AY, Gan QF, Ramesha CS, Mulkins MA, Dunn J, So OY, Biegel T, Dinh M, Volkel P, Barnett J, Dalrymple SA, Lee S, Huber M.

J Biol Chem. 2002 Jun 28;277(26):23573-81. Epub 2002 Apr 11.

37.
38.

Quantitative expression analysis of the cellular specificity of HECT-domain ubiquitin E3 ligases.

Scarafia LE, Winter A, Swinney DC.

Physiol Genomics. 2000 Dec 18;4(2):147-153.

PMID:
11120875
41.

Differential allosteric regulation of prostaglandin H synthase 1 and 2 by arachidonic acid.

Swinney DC, Mak AY, Barnett J, Ramesha CS.

J Biol Chem. 1997 May 9;272(19):12393-8.

43.

Cloning and functional expression of the cDNA encoding rat lanosterol 14-alpha demethylase.

Sloane DL, So OY, Leung R, Scarafia LE, Saldou N, Jarnagin K, Swinney DC.

Gene. 1995 Aug 19;161(2):243-8.

PMID:
7665087
44.

Azalanstat (RS-21607), a lanosterol 14 alpha-demethylase inhibitor with cholesterol-lowering activity.

Burton PM, Swinney DC, Heller R, Dunlap B, Chiou M, Malonzo E, Haller J, Walker KA, Salari A, Murakami S, et al.

Biochem Pharmacol. 1995 Aug 8;50(4):529-44.

PMID:
7646560
46.

Selective inhibition of mammalian lanosterol 14 alpha-demethylase by RS-21607 in vitro and in vivo.

Swinney DC, So OY, Watson DM, Berry PW, Webb AS, Kertesz DJ, Shelton EJ, Burton PM, Walker KA.

Biochemistry. 1994 Apr 19;33(15):4702-13.

PMID:
8161528
49.

Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.

Walker KA, Kertesz DJ, Rotstein DM, Swinney DC, Berry PW, So OY, Webb AS, Watson DM, Mak AY, Burton PM, et al.

J Med Chem. 1993 Jul 23;36(15):2235-7. No abstract available.

PMID:
8340925
50.

Cyclosporine metabolism by rat liver microsomes. Evidence for involvement of enzyme(s) other than cytochromes P-450 3A.

Prueksaritanont T, Correia MA, Rettie AE, Swinney DC, Thomas PE, Benet LZ.

Drug Metab Dispos. 1993 Jul-Aug;21(4):730-7.

PMID:
8104135

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