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Items: 44

1.

Pharmacokinetic and Pharmacodynamic Considerations for Drugs Binding to Alpha-1-Acid Glycoprotein.

Smith SA, Waters NJ.

Pharm Res. 2018 Dec 28;36(2):30. doi: 10.1007/s11095-018-2551-x. Review.

PMID:
30593605
2.

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.

Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA.

PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018.

3.

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia.

Stein EM, Garcia-Manero G, Rizzieri DA, Tibes R, Berdeja JG, Savona MR, Jongen-Lavrenic M, Altman JK, Thomson B, Blakemore SJ, Daigle SR, Waters NJ, Suttle AB, Clawson A, Pollock R, Krivtsov A, Armstrong SA, DiMartino J, Hedrick E, Löwenberg B, Tallman MS.

Blood. 2018 Jun 14;131(24):2661-2669. doi: 10.1182/blood-2017-12-818948. Epub 2018 May 3.

4.

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.

Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA.

Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z.

5.

Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in MLL-Rearranged Leukemia.

Campbell CT, Haladyna JN, Drubin DA, Thomson TM, Maria MJ, Yamauchi T, Waters NJ, Olhava EJ, Pollock RM, Smith JJ, Copeland RA, Blakemore SJ, Bernt KM, Daigle SR.

Mol Cancer Ther. 2017 Aug;16(8):1669-1679. doi: 10.1158/1535-7163.MCT-16-0693. Epub 2017 Apr 20.

6.

Implications for Metabolite Quantification by Mass Spectrometry in the Absence of Authentic Standards.

Hatsis P, Waters NJ, Argikar UA.

Drug Metab Dispos. 2017 May;45(5):492-496. doi: 10.1124/dmd.117.075259. Epub 2017 Mar 2.

PMID:
28254953
7.

Preclinical Pharmacokinetics and Pharmacodynamics of Pinometostat (EPZ-5676), a First-in-Class, Small Molecule S-Adenosyl Methionine Competitive Inhibitor of DOT1L.

Waters NJ.

Eur J Drug Metab Pharmacokinet. 2017 Dec;42(6):891-901. doi: 10.1007/s13318-017-0404-3. Review.

PMID:
28229434
8.

Mechanistic investigations into the species differences in pinometostat clearance: impact of binding to alpha-1-acid glycoprotein and permeability-limited hepatic uptake.

Smith SA, Gagnon S, Waters NJ.

Xenobiotica. 2017 Mar;47(3):185-193. doi: 10.3109/00498254.2016.1173265. Epub 2016 May 10.

PMID:
27160567
9.

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.

Duncan KW, Rioux N, Boriack-Sjodin PA, Munchhof MJ, Reiter LA, Majer CR, Jin L, Johnston LD, Chan-Penebre E, Kuplast KG, Porter Scott M, Pollock RM, Waters NJ, Smith JJ, Moyer MP, Copeland RA, Chesworth R.

ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380. eCollection 2016 Feb 11.

10.

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R.

ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11.

11.

Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development.

Rioux N, Waters NJ.

Drug Metab Dispos. 2016 Jul;44(7):934-43. doi: 10.1124/dmd.115.068031. Epub 2016 Mar 2. Review.

PMID:
26936973
12.

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.

Waters NJ, Smith SA, Olhava EJ, Duncan KW, Burton RD, O'Neill J, Rodrigue ME, Pollock RM, Moyer MP, Chesworth R.

Cancer Chemother Pharmacol. 2016 Jan;77(1):43-62. doi: 10.1007/s00280-015-2929-y. Epub 2015 Dec 8.

PMID:
26645404
13.

Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target.

Waters NJ, Daigle SR, Rehlaender BN, Basavapathruni A, Campbell CT, Jensen TB, Truitt BF, Olhava EJ, Pollock RM, Stickland KA, Dovletoglou A.

J Control Release. 2015 Dec 28;220(Pt B):758-65. doi: 10.1016/j.jconrel.2015.09.023. Epub 2015 Sep 15.

PMID:
26385168
14.

Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.

Rioux N, Duncan KW, Lantz RJ, Miao X, Chan-Penebre E, Moyer MP, Munchhof MJ, Copeland RA, Chesworth R, Waters NJ.

Xenobiotica. 2016;46(3):268-77.

PMID:
26294260
15.

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.

Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA.

ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. doi: 10.1021/acsmedchemlett.5b00071. eCollection 2015 Jun 11.

16.

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

Campbell JE, Kuntz KW, Knutson SK, Warholic NM, Keilhack H, Wigle TJ, Raimondi A, Klaus CR, Rioux N, Yokoi A, Kawano S, Minoshima Y, Choi HW, Porter Scott M, Waters NJ, Smith JJ, Chesworth R, Moyer MP, Copeland RA.

ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037. eCollection 2015 May 14.

17.

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.

Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW.

Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27.

PMID:
25915199
18.

Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652.

Rioux N, Mitchell LH, Tiller P, Plant K, Shaw J, Frost K, Ribich S, Moyer MP, Copeland RA, Chesworth R, Waters NJ.

Drug Metab Dispos. 2015 Jul;43(7):936-43. doi: 10.1124/dmd.115.064014. Epub 2015 Apr 17.

PMID:
25887455
19.
20.

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.

Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H.

Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21.

21.

Consideration of the unbound drug concentration in enzyme kinetics.

Waters NJ, Obach RS, Di L.

Methods Mol Biol. 2014;1113:119-45. doi: 10.1007/978-1-62703-758-7_7. Review.

PMID:
24523111
22.

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

Basavapathruni A, Olhava EJ, Daigle SR, Therkelsen CA, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Dovletoglou A, Richon VM, Pollock RM, Copeland RA, Moyer MP, Chesworth R, Pearson PG, Waters NJ.

Biopharm Drug Dispos. 2014 May;35(4):237-52. doi: 10.1002/bdd.1889. Epub 2014 Feb 14.

PMID:
24415392
23.

Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.

Shultz MD, Majumdar D, Chin DN, Fortin PD, Feng Y, Gould T, Kirby CA, Stams T, Waters NJ, Shao W.

J Med Chem. 2013 Sep 12;56(17):7049-59. doi: 10.1021/jm400826j. Epub 2013 Aug 14.

PMID:
23879431
24.

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Touré BB, Visser M, Wang RM, Waters NJ, Shao W.

J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13.

PMID:
23844574
25.

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.

Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Waters NJ, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM.

Blood. 2013 Aug 8;122(6):1017-25. doi: 10.1182/blood-2013-04-497644. Epub 2013 Jun 25.

26.

Comprehensive assessment of human pharmacokinetic prediction based on in vivo animal pharmacokinetic data, part 2: clearance.

Lombardo F, Waters NJ, Argikar UA, Dennehy MK, Zhan J, Gunduz M, Harriman SP, Berellini G, Liric Rajlic I, Obach RS.

J Clin Pharmacol. 2013 Feb;53(2):178-91. doi: 10.1177/0091270012440282. Epub 2013 Jan 24.

PMID:
23436263
27.

Comprehensive assessment of human pharmacokinetic prediction based on in vivo animal pharmacokinetic data, part 1: volume of distribution at steady state.

Lombardo F, Waters NJ, Argikar UA, Dennehy MK, Zhan J, Gunduz M, Harriman SP, Berellini G, Rajlic IL, Obach RS.

J Clin Pharmacol. 2013 Feb;53(2):167-77. doi: 10.1177/0091270012440281. Epub 2013 Jan 24. Erratum in: J Clin Pharmacol. 2013 May;53(5):574.

PMID:
23436262
28.

In silico prediction of total human plasma clearance.

Berellini G, Waters NJ, Lombardo F.

J Chem Inf Model. 2012 Aug 27;52(8):2069-78. doi: 10.1021/ci300155y. Epub 2012 Jul 18.

PMID:
22715914
29.

Protein kinase C inhibitor sotrastaurin selectively inhibits the growth of CD79 mutant diffuse large B-cell lymphomas.

Naylor TL, Tang H, Ratsch BA, Enns A, Loo A, Chen L, Lenz P, Waters NJ, Schuler W, Dörken B, Yao YM, Warmuth M, Lenz G, Stegmeier F.

Cancer Res. 2011 Apr 1;71(7):2643-53. doi: 10.1158/0008-5472.CAN-10-2525. Epub 2011 Feb 15.

30.

Drug design from the ADME/PK perspective: does chemical intuition suffice in multifaceted drug discovery?

Lombando F, Waters NJ.

Curr Top Med Chem. 2011;11(4):331-3. No abstract available.

PMID:
21320061
31.

Selective blockade of oxytocin and vasopressin V(1a) receptors in anaesthetised rats: evidence that activation of oxytocin receptors rather than V(1a) receptors increases sodium excretion.

Shirley DG, Walter MF, Keeler BD, Waters NJ, Walter SJ.

Nephron Physiol. 2011;117(3):p21-6. doi: 10.1159/000320290. Epub 2010 Nov 11.

PMID:
21071981
32.

The role of metabonomics at the interface between drug metabolism and safety assessment.

Waters NJ.

Curr Drug Metab. 2010 Oct;11(8):686-92. Review.

PMID:
20973758
33.

Use of the Øie-Tozer model in understanding mechanisms and determinants of drug distribution.

Waters NJ, Lombardo F.

Drug Metab Dispos. 2010 Jul;38(7):1159-65. doi: 10.1124/dmd.110.032458. Epub 2010 Apr 7.

PMID:
20375179
34.

In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set.

Berellini G, Springer C, Waters NJ, Lombardo F.

J Med Chem. 2009 Jul 23;52(14):4488-95. doi: 10.1021/jm9004658.

PMID:
19603833
35.

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Obach RS, Lombardo F, Waters NJ.

Drug Metab Dispos. 2008 Jul;36(7):1385-405. doi: 10.1124/dmd.108.020479. Epub 2008 Apr 21.

PMID:
18426954
36.

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.

PMID:
18356267
37.

Validation of a rapid equilibrium dialysis approach for the measurement of plasma protein binding.

Waters NJ, Jones R, Williams G, Sohal B.

J Pharm Sci. 2008 Oct;97(10):4586-95. doi: 10.1002/jps.21317.

PMID:
18300299
38.

Quantitative structure activity relationships in drug metabolism.

Chohan KK, Paine SW, Waters NJ.

Curr Top Med Chem. 2006;6(15):1569-78. Review.

PMID:
16918469
39.

Integrated metabonomic analysis of bromobenzene-induced hepatotoxicity: novel induction of 5-oxoprolinosis.

Waters NJ, Waterfield CJ, Farrant RD, Holmes E, Nicholson JK.

J Proteome Res. 2006 Jun;5(6):1448-59.

PMID:
16739996
40.

In silico human and rat Vss quantitative structure-activity relationship models.

Gleeson MP, Waters NJ, Paine SW, Davis AM.

J Med Chem. 2006 Mar 23;49(6):1953-63.

PMID:
16539383
41.

Metabonomic deconvolution of embedded toxicity: application to thioacetamide hepato- and nephrotoxicity.

Waters NJ, Waterfield CJ, Farrant RD, Holmes E, Nicholson JK.

Chem Res Toxicol. 2005 Apr;18(4):639-54.

PMID:
15833024
42.

NMR and pattern recognition studies on liver extracts and intact livers from rats treated with alpha-naphthylisothiocyanate.

Waters NJ, Holmes E, Waterfield CJ, Farrant RD, Nicholson JK.

Biochem Pharmacol. 2002 Jul 1;64(1):67-77.

PMID:
12106607
43.
44.

High-resolution magic angle spinning (1)H NMR spectroscopy of intact liver and kidney: optimization of sample preparation procedures and biochemical stability of tissue during spectral acquisition.

Waters NJ, Garrod S, Farrant RD, Haselden JN, Connor SC, Connelly J, Lindon JC, Holmes E, Nicholson JK.

Anal Biochem. 2000 Jun 15;282(1):16-23.

PMID:
10860494

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