Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 30

1.

6-Chloro-5-[4-(1-Hydroxycyclobutyl)Phenyl]-1H-Indole-3-Carboxylic Acid is a Highly Selective Substrate for Glucuronidation by UGT1A1, Relative to β-Estradiol.

Lapham K, Lin J, Novak J, Orozco C, Niosi M, Di L, Goosen TC, Ryu S, Riccardi K, Eng H, Cameron KO, Kalgutkar AS.

Drug Metab Dispos. 2018 Dec;46(12):1836-1846. doi: 10.1124/dmd.118.083709. Epub 2018 Sep 7.

PMID:
30194276
2.

Organic Anion Transporter 2-Mediated Hepatic Uptake Contributes to the Clearance of High-Permeability-Low-Molecular-Weight Acid and Zwitterion Drugs: Evaluation Using 25 Drugs.

Kimoto E, Mathialagan S, Tylaska L, Niosi M, Lin J, Carlo AA, Tess DA, Varma MVS.

J Pharmacol Exp Ther. 2018 Nov;367(2):322-334. doi: 10.1124/jpet.118.252049. Epub 2018 Aug 22.

PMID:
30135178
3.

Delineating the role of cooperativity in the design of potent PROTACs for BTK.

Zorba A, Nguyen C, Xu Y, Starr J, Borzilleri K, Smith J, Zhu H, Farley KA, Ding W, Schiemer J, Feng X, Chang JS, Uccello DP, Young JA, Garcia-Irrizary CN, Czabaniuk L, Schuff B, Oliver R, Montgomery J, Hayward MM, Coe J, Chen J, Niosi M, Luthra S, Shah JC, El-Kattan A, Qiu X, West GM, Noe MC, Shanmugasundaram V, Gilbert AM, Brown MF, Calabrese MF.

Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7285-E7292. doi: 10.1073/pnas.1803662115. Epub 2018 Jul 16.

PMID:
30012605
4.

Predicting Human Clearance of Organic Anion Transporting Polypeptide Substrates Using Cynomolgus Monkey: In Vitro-In Vivo Scaling of Hepatic Uptake Clearance.

De Bruyn T, Ufuk A, Cantrill C, Kosa RE, Bi YA, Niosi M, Modi S, Rodrigues AD, Tremaine LM, Varma MVS, Galetin A, Houston JB.

Drug Metab Dispos. 2018 Jul;46(7):989-1000. doi: 10.1124/dmd.118.081315. Epub 2018 May 2.

PMID:
29720472
5.

Data Generated by Quantitative Liquid Chromatography-Mass Spectrometry Proteomics Are Only the Start and Not the Endpoint: Optimization of Quantitative Concatemer-Based Measurement of Hepatic Uridine-5'-Diphosphate-Glucuronosyltransferase Enzymes with Reference to Catalytic Activity.

Achour B, Dantonio A, Niosi M, Novak JJ, Al-Majdoub ZM, Goosen TC, Rostami-Hodjegan A, Barber J.

Drug Metab Dispos. 2018 Jun;46(6):805-812. doi: 10.1124/dmd.117.079475. Epub 2018 Mar 26.

PMID:
29581103
6.

2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.

Dow RL, Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Cortes C, El-Kattan AF, Ford K, Freeman GB, Guimarães CRW, Liu S, Niosi M, Skoura A, Tess D.

J Med Chem. 2018 Apr 12;61(7):3114-3125. doi: 10.1021/acs.jmedchem.8b00152. Epub 2018 Apr 3.

PMID:
29570292
7.

A sensitive method for the quantitation of the peptide-based glucagon-like peptide-1 receptor agonist liraglutide in plasma using microfluidics chromatography tandem MS.

King-Ahmad AJ, Kalgutkar AS, Niosi M, Eng H, Holliman C.

Bioanalysis. 2018 Mar 1;10(5):357-368. doi: 10.4155/bio-2017-0239. Epub 2018 Mar 8.

PMID:
29516741
8.

A Study on Pharmacokinetics of Bosentan with Systems Modeling, Part 2: Prospectively Predicting Systemic and Liver Exposure in Healthy Subjects.

Li R, Kimoto E, Niosi M, Tess DA, Lin J, Tremaine LM, Di L.

Drug Metab Dispos. 2018 Apr;46(4):357-366. doi: 10.1124/dmd.117.078808. Epub 2018 Jan 12. Erratum in: Drug Metab Dispos. 2018 Apr;46(4):484.

PMID:
29330219
9.

A Study on Pharmacokinetics of Bosentan with Systems Modeling, Part 1: Translating Systemic Plasma Concentration to Liver Exposure in Healthy Subjects.

Li R, Niosi M, Johnson N, Tess DA, Kimoto E, Lin J, Yang X, Riccardi KA, Ryu S, El-Kattan AF, Maurer TS, Tremaine LM, Di L.

Drug Metab Dispos. 2018 Apr;46(4):346-356. doi: 10.1124/dmd.117.078790. Epub 2018 Jan 12. Erratum in: Drug Metab Dispos. 2018 Apr;46(4):483.

PMID:
29330218
10.

Quantitative Characterization of Major Hepatic UDP-Glucuronosyltransferase Enzymes in Human Liver Microsomes: Comparison of Two Proteomic Methods and Correlation with Catalytic Activity.

Achour B, Dantonio A, Niosi M, Novak JJ, Fallon JK, Barber J, Smith PC, Rostami-Hodjegan A, Goosen TC.

Drug Metab Dispos. 2017 Oct;45(10):1102-1112. doi: 10.1124/dmd.117.076703. Epub 2017 Aug 2.

11.

Leveraging of Rifampicin-Dosed Cynomolgus Monkeys to Identify Bile Acid 3-O-Sulfate Conjugates as Potential Novel Biomarkers for Organic Anion-Transporting Polypeptides.

Thakare R, Gao H, Kosa RE, Bi YA, Varma MVS, Cerny MA, Sharma R, Kuhn M, Huang B, Liu Y, Yu A, Walker GS, Niosi M, Tremaine L, Alnouti Y, Rodrigues AD.

Drug Metab Dispos. 2017 Jul;45(7):721-733. doi: 10.1124/dmd.117.075275. Epub 2017 Apr 10.

12.

Novel Method to Predict In Vivo Liver-to-Plasma Kpuu for OATP Substrates Using Suspension Hepatocytes.

Riccardi K, Lin J, Li Z, Niosi M, Ryu S, Hua W, Atkinson K, Kosa RE, Litchfield J, Di L.

Drug Metab Dispos. 2017 May;45(5):576-580. doi: 10.1124/dmd.116.074575. Epub 2017 Mar 3.

13.

Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile.

Futatsugi K, Huard K, Kung DW, Pettersen JC, Flynn DA, Gosset JR, Aspnes GE, Barnes RJ, Cabral S, Dowling MS, Fernando DP, Goosen TC, Gorczyca WP, Hepworth D, Herr M, Lavergne S, Li Q, Niosi M, Orr STM, Pardo ID, Perez SM, Purkal J, Schmahai TJ, Shirai N, Shoieb AM, Zhou J, Goodwin B.

Medchemcomm. 2016 Nov 22;8(4):771-779. doi: 10.1039/c6md00564k. eCollection 2017 Apr 1.

14.

Determination of Unbound Partition Coefficient and in Vitro-in Vivo Extrapolation for SLC13A Transporter-Mediated Uptake.

Riccardi K, Li Z, Brown JA, Gorgoglione MF, Niosi M, Gosset J, Huard K, Erion DM, Di L.

Drug Metab Dispos. 2016 Oct;44(10):1633-42. doi: 10.1124/dmd.116.071837. Epub 2016 Jul 14.

15.

Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.

Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM.

J Med Chem. 2016 Feb 11;59(3):1165-75. doi: 10.1021/acs.jmedchem.5b01752. Epub 2016 Jan 27.

PMID:
26734723
16.

Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5).

Huard K, Brown J, Jones JC, Cabral S, Futatsugi K, Gorgoglione M, Lanba A, Vera NB, Zhu Y, Yan Q, Zhou Y, Vernochet C, Riccardi K, Wolford A, Pirman D, Niosi M, Aspnes G, Herr M, Genung NE, Magee TV, Uccello DP, Loria P, Di L, Gosset JR, Hepworth D, Rolph T, Pfefferkorn JA, Erion DM.

Sci Rep. 2015 Dec 1;5:17391. doi: 10.1038/srep17391.

17.

Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase.

Kung DW, Griffith DA, Esler WP, Vajdos FF, Mathiowetz AM, Doran SD, Amor PA, Bagley SW, Banks T, Cabral S, Ford K, Garcia-Irizarry CN, Landis MS, Loomis K, McPherson K, Niosi M, Rockwell KL, Rose C, Smith AC, Southers JA, Tapley S, Tu M, Valentine JJ.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5352-6. doi: 10.1016/j.bmcl.2015.09.035. Epub 2015 Sep 15.

PMID:
26411795
18.

Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).

Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B.

J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006.

PMID:
26349027
19.

Plasma Protein Binding of Challenging Compounds.

Riccardi K, Cawley S, Yates PD, Chang C, Funk C, Niosi M, Lin J, Di L.

J Pharm Sci. 2015 Aug;104(8):2627-36. doi: 10.1002/jps.24506. Epub 2015 Jun 2.

PMID:
26037784
20.

Optimized contrast-enhanced ultrasonography for characterization of focal liver lesions in cirrhosis: A single-center retrospective study.

de Sio I, Iadevaia MD, Vitale LM, Niosi M, Del Prete A, de Sio C, Romano L, Funaro A, Meucci R, Federico A, Loguercio C, Romano M.

United European Gastroenterol J. 2014 Aug;2(4):279-87. doi: 10.1177/2050640614538964.

21.

Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor.

Dow RL, Andrews MP, Li JC, Michael Gibbs E, Guzman-Perez A, Laperle JL, Li Q, Mather D, Munchhof MJ, Niosi M, Patel L, Perreault C, Tapley S, Zavadoski WJ.

Bioorg Med Chem. 2013 Sep 1;21(17):5081-97. doi: 10.1016/j.bmc.2013.06.045. Epub 2013 Jul 1.

PMID:
23871442
22.

Ultrasound-guided percutaneous biopsy for diagnosis of gastrointestinal lesions.

de Sio I, Funaro A, Vitale LM, Niosi M, Francica G, Federico A, Sgambato D, Loguercio C, Romano M.

Dig Liver Dis. 2013 Oct;45(10):816-9. doi: 10.1016/j.dld.2013.04.003. Epub 2013 May 24.

PMID:
23707404
23.

Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections.

Mitton-Fry MJ, Arcari JT, Brown MF, Casavant JM, Finegan SM, Flanagan ME, Gao H, George DM, Gerstenberger BS, Han S, Hardink JR, Harris TM, Hoang T, Huband MD, Irvine R, Lall MS, Megan Lemmon M, Li C, Lin J, McCurdy SP, Mueller JP, Mullins L, Niosi M, Noe MC, Pattavina D, Penzien J, Plummer MS, Risley H, Schuff BP, Shanmugasundaram V, Starr JT, Sun J, Winton J, Young JA.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5989-94. doi: 10.1016/j.bmcl.2012.07.005. Epub 2012 Jul 20. Erratum in: Bioorg Med Chem Lett. 2015 Sep 15;25(18):4029.

PMID:
22892121
24.

Interaction of alcohol intake and cofactors on the risk of cirrhosis.

Stroffolini T, Cotticelli G, Medda E, Niosi M, Del Vecchio-Blanco C, Addolorato G, Petrelli E, Salerno MT, Picardi A, Bernardi M, Almasio P, Bellentani S, Surace LA, Loguercio C.

Liver Int. 2010 Jul;30(6):867-70. doi: 10.1111/j.1478-3231.2010.02261.x. Epub 2010 May 14.

PMID:
20492499
25.

Utility of the carboxylesterase inhibitor bis-para-nitrophenylphosphate (BNPP) in the plasma unbound fraction determination for a hydrolytically unstable amide derivative and agonist of the TGR5 receptor.

Eng H, Niosi M, McDonald TS, Wolford A, Chen Y, Simila ST, Bauman JN, Warmus J, Kalgutkar AS.

Xenobiotica. 2010 Jun;40(6):369-80. doi: 10.3109/00498251003706598.

PMID:
20297923
26.

Emerging drugs for non-alcoholic fatty liver disease.

Federico A, Niosi M, Vecchio Blanco CD, Loguercio C.

Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. doi: 10.1517/14728214.13.1.145 . Review.

PMID:
18321154
27.

The effect of a silybin-vitamin e-phospholipid complex on nonalcoholic fatty liver disease: a pilot study.

Loguercio C, Federico A, Trappoliere M, Tuccillo C, de Sio I, Di Leva A, Niosi M, D'Auria MV, Capasso R, Del Vecchio Blanco C; Real Sud Group.

Dig Dis Sci. 2007 Sep;52(9):2387-95. Epub 2007 Apr 5.

PMID:
17410454
28.

The treatment of NAFLD.

Trappoliere M, Tuccillo C, Federico A, Di Leva A, Niosi M, D'Alessio C, Capasso R, Coppola F, Dauria M, Loguercio C.

Eur Rev Med Pharmacol Sci. 2005 Sep-Oct;9(5):299-304. Review.

PMID:
16231594
29.

[Effects of a new pharmacological complex (silybin + vitamin-E + phospholipids) on some markers of the metabolic syndrome and of liver fibrosis in patients with hepatic steatosis. Preliminary study].

Trappoliere M, Federico A, Tuccillo C, de Sio I, Di Leva A, Niosi M, D'Auria M, Loguercio C; Real Sud Group 2.

Minerva Gastroenterol Dietol. 2005 Jun;51(2):193-9. Italian.

PMID:
15990709
30.

A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats.

Wu G, Whiteside GT, Lee G, Nolan S, Niosi M, Pearson MS, Ilyin VI.

Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53.

PMID:
15507220

Supplemental Content

Support Center