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Items: 41

1.

Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.

Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M.

J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30.

PMID:
30995036
2.

Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.

Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J.

Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29.

3.

Models and Approaches Describing the Metabolism, Transport, and Toxicity of Drugs Administered by the Ocular Route.

Dumouchel JL, Chemuturi N, Milton MN, Camenisch G, Chastain J, Walles M, Sasseville V, Gunduz M, Iyer GR, Argikar UA.

Drug Metab Dispos. 2018 Nov;46(11):1670-1683. doi: 10.1124/dmd.118.082974. Epub 2018 Aug 15. Review.

PMID:
30111625
4.

The mesentery: an ADME perspective on a 'new' organ.

Argikar AA, Argikar UA.

Drug Metab Rev. 2018 Aug;50(3):398-405. doi: 10.1080/03602532.2018.1484756. Epub 2018 Jul 16. Review.

PMID:
30009643
5.

New Perspectives on Acyl Glucuronide Risk Assessment in Drug Discovery: Investigation of In vitro Stability, In situ Reactivity, and Bioactivation.

Gunduz M, Argikar UA, Cirello AL, Dumouchel JL.

Drug Metab Lett. 2018;12(2):84-92. doi: 10.2174/1872312812666180611113656.

6.

Saccharolactone: The History, the Myth, and the Practice.

Argikar UA.

Curr Drug Metab. 2018;19(4):304-309. doi: 10.2174/1389200219666171229232007. Review.

PMID:
29298647
7.

Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.

Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):365-370. doi: 10.1016/j.bmcl.2017.12.037. Epub 2017 Dec 18.

PMID:
29275937
8.

Genotoxicity of 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4] triazolo[4,3-a]pyrazine, a Potent H4 Receptor Antagonist for the Treatment of Allergy: Evidence of Glyoxal Intermediate Involvement.

Gunduz M, Cirello AL, Klimko P, Dumouchel JL, Argikar UA.

Drug Metab Lett. 2017;11(2):144-148. doi: 10.2174/1872312811666171106151730.

PMID:
29110630
9.

Investigation of Ocular Bioactivation Potential and the Role of Cytochrome P450 2D Enzymes in Rat.

Dumouchel JL, Argikar UA, Spear J, Brown A, Dunne CE, Kramlinger VM, Cirello AL, Gunduz M.

Drug Metab Lett. 2017;11(2):102-110. doi: 10.2174/1872312811666170911122919.

PMID:
28891437
10.

Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.

Yamada K, Levell J, Yoon T, Kohls D, Yowe D, Rigel DF, Imase H, Yuan J, Yasoshima K, DiPetrillo K, Monovich L, Xu L, Zhu M, Kato M, Jain M, Idamakanti N, Taslimi P, Kawanami T, Argikar UA, Kunjathoor V, Xie X, Yagi YI, Iwaki Y, Robinson Z, Park HM.

J Med Chem. 2017 Aug 24;60(16):7099-7107. doi: 10.1021/acs.jmedchem.7b00708. Epub 2017 Aug 3.

PMID:
28771350
11.

Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.

Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J.

J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30.

PMID:
28621538
12.

Ocular non-P450 oxidative, reductive, hydrolytic, and conjugative drug metabolizing enzymes.

Argikar UA, Dumouchel JL, Dunne CE, Bushee AJ.

Drug Metab Rev. 2017 Aug;49(3):372-394. doi: 10.1080/03602532.2017.1322609. Epub 2017 May 17. Review.

PMID:
28438049
13.

Do We Need to Study Metabolism and Distribution in the Eye: Why, When, and Are We There Yet?

Argikar UA, Dumouchel JL, Kramlinger VM, Cirello AL, Gunduz M, Dunne CE, Sohal B.

J Pharm Sci. 2017 Sep;106(9):2276-2281. doi: 10.1016/j.xphs.2017.03.008. Epub 2017 Mar 18. Review.

PMID:
28322939
14.

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
15.

In vitro ocular metabolism and bioactivation of ketoconazole in rat, rabbit and human.

Cirello AL, Dumouchel JL, Gunduz M, Dunne CE, Argikar UA.

Drug Metab Pharmacokinet. 2017 Apr;32(2):121-126. doi: 10.1016/j.dmpk.2016.11.001. Epub 2016 Nov 19.

PMID:
28139372
17.

Compound Property Optimization in Drug Discovery Using Quantitative Surface Sampling Micro Liquid Chromatography with Tandem Mass Spectrometry.

Chen X, Hatsis P, Judge J, Argikar UA, Ren X, Sarber J, Mansfield K, Liang G, Amaral A, Catoire A, Bentley A, Ramos L, Moench P, Hintermann S, Carcache D, Glick J, Flarakos J.

Anal Chem. 2016 Dec 6;88(23):11813-11820. Epub 2016 Nov 16.

PMID:
27797491
18.

Ocular Metabolism of Levobunolol: Historic and Emerging Metabolic Pathways.

Argikar UA, Dumouchel JL, Dunne CE, Saran C, Cirello AL, Gunduz M.

Drug Metab Dispos. 2016 Aug;44(8):1304-12. doi: 10.1124/dmd.116.070458. Epub 2016 May 17.

PMID:
27190057
19.

An in vitro approach to investigate ocular metabolism of a topical, selective β1-adrenergic blocking agent, betaxolol.

Bushee JL, Dunne CE, Argikar UA.

Xenobiotica. 2015 May;45(5):396-405. doi: 10.3109/00498254.2014.987191. Epub 2014 Dec 5.

PMID:
25475994
20.

A numerical method for analysis of in vitro time-dependent inhibition data. Part 2. Application to experimental data.

Korzekwa K, Tweedie D, Argikar UA, Whitcher-Johnstone A, Bell L, Bickford S, Nagar S.

Drug Metab Dispos. 2014 Sep;42(9):1587-95. doi: 10.1124/dmd.114.058297. Epub 2014 Jun 17.

21.

Case study 2. Practical analytical considerations for conducting in vitro enzyme kinetic studies.

Argikar UA, Nagar S.

Methods Mol Biol. 2014;1113:431-9. doi: 10.1007/978-1-62703-758-7_19.

PMID:
24523123
22.

Enzyme kinetics in drug metabolism: fundamentals and applications.

Nagar S, Argikar UA, Tweedie DJ.

Methods Mol Biol. 2014;1113:1-6. doi: 10.1007/978-1-62703-758-7_1.

PMID:
24523105
23.

Identification of saturated and unsaturated fatty acids released during microsomal incubations.

Bushee JL, Liang G, Dunne CE, Harriman SP, Argikar UA.

Xenobiotica. 2014 Aug;44(8):687-95. doi: 10.3109/00498254.2014.884253. Epub 2014 Feb 6.

PMID:
24502389
24.

Identification of domperidone metabolites in plasma and urine of gastroparesis patients with LC-ESI-MS/MS.

Youssef AS, Argikar UA, Pathikonda M, Parkman HP, Nagar S.

Xenobiotica. 2013 Dec;43(12):1073-83. doi: 10.3109/00498254.2013.797623. Epub 2013 May 24.

PMID:
23705785
25.

Metabolism of bromopride in mouse, rat, rabbit, dog, monkey, and human hepatocytes.

Dunne CE, Bushee JL, Argikar UA.

Drug Metab Pharmacokinet. 2013;28(6):453-61. Epub 2013 Apr 23.

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.

Oxidative ipso substitution of 2,4-difluoro-benzylphthalazines: identification of a rare stable quinone methide and subsequent GSH conjugate.

Gunduz M, Argikar UA, Kamel A, Colizza K, Bushee JL, Cirello A, Lombardo F, Harriman S.

Drug Metab Dispos. 2012 Nov;40(11):2074-80. doi: 10.1124/dmd.112.046268. Epub 2012 Jul 30.

PMID:
22851614
29.

Unusual glucuronides.

Argikar UA.

Drug Metab Dispos. 2012 Jul;40(7):1239-51. doi: 10.1124/dmd.112.045096. Epub 2012 Apr 19. Review.

PMID:
22517971
30.

Functional analysis of UGT1A4(P24T) and UGT1A4(L48V) variant enzymes.

Zhou J, Argikar UA, Remmel RP.

Pharmacogenomics. 2011 Dec;12(12):1671-9. doi: 10.2217/pgs.11.105. Epub 2011 Nov 2.

PMID:
22047493
31.

An experimental approach to enhance precursor ion fragmentation for metabolite identification studies: application of dual collision cells in an orbital trap.

Bushee JL, Argikar UA.

Rapid Commun Mass Spectrom. 2011 May 30;25(10):1356-62. doi: 10.1002/rcm.4996.

PMID:
21504000
32.

Strategies and chemical design approaches to reduce the potential for formation of reactive metabolic species.

Argikar UA, Mangold JB, Harriman SP.

Curr Top Med Chem. 2011;11(4):419-49. Review.

PMID:
21320068
33.
34.

Identification of novel metoclopramide metabolites in humans: in vitro and in vivo studies.

Argikar UA, Gomez J, Ung D, Parkman HP, Nagar S.

Drug Metab Dispos. 2010 Aug;38(8):1295-307. doi: 10.1124/dmd.110.033357. Epub 2010 Apr 27. Erratum in: Drug Metab Dispos. 2012 Sep;40(9):1866-7.

PMID:
20423954
35.

Identification of a novel N-carbamoyl glucuronide: in vitro, in vivo, and mechanistic studies.

Gunduz M, Argikar UA, Baeschlin D, Ferreira S, Hosagrahara V, Harriman S.

Drug Metab Dispos. 2010 Mar;38(3):361-7. doi: 10.1124/dmd.109.030650. Epub 2009 Dec 11.

PMID:
20008038
36.

Studies on induction of lamotrigine metabolism in transgenic UGT1 mice.

Argikar UA, Senekeo-Effenberger K, Larson EE, Tukey RH, Remmel RP.

Xenobiotica. 2009 Nov;39(11):826-35. doi: 10.3109/00498250903188985.

37.

Variation in glucuronidation of lamotrigine in human liver microsomes.

Argikar UA, Remmel RP.

Xenobiotica. 2009 May;39(5):355-63. doi: 10.1080/00498250902745082.

PMID:
19387891
38.

Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10.

Argikar UA, Remmel RP.

Drug Metab Dispos. 2009 Jan;37(1):229-36. doi: 10.1124/dmd.108.022426. Epub 2008 Oct 6.

39.

Update on tools for evaluation of uridine diphosphoglucuronosyltransferase polymorphisms.

Argikar UA, Iwuchukwu OF, Nagar S.

Expert Opin Drug Metab Toxicol. 2008 Jul;4(7):879-94. doi: 10.1517/17425255.4.7.879 . Review.

PMID:
18624677
40.

Paradoxical urinary phenytoin metabolite (S)/(R) ratios in CYP2C19*1/*2 patients.

Argikar UA, Cloyd JC, Birnbaum AK, Leppik IE, Conway J, Kshirsagar S, Oetting WS, Klein EC, Remmel RP.

Epilepsy Res. 2006 Sep;71(1):54-63. Epub 2006 Jul 3.

PMID:
16815679
41.

Rapid, large-scale formation of porcine hepatocyte spheroids in a novel spheroid reservoir bioartificial liver.

Nyberg SL, Hardin J, Amiot B, Argikar UA, Remmel RP, Rinaldo P.

Liver Transpl. 2005 Aug;11(8):901-10.

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