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Items: 1 to 50 of 61

1.

Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.

Cioffi CL, Racz B, Varadi A, Freeman EE, Conlon MP, Chen P, Zhu L, Kitchen DB, Barnes KD, Martin WH, Pearson PG, Johnson G, Blaner WS, Petrukhin K.

J Med Chem. 2019 Jun 13;62(11):5470-5500. doi: 10.1021/acs.jmedchem.9b00352. Epub 2019 May 28.

2.

Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans.

Podoll T, Pearson PG, Evarts J, Ingallinera T, Bibikova E, Sun H, Gohdes M, Cardinal K, Sanghvi M, Slatter JG.

Drug Metab Dispos. 2019 Feb;47(2):145-154. doi: 10.1124/dmd.118.084459. Epub 2018 Nov 15.

PMID:
30442651
3.

A non-retinoid antagonist of retinol-binding protein 4 rescues phenotype in a model of Stargardt disease without inhibiting the visual cycle.

Racz B, Varadi A, Kong J, Allikmets R, Pearson PG, Johnson G, Cioffi CL, Petrukhin K.

J Biol Chem. 2018 Jul 20;293(29):11574-11588. doi: 10.1074/jbc.RA118.002062. Epub 2018 Jun 5.

4.

ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing's syndrome.

Langlois DK, Fritz MC, Schall WD, Bari Olivier N, Smedley RC, Pearson PG, Bailie MB, Hunt SW 3rd.

BMC Endocr Disord. 2018 May 2;18(1):24. doi: 10.1186/s12902-018-0251-5.

5.

Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.

Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, van Hoek M, de Zwart E, Mittag D, Demont D, Verkaik S, Krantz F, Pearson PG, Ulrich R, Kaptein A.

J Pharmacol Exp Ther. 2017 Nov;363(2):240-252. doi: 10.1124/jpet.117.242909. Epub 2017 Sep 7.

PMID:
28882879
6.

Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.

Cioffi CL, Racz B, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Zhu L, Kitchen DB, Barnes KD, Dobri N, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K.

J Med Chem. 2015 Aug 13;58(15):5863-88. doi: 10.1021/acs.jmedchem.5b00423. Epub 2015 Aug 4.

7.

Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.

Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K.

J Med Chem. 2014 Sep 25;57(18):7731-57. doi: 10.1021/jm5010013. Epub 2014 Sep 11.

8.

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
9.

Copy number variations in three children with sudden infant death.

Toruner GA, Kurvathi R, Sugalski R, Shulman L, Twersky S, Pearson PG, Tozzi R, Schwalb MN, Wallerstein R.

Clin Genet. 2009 Jul;76(1):63-8. doi: 10.1111/j.1399-0004.2009.01161.x.

PMID:
19659761
10.

An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.

Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK.

Drug Metab Dispos. 2009 Mar;37(3):502-13. doi: 10.1124/dmd.108.021931. Epub 2008 Dec 16.

PMID:
19088267
11.

Sleep environment, positional, lifestyle, and demographic characteristics associated with bed sharing in sudden infant death syndrome cases: a population-based study.

Ostfeld BM, Perl H, Esposito L, Hempstead K, Hinnen R, Sandler A, Pearson PG, Hegyi T.

Pediatrics. 2006 Nov;118(5):2051-9.

PMID:
17079578
12.

Hepatic uptake of the novel antifungal agent caspofungin.

Sandhu P, Lee W, Xu X, Leake BF, Yamazaki M, Stone JA, Lin JH, Pearson PG, Kim RB.

Drug Metab Dispos. 2005 May;33(5):676-82. Epub 2005 Feb 16.

PMID:
15716364
13.

Evaluation of microdosing strategies for studies in preclinical drug development: demonstration of linear pharmacokinetics in dogs of a nucleoside analog over a 50-fold dose range.

Sandhu P, Vogel JS, Rose MJ, Ubick EA, Brunner JE, Wallace MA, Adelsberger JK, Baker MP, Henderson PT, Pearson PG, Baillie TA.

Drug Metab Dispos. 2004 Nov;32(11):1254-9. Epub 2004 Jul 30.

PMID:
15286054
14.

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.

Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Guare JP Jr, Egbertson MS, Vacca JP, Huff JR, Felock PJ, Witmer MV, Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen IW, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PG, Schleif WA, Cortese R, Emini E, Summa V, Holloway MK, Young SD.

Proc Natl Acad Sci U S A. 2004 Aug 3;101(31):11233-8. Epub 2004 Jul 26.

15.

Disposition of caspofungin, a novel antifungal agent, in mice, rats, rabbits, and monkeys.

Sandhu P, Xu X, Bondiskey PJ, Balani SK, Morris ML, Tang YS, Miller AR, Pearson PG.

Antimicrob Agents Chemother. 2004 Apr;48(4):1272-80.

16.

Disposition of caspofungin: role of distribution in determining pharmacokinetics in plasma.

Stone JA, Xu X, Winchell GA, Deutsch PJ, Pearson PG, Migoya EM, Mistry GC, Xi L, Miller A, Sandhu P, Singh R, deLuna F, Dilzer SC, Lasseter KC.

Antimicrob Agents Chemother. 2004 Mar;48(3):815-23.

17.

Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.

Kumar S, Kwei GY, Poon GK, Iliff SA, Wang Y, Chen Q, Franklin RB, Didolkar V, Wang RW, Yamazaki M, Chiu SH, Lin JH, Pearson PG, Baillie TA.

J Pharmacol Exp Ther. 2003 Mar;304(3):1161-71.

PMID:
12604693
18.

Metabolic activation of a pyrazinone-containing thrombin inhibitor. Evidence for novel biotransformation involving pyrazinone ring oxidation, rearrangement, and covalent binding to proteins.

Singh R, Silva Elipe MV, Pearson PG, Arison BH, Wong BK, White R, Yu X, Burgey CS, Lin JH, Baillie TA.

Chem Res Toxicol. 2003 Feb;16(2):198-207.

PMID:
12588191
19.
20.

Mechanistic studies on metabolic interactions between gemfibrozil and statins.

Prueksaritanont T, Zhao JJ, Ma B, Roadcap BA, Tang C, Qiu Y, Liu L, Lin JH, Pearson PG, Baillie TA.

J Pharmacol Exp Ther. 2002 Jun;301(3):1042-51.

PMID:
12023536
21.

Glucuronidation of statins in animals and humans: a novel mechanism of statin lactonization.

Prueksaritanont T, Subramanian R, Fang X, Ma B, Qiu Y, Lin JH, Pearson PG, Baillie TA.

Drug Metab Dispos. 2002 May;30(5):505-12.

PMID:
11950779
22.

Enzyme kinetics of cytochrome P450-mediated reactions.

Shou M, Lin Y, Lu P, Tang C, Mei Q, Cui D, Tang W, Ngui JS, Lin CC, Singh R, Wong BK, Yergey JA, Lin JH, Pearson PG, Baillie TA, Rodrigues AD, Rushmore TH.

Curr Drug Metab. 2001 Mar;2(1):17-36. Review.

PMID:
11465149
23.

Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission.

Kassahun K, Pearson PG, Tang W, McIntosh I, Leung K, Elmore C, Dean D, Wang R, Doss G, Baillie TA.

Chem Res Toxicol. 2001 Jan;14(1):62-70.

PMID:
11170509
24.

Metabolites of caspofungin acetate, a potent antifungal agent, in human plasma and urine.

Balani SK, Xu X, Arison BH, Silva MV, Gries A, DeLuna FA, Cui D, Kari PH, Ly T, Hop CE, Singh R, Wallace MA, Dean DC, Lin JH, Pearson PG, Baillie TA.

Drug Metab Dispos. 2000 Nov;28(11):1274-8.

PMID:
11038152
25.

Hormonal effects on tirilazad clearance in women: assessment of the role of CYP3A.

Fleishaker JC, Pearson LK, Pearson PG, Wienkers LC, Hopkins NK, Peters GR.

J Clin Pharmacol. 1999 Mar;39(3):260-7.

PMID:
10073325
26.

Biotransformation of tirilazad in human: 4. effect of finasteride on tirilazad clearance and reduced metabolite formation.

Fleishaker JC, Pearson PG, Wienkers LC, Pearson LK, Moore TA, Peters GR.

J Pharmacol Exp Ther. 1998 Nov;287(2):591-7.

PMID:
9808685
27.

Biotransformation of tirilazad in human: 3. tirilazad A-ring reduction by human liver microsomal 5alpha-reductase type 1 and type 2.

Wienkers LC, Steenwyk RC, Hauer MJ, Fleishaker JC, Pearson PG.

J Pharmacol Exp Ther. 1998 Nov;287(2):583-90.

PMID:
9808684
28.

In vitro metabolic transformations of 2,4-dipyrrolidinylpyrimidine: a chemical probe for P450-mediated oxidation of tirilazad mesylate.

Streeper RT, Pearson PG, Zhao Z, Mizsak SA, Sanders PE, Wienkers LC, Vrbanac JJ.

Xenobiotica. 1997 Nov;27(11):1131-45.

PMID:
9413917
29.

Replacing 14C with stable isotopes in drug metabolism studies.

Abramson FP, Teffera Y, Kusmierz J, Steenwyk RC, Pearson PG.

Drug Metab Dispos. 1996 Jul;24(7):697-701.

PMID:
8818564
30.

Biotransformation of tirilazad in human: 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability.

Fleishaker JC, Pearson PG, Wienkers LC, Pearson LK, Peters GR.

J Pharmacol Exp Ther. 1996 May;277(2):991-8.

PMID:
8627582
31.

Biotransformation of tirilazad in human: 1. Cytochrome P450 3A-mediated hydroxylation of tirilazad mesylate in human liver microsomes.

Wienkers LC, Steenwyk RC, Sanders PE, Pearson PG.

J Pharmacol Exp Ther. 1996 May;277(2):982-90.

PMID:
8627581
32.

Deuterium isotope effect on the metabolism of the flame retardant tris(2,3-dibromopropyl) phosphate in the isolated perfused rat liver.

Van Beerendonk GJ, Pearson PG, Meijer DK, Mulder GJ, Nelson SD, Meerman JH.

Fundam Appl Toxicol. 1995 Nov;28(1):111-7.

PMID:
8566475
33.
34.

In vitro metabolism of tirilazad mesylate in male and female rats. Contribution of cytochrome P4502C11 and delta 4-5 alpha-reductase.

Wienkers LC, Steenwyk RC, Mizsak SA, Pearson PG.

Drug Metab Dispos. 1995 Mar;23(3):383-92.

PMID:
7628305
35.

Blocking of in vitro DNA replication by deoxycytidine adducts of the mutagen and clastogen 2-bromoacrolein.

van Beerendonk GJ, van Gog FB, Vrieling H, Pearson PG, Nelson SD, Meerman JH.

Cancer Res. 1994 Feb 1;54(3):679-84.

36.

Inhibition of in vitro lipid peroxidation by 21-aminosteroids. Evidence for differential mechanisms.

Ryan TP, Steenwyk RC, Pearson PG, Petry TW.

Biochem Pharmacol. 1993 Sep 1;46(5):877-84.

PMID:
8373438
37.

Studies on the metabolic fate of caracemide, an experimental antitumor agent, in the rat. Evidence for the release of methyl isocyanate in vivo.

Slatter JG, Davis MR, Han DH, Pearson PG, Baillie TA.

Chem Res Toxicol. 1993 May-Jun;6(3):335-40.

PMID:
8318655
38.

Metabolic activation of tris(2,3-dibromopropyl)phosphate to reactive intermediates. II. Covalent binding, reactive metabolite formation, and differential metabolite-specific DNA damage in vivo.

Pearson PG, Omichinski JG, Holme JA, McClanahan RH, Brunborg G, Søderlund EJ, Dybing E, Nelson SD.

Toxicol Appl Pharmacol. 1993 Feb;118(2):196-204.

PMID:
8441998
39.

Metabolic activation of tris(2,3-dibromopropyl)phosphate to reactive intermediates. I. Covalent binding and reactive metabolite formation in vitro.

Pearson PG, Omichinski JG, McClanahan RH, Søderlund EJ, Dybing E, Nelson SD.

Toxicol Appl Pharmacol. 1993 Feb;118(2):186-95.

PMID:
8441997
40.

2-Amino-3-(methylamino)propanoic acid (BMAA) bioavailability in the primate.

Duncan MW, Markey SP, Weick BG, Pearson PG, Ziffer H, Hu Y, Kopin IJ.

Neurobiol Aging. 1992 Mar-Apr;13(2):333-7.

PMID:
1522948
41.
42.

2-amino-3-(methylamino)-propanoic acid (BMAA) pharmacokinetics and blood-brain barrier permeability in the rat.

Duncan MW, Villacreses NE, Pearson PG, Wyatt L, Rapoport SI, Kopin IJ, Markey SP, Smith QR.

J Pharmacol Exp Ther. 1991 Jul 1;258(1):27-35.

PMID:
2072299
43.
44.
45.

Testicular metabolism and toxicity of halogenated propanes.

Dybing E, Soderlund EJ, Låg M, Brunborg G, Holme JA, Omichinski JG, Pearson PG, Nelson SD.

Adv Exp Med Biol. 1991;283:471-6. No abstract available.

PMID:
2069019
46.

Metabolic activation of 1,2-dibromo-3-chloropropane to mutagenic metabolites: detection and mechanism of formation of (Z)- and (E)-2-chloro-3-(bromomethyl)oxirane.

Pearson PG, Omichinski JG, Myers TG, Søderlund EJ, Dybing E, Nelson SD.

Chem Res Toxicol. 1990 Sep-Oct;3(5):458-66.

PMID:
2133097
47.

Metabolic activation of 1,2-dibromo-3-chloropropane: evidence for the formation of reactive episulfonium ion intermediates.

Pearson PG, Soderlund EJ, Dybing E, Nelson SD.

Biochemistry. 1990 May 22;29(20):4971-81.

PMID:
2364069
48.

Chemical synthesis and cytotoxic properties of N-alkylcarbamic acid thioesters, metabolites of hepatotoxic formamides.

Han DH, Pearson PG, Baillie TA, Dayal R, Tsang LH, Gescher A.

Chem Res Toxicol. 1990 Mar-Apr;3(2):118-24.

PMID:
2130938
49.

S-(N-methylcarbamoyl)glutathione: a reactive S-linked metabolite of methyl isocyanate.

Pearson PG, Slatter JG, Rashed MS, Han DH, Grillo MP, Baillie TA.

Biochem Biophys Res Commun. 1990 Jan 15;166(1):245-50.

PMID:
2302207
50.

Covalent and noncovalent interactions in acute lethal cell injury caused by chemicals.

Nelson SD, Pearson PG.

Annu Rev Pharmacol Toxicol. 1990;30:169-95. Review. No abstract available.

PMID:
2188567

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