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Items: 17


Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs.

Sun H, Piotrowski DW, Orr STM, Warmus JS, Wolford AC, Coffey SB, Futatsugi K, Zhang Y, Vaz ADN.

PLoS One. 2018 Nov 14;13(11):e0206279. doi: 10.1371/journal.pone.0206279. eCollection 2018.


Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Ryder TF, Calabrese MF, Walker GS, Cameron KO, Reyes AR, Borzilleri KA, Delmore J, Miller R, Kurumbail RG, Ward J, Kung DW, Brown JA, Edmonds DJ, Eng H, Wolford AC, Kalgutkar AS.

J Med Chem. 2018 Aug 23;61(16):7273-7288. doi: 10.1021/acs.jmedchem.8b00807. Epub 2018 Aug 2.


Mepolizumab for the treatment of severe eosinophilic asthma.

Poulakos MN, Cargill SM, Waineo MF, Wolford AL Jr.

Am J Health Syst Pharm. 2017 Jul 1;74(13):963-969. doi: 10.2146/ajhp160291. Review.


Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.

Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J.

J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20.


Species Differences in the Oxidative Desulfurization of a Thiouracil-Based Irreversible Myeloperoxidase Inactivator by Flavin-Containing Monooxygenase Enzymes.

Eng H, Sharma R, Wolford A, Di L, Ruggeri RB, Buckbinder L, Conn EL, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2016 Aug;44(8):1262-9. doi: 10.1124/dmd.116.070185. Epub 2016 Apr 14.


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.


Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans.

Dong JQ, Varma MV, Wolford A, Ryder T, Di L, Feng B, Terra SG, Sagawa K, Kalgutkar AS.

Drug Metab Dispos. 2016 Feb;44(2):209-19. doi: 10.1124/dmd.115.067868. Epub 2015 Nov 25.


Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.

Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS.

J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28.


A "middle-out" approach to human pharmacokinetic predictions for OATP substrates using physiologically-based pharmacokinetic modeling.

Li R, Barton HA, Yates PD, Ghosh A, Wolford AC, Riccardi KA, Maurer TS.

J Pharmacokinet Pharmacodyn. 2014 Jun;41(3):197-209. doi: 10.1007/s10928-014-9357-1. Epub 2014 Apr 10.


Toxicities associated with 1-month treatment with propylthiouracil (PTU) and methimazole (MMI) in male rats.

Nambiar PR, Palanisamy GS, Okerberg C, Wolford A, Walters K, Buckbinder L, Reagan WJ.

Toxicol Pathol. 2014 Aug;42(6):970-83. doi: 10.1177/0192623313502708. Epub 2013 Sep 25.


Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

Piotrowski DW, Futatsugi K, Warmus JS, Orr ST, Freeman-Cook KD, Londregan AT, Wei L, Jennings SM, Herr M, Coffey SB, Jiao W, Storer G, Hepworth D, Wang J, Lavergne SY, Chin JE, Hadcock JR, Brenner MB, Wolford AC, Janssen AM, Roush NS, Buxton J, Hinchey T, Kalgutkar AS, Sharma R, Flynn DA.

ACS Med Chem Lett. 2012 Nov 9;4(1):63-8. doi: 10.1021/ml300277t. eCollection 2013 Jan 10.


A novel relay method for determining low-clearance values.

Di L, Trapa P, Obach RS, Atkinson K, Bi YA, Wolford AC, Tan B, McDonald TS, Lai Y, Tremaine LM.

Drug Metab Dispos. 2012 Sep;40(9):1860-5. doi: 10.1124/dmd.112.046425. Epub 2012 May 29.


Immune-mediated agranulocytosis caused by the cocaine adulterant levamisole: a case for reactive metabolite(s) involvement.

Wolford A, McDonald TS, Eng H, Hansel S, Chen Y, Bauman J, Sharma R, Kalgutkar AS.

Drug Metab Dispos. 2012 Jun;40(6):1067-75. doi: 10.1124/dmd.112.045021. Epub 2012 Mar 5. Review.


Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.

Sharma R, Eng H, Walker GS, Barreiro G, Stepan AF, McClure KF, Wolford A, Bonin PD, Cornelius P, Kalgutkar AS.

Chem Res Toxicol. 2011 Dec 19;24(12):2207-16. doi: 10.1021/tx200329k. Epub 2011 Oct 4.


Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.

Robinson RP, Bartlett JA, Bertinato P, Bessire AJ, Cosgrove J, Foley PM, Manion TB, Minich ML, Ramos B, Reese MR, Schmahai TJ, Swick AG, Tess DA, Vaz A, Wolford A.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. doi: 10.1016/j.bmcl.2011.05.099. Epub 2011 Jun 2.


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.


Results of 1236 endoscopic carpal tunnel release procedures using the Brown technique.

Brown MG, Rothenberg ES, Keyser B, Woloszyn TT, Wolford A.

Contemp Orthop. 1993 Sep;27(3):251-8.


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