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Targeting a ceramide double bond improves insulin resistance and hepatic steatosis.

Chaurasia B, Tippetts TS, Mayoral Monibas R, Liu J, Li Y, Wang L, Wilkerson JL, Sweeney CR, Pereira RF, Sumida DH, Maschek JA, Cox JE, Kaddai V, Lancaster GI, Siddique MM, Poss A, Pearson M, Satapati S, Zhou H, McLaren DG, Previs SF, Chen Y, Qian Y, Petrov A, Wu M, Shen X, Yao J, Nunes CN, Howard AD, Wang L, Erion MD, Rutter J, Holland WL, Kelley DE, Summers SA.

Science. 2019 Jul 26;365(6451):386-392. doi: 10.1126/science.aav3722. Epub 2019 Jul 4.


Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver.

Muise ES, Guan HP, Liu J, Nawrocki AR, Yang X, Wang C, Rodríguez CG, Zhou D, Gorski JN, Kurtz MM, Feng D, Leavitt KJ, Wei L, Wilkening RR, Apgar JM, Xu S, Lu K, Feng W, Li Y, He H, Previs SF, Shen X, van Heek M, Souza SC, Rosenbach MJ, Biftu T, Erion MD, Kelley DE, Kemp DM, Myers RW, Sebhat IK.

PLoS One. 2019 Feb 27;14(2):e0211568. doi: 10.1371/journal.pone.0211568. eCollection 2019.


A Long-Acting PYY3-36 Analog Mediates Robust Anorectic Efficacy with Minimal Emesis in Nonhuman Primates.

Rangwala SM, D'Aquino K, Zhang YM, Bader L, Edwards W, Zheng S, Eckardt A, Lacombe A, Pick R, Moreno V, Kang L, Jian W, Arnoult E, Case M, Jenkinson C, Chi E, Swanson RV, Kievit P, Grove K, Macielag M, Erion MD, SinhaRoy R, Leonard JN.

Cell Metab. 2019 Apr 2;29(4):837-843.e5. doi: 10.1016/j.cmet.2019.01.017. Epub 2019 Feb 14.


Using [2H]water to quantify the contribution of de novo palmitate synthesis in plasma: enabling back-to-back studies.

Previs SF, Herath K, Nawrocki AR, Rodriguez CG, Slipetz D, Singh SB, Kang L, Bhat G, Roddy TP, Conarello S, Terebetski J, Erion MD, Kelley DE.

Am J Physiol Endocrinol Metab. 2018 Jul 1;315(1):E63-E71. doi: 10.1152/ajpendo.00010.2017. Epub 2018 Jan 2.


A glucose-responsive insulin therapy protects animals against hypoglycemia.

Yang R, Wu M, Lin S, Nargund RP, Li X, Kelly T, Yan L, Dai G, Qian Y, Dallas-Yang Q, Fischer PA, Cui Y, Shen X, Huo P, Feng DD, Erion MD, Kelley DE, Mu J.

JCI Insight. 2018 Jan 11;3(1). pii: 97476. doi: 10.1172/jci.insight.97476. eCollection 2018 Jan 11.


Enhancing Studies of Pharmacodynamic Mechanisms via Measurements of Metabolic Flux: Fundamental Concepts and Guiding Principles for Using Stable Isotope Tracers.

Daurio NA, Wang SP, Chen Y, Zhou H, McLaren DG, Roddy TP, Johns DG, Milot D, Kasumov T, Erion MD, Kelley DE, Previs SF.

J Pharmacol Exp Ther. 2017 Oct;363(1):80-91. doi: 10.1124/jpet.117.241091. Epub 2017 Jul 19. Review.


Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.

Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE, Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M, Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM, Sebhat IK.

Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13.


Quantifying rates of glucose production in vivo following an intraperitoneal tracer bolus.

Wang SP, Zhou D, Yao Z, Satapati S, Chen Y, Daurio NA, Petrov A, Shen X, Metzger D, Yin W, Nawrocki AR, Eiermann GJ, Hwa J, Fancourt C, Miller C, Herath K, Roddy TP, Slipetz D, Erion MD, Previs SF, Kelley DE.

Am J Physiol Endocrinol Metab. 2016 Dec 1;311(6):E911-E921. doi: 10.1152/ajpendo.00182.2016. Epub 2016 Sep 20.


Physiological Expression of AMPKγ2RG Mutation Causes Wolff-Parkinson-White Syndrome and Induces Kidney Injury in Mice.

Yang X, Mudgett J, Bou-About G, Champy MF, Jacobs H, Monassier L, Pavlovic G, Sorg T, Herault Y, Petit-Demoulière B, Lu K, Feng W, Wang H, Ma LJ, Askew R, Erion MD, Kelley DE, Myers RW, Li C, Guan HP.

J Biol Chem. 2016 Nov 4;291(45):23428-23439. Epub 2016 Sep 12.


Glucagon receptor antagonism induces increased cholesterol absorption.

Guan HP, Yang X, Lu K, Wang SP, Castro-Perez JM, Previs S, Wright M, Shah V, Herath K, Xie D, Szeto D, Forrest G, Xiao JC, Palyha O, Sun LP, Andryuk PJ, Engel SS, Xiong Y, Lin S, Kelley DE, Erion MD, Davis HR, Wang L.

J Lipid Res. 2015 Nov;56(11):2183-95. doi: 10.1194/jlr.M060897. Epub 2015 Sep 15.


Free energy calculations to estimate ligand-binding affinities in structure-based drug design.

Reddy MR, Reddy CR, Rathore RS, Erion MD, Aparoy P, Reddy RN, Reddanna P.

Curr Pharm Des. 2014;20(20):3323-37. Review.


Advances in binding free energies calculations: QM/MM-based free energy perturbation method for drug design.

Rathore RS, Sumakanth M, Reddy MS, Reddanna P, Rao AA, Erion MD, Reddy MR.

Curr Pharm Des. 2013;19(26):4674-86. Review.


Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents.

Day JW, Gelfanov V, Smiley D, Carrington PE, Eiermann G, Chicchi G, Erion MD, Gidda J, Thornberry NA, Tschöp MH, Marsh DJ, SinhaRoy R, DiMarchi R, Pocai A.

Biopolymers. 2012;98(5):443-50. doi: 10.1002/bip.22072.


Chronic treatment with a glucokinase activator delays the onset of hyperglycaemia and preserves beta cell mass in the Zucker diabetic fatty rat.

Futamura M, Yao J, Li X, Bergeron R, Tran JL, Zycband E, Woods J, Zhu Y, Shao Q, Maruki-Uchida H, Goto-Shimazaki H, Langdon RB, Erion MD, Eiki J, Zhou YP.

Diabetologia. 2012 Apr;55(4):1071-80. doi: 10.1007/s00125-011-2439-3. Epub 2012 Jan 11.


Antiviral efficacy upon administration of a HepDirect prodrug of 2'-C-methylcytidine to hepatitis C virus-infected chimpanzees.

Carroll SS, Koeplinger K, Vavrek M, Zhang NR, Handt L, MacCoss M, Olsen DB, Reddy KR, Sun Z, van Poelje PD, Fujitaki JM, Boyer SH, Linemeyer DL, Hecker SJ, Erion MD.

Antimicrob Agents Chemother. 2011 Aug;55(8):3854-60. doi: 10.1128/AAC.01152-10. Epub 2011 May 31.


Fructose-1, 6-bisphosphatase inhibitors for reducing excessive endogenous glucose production in type 2 diabetes.

van Poelje PD, Potter SC, Erion MD.

Handb Exp Pharmacol. 2011;(203):279-301. doi: 10.1007/978-3-642-17214-4_12. Review.


A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis.

Gómez-Galeno JE, Dang Q, Nguyen TH, Boyer SH, Grote MP, Sun Z, Chen M, Craigo WA, van Poelje PD, MacKenna DA, Cable EE, Rolzin PA, Finn PD, Chi B, Linemeyer DL, Hecker SJ, Erion MD.

ACS Med Chem Lett. 2010 Aug 30;1(9):478-82. doi: 10.1021/ml100143q. eCollection 2010 Dec 9.


Discovery of a series of phosphonic acid-containing thiazoles and orally bioavailable diamide prodrugs that lower glucose in diabetic animals through inhibition of fructose-1,6-bisphosphatase.

Dang Q, Liu Y, Cashion DK, Kasibhatla SR, Jiang T, Taplin F, Jacintho JD, Li H, Sun Z, Fan Y, DaRe J, Tian F, Li W, Gibson T, Lemus R, van Poelje PD, Potter SC, Erion MD.

J Med Chem. 2011 Jan 13;54(1):153-65. doi: 10.1021/jm101035x. Epub 2010 Dec 2.


Synthesis of 3'-amino-3'-deoxyguanosine and 3'-amino-3'-deoxyxyloguanosine monophosphate HepDirect prodrugs from guanosine.

Bookser BC, Raffaele NB, Reddy KR, Fan K, Huang W, Erion MD.

Nucleosides Nucleotides Nucleic Acids. 2009 Oct;28(10):969-86. doi: 10.1080/15257770903307151.


Fructose-1,6-bisphosphatase Inhibitors. 2. Design, synthesis, and structure-activity relationship of a series of phosphonic acid containing benzimidazoles that function as 5'-adenosinemonophosphate (AMP) mimics.

Dang Q, Kasibhatla SR, Xiao W, Liu Y, Dare J, Taplin F, Reddy KR, Scarlato GR, Gibson T, van Poelje PD, Potter SC, Erion MD.

J Med Chem. 2010 Jan 14;53(1):441-51. doi: 10.1021/jm901420x.


Relative solvation free energies calculated using an ab initio QM/MM-based free energy perturbation method: dependence of results on simulation length.

Reddy MR, Erion MD.

J Comput Aided Mol Des. 2009 Dec;23(12):837-43. doi: 10.1007/s10822-009-9300-5. Epub 2009 Sep 17.


Fructose-1,6-bisphosphatase inhibitors. 1. Purine phosphonic acids as novel AMP mimics.

Dang Q, Brown BS, Liu Y, Rydzewski RM, Robinson ED, van Poelje PD, Reddy MR, Erion MD.

J Med Chem. 2009 May 14;52(9):2880-98. doi: 10.1021/jm900078f.


Delivery of high levels of anti-proliferative nucleoside triphosphates to CYP3A-expressing cells as a potential treatment for hepatocellular carcinoma.

MacKenna DA, Montag A, Boyer SH, Linemeyer DL, Erion MD.

Cancer Chemother Pharmacol. 2009 Oct;64(5):981-91. doi: 10.1007/s00280-009-0953-5. Epub 2009 Mar 13.


Thyroid hormone beta receptor activation has additive cholesterol lowering activity in combination with atorvastatin in rabbits, dogs and monkeys.

Ito BR, Zhang BH, Cable EE, Song X, Fujitaki JM, MacKenna DA, Wilker CE, Chi B, van Poelje PD, Linemeyer DL, Erion MD.

Br J Pharmacol. 2009 Feb;156(3):454-65. doi: 10.1111/j.1750-3639.2009.00038.x. Epub 2009 Jan 22.


Reduction of hepatic steatosis in rats and mice after treatment with a liver-targeted thyroid hormone receptor agonist.

Cable EE, Finn PD, Stebbins JW, Hou J, Ito BR, van Poelje PD, Linemeyer DL, Erion MD.

Hepatology. 2009 Feb;49(2):407-17. doi: 10.1002/hep.22572.


Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.

Boyer SH, Jiang H, Jacintho JD, Reddy MV, Li H, Li W, Godwin JL, Schulz WG, Cable EE, Hou J, Wu R, Fujitaki JM, Hecker SJ, Erion MD.

J Med Chem. 2008 Nov 27;51(22):7075-93. doi: 10.1021/jm800824d.


Preclinical pharmacokinetics of a HepDirect prodrug of a novel phosphonate-containing thyroid hormone receptor agonist.

Fujitaki JM, Cable EE, Ito BR, Zhang BH, Hou J, Yang C, Bullough DA, Ferrero JL, van Poelje PD, Linemeyer DL, Erion MD.

Drug Metab Dispos. 2008 Nov;36(11):2393-403. doi: 10.1124/dmd.108.021642. Epub 2008 Aug 14.


Discovery of phosphonic diamide prodrugs and their use for the oral delivery of a series of fructose 1,6-bisphosphatase inhibitors.

Dang Q, Kasibhatla SR, Jiang T, Fan K, Liu Y, Taplin F, Schulz W, Cashion DK, Reddy KR, van Poelje PD, Fujitaki JM, Potter SC, Erion MD.

J Med Chem. 2008 Jul 24;51(14):4331-9. doi: 10.1021/jm8001235. Epub 2008 Jun 21.


Prodrugs of phosphates and phosphonates.

Hecker SJ, Erion MD.

J Med Chem. 2008 Apr 24;51(8):2328-45. doi: 10.1021/jm701260b. Epub 2008 Feb 1. No abstract available.


Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B.

Reddy KR, Matelich MC, Ugarkar BG, Gómez-Galeno JE, DaRe J, Ollis K, Sun Z, Craigo W, Colby TJ, Fujitaki JM, Boyer SH, van Poelje PD, Erion MD.

J Med Chem. 2008 Feb 14;51(3):666-76. doi: 10.1021/jm7012216. Epub 2008 Jan 4.


Discovery of potent and specific fructose-1,6-bisphosphatase inhibitors and a series of orally-bioavailable phosphoramidase-sensitive prodrugs for the treatment of type 2 diabetes.

Dang Q, Kasibhatla SR, Reddy KR, Jiang T, Reddy MR, Potter SC, Fujitaki JM, van Poelje PD, Huang J, Lipscomb WN, Erion MD.

J Am Chem Soc. 2007 Dec 19;129(50):15491-502. Epub 2007 Nov 28.


Structure-guided design of AMP mimics that inhibit fructose-1,6-bisphosphatase with high affinity and specificity.

Erion MD, Dang Q, Reddy MR, Kasibhatla SR, Huang J, Lipscomb WN, van Poelje PD.

J Am Chem Soc. 2007 Dec 19;129(50):15480-90. Epub 2007 Nov 28.


Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.

Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, Zhang BH, Hou J, Boyer SH, van Poelje PD, Linemeyer DL.

Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. Epub 2007 Sep 18.


Discovery of fructose-1,6-bisphosphatase inhibitors for the treatment of type 2 diabetes.

van Poelje PD, Dang Q, Erion MD.

Curr Opin Drug Discov Devel. 2007 Jul;10(4):430-7. Review.


Liver-targeted prodrugs of 2'-C-methyladenosine for therapy of hepatitis C virus infection.

Hecker SJ, Reddy KR, van Poelje PD, Sun Z, Huang W, Varkhedkar V, Reddy MV, Fujitaki JM, Olsen DB, Koeplinger KA, Boyer SH, Linemeyer DL, MacCoss M, Erion MD.

J Med Chem. 2007 Aug 9;50(16):3891-6. Epub 2007 Jul 18.


Relative binding affinities of fructose-1,6-bisphosphatase inhibitors calculated using a quantum mechanics-based free energy perturbation method.

Reddy MR, Erion MD.

J Am Chem Soc. 2007 Aug 1;129(30):9296-7. Epub 2007 Jul 7. No abstract available.


Bis[(para-methoxy)benzyl] phosphonate prodrugs with improved stability and enhanced cell penetration.

Dang Q, Liu Y, Rydzewski RM, Brown BS, Robinson E, van Poelje PD, Colby TJ, Erion MD.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3412-6. Epub 2007 Apr 2.


Synthesis and characterization of a novel liver-targeted prodrug of cytosine-1-beta-D-arabinofuranoside monophosphate for the treatment of hepatocellular carcinoma.

Boyer SH, Sun Z, Jiang H, Esterbrook J, Gómez-Galeno JE, Craigo W, Reddy KR, Ugarkar BG, MacKenna DA, Erion MD.

J Med Chem. 2006 Dec 28;49(26):7711-20.


Inhibition of fructose 1,6-bisphosphatase reduces excessive endogenous glucose production and attenuates hyperglycemia in Zucker diabetic fatty rats.

van Poelje PD, Potter SC, Chandramouli VC, Landau BR, Dang Q, Erion MD.

Diabetes. 2006 Jun;55(6):1747-54.


HepDirect prodrugs for targeting nucleotide-based antiviral drugs to the liver.

Erion MD, Bullough DA, Lin CC, Hong Z.

Curr Opin Investig Drugs. 2006 Feb;7(2):109-17. Review.


Adenosine kinase inhibitors. 6. Synthesis, water solubility, and antinociceptive activity of 5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidines substituted at C4 with glycinamides and related compounds.

Bookser BC, Ugarkar BG, Matelich MC, Lemus RH, Allan M, Tsuchiya M, Nakane M, Nagahisa A, Wiesner JB, Erion MD.

J Med Chem. 2005 Dec 1;48(24):7808-20.


Liver targeting of hepatitis-B antiviral lamivudine using the HepDirect prodrug technology.

Reddy KR, Colby TJ, Fujitaki JM, van Poelje PD, Erion MD.

Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):375-81.


Adenosine kinase inhibitors. 5. Synthesis, enzyme inhibition, and analgesic activity of diaryl-erythro-furanosyltubercidin analogues.

Boyer SH, Ugarkar BG, Solbach J, Kopcho J, Matelich MC, Ollis K, Gomez-Galeno JE, Mendonca R, Tsuchiya M, Nagahisa A, Nakane M, Wiesner JB, Erion MD.

J Med Chem. 2005 Oct 6;48(20):6430-41.


The therapeutic potential of agents acting via purine receptors.

Appleman JR, Erion MD.

Expert Opin Investig Drugs. 1998 Feb;7(2):225-43.


MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes.

Erion MD, van Poelje PD, Dang Q, Kasibhatla SR, Potter SC, Reddy MR, Reddy KR, Jiang T, Lipscomb WN.

Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5. Epub 2005 May 23.


Remofovir mesylate: a prodrug of PMEA with improved liver-targeting and safety in rats and monkeys.

Lin CC, Yeh LT, Vitarella D, Hong Z, Erion MD.

Antivir Chem Chemother. 2004 Nov;15(6):307-17.


Liver-targeted drug delivery using HepDirect prodrugs.

Erion MD, van Poelje PD, Mackenna DA, Colby TJ, Montag AC, Fujitaki JM, Linemeyer DL, Bullough DA.

J Pharmacol Exp Ther. 2005 Feb;312(2):554-60. Epub 2004 Aug 31.


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