Mark D Erion

Mark D Erion

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Mark D Erion

Mark D Erion

Publications by authors named "Mark D Erion"

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

J Pharmacol Exp Ther 2017 10 19;363(1):80-91. Epub 2017 Jul 19.

Merck & Company, Inc., Kenilworth, New Jersey (N.A.D., S.P.W., Y.C., H.Z., D.G.M., T.P.R., D.G.J., D.M.E., D.E.K., S.P.F.), and Department of Pharmaceutical Sciences, College of Pharmacy, Northeast Ohio Medical University, Rootstown, Ohio (T.K.)

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http://dx.doi.org/10.1124/jpet.117.241091DOI Listing
October 2017

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

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

RR Labs, Inc., 8013 Los Sabalos Street, San Diego, CA 92126, USA.

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http://dx.doi.org/10.2174/13816128113199990604DOI Listing
March 2015

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

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

Rational Labs Pvt Ltd, Plot # 177, IDA Mallapur, Hyderabad-500 076, India.

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http://dx.doi.org/10.2174/1381612811319260002DOI Listing
February 2014

Use of a QM/MM-based FEP method to evaluate the anomalous hydration behavior of simple alkyl amines and amides: application to the design of FBPase inhibitors for the treatment of type-2 diabetes.

J Am Chem Soc 2011 Jun 5;133(21):8059-61. Epub 2011 May 5.

Computer Modelling, Simulations and Design, University of Hyderabad, Hyderabad, India 500 034.

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http://dx.doi.org/10.1021/ja201637qDOI Listing
June 2011

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

Handb Exp Pharmacol 2011 (203):279-301

Pfizer Inc., Eastern Point Road, Groton, CT 06340, USA.

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http://dx.doi.org/10.1007/978-3-642-17214-4_12DOI Listing
May 2011

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

J Comput Aided Mol Des 2009 Dec 17;23(12):837-43. Epub 2009 Sep 17.

Metabasis Therapeutics, Inc., La Jolla, CA 92037, USA.

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http://link.springer.com/10.1007/s10822-009-9300-5
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http://dx.doi.org/10.1007/s10822-009-9300-5DOI Listing
December 2009

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

Cancer Chemother Pharmacol 2009 Oct 13;64(5):981-91. Epub 2009 Mar 13.

Departments of Biological Sciences and Medicinal Chemistry, Metabasis Therapeutics Inc, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1007/s00280-009-0953-5DOI Listing
October 2009

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

Nucleosides Nucleotides Nucleic Acids 2009 Oct;28(10):969-86

Metabasis Therapeutics, Inc., La Jolla, California, USA.

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http://dx.doi.org/10.1080/15257770903307151DOI Listing
October 2009

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

J Med Chem 2009 May;52(9):2880-98

Department of Medicinal Chemistry, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/jm900078fDOI Listing
May 2009

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

Drug Metab Dispos 2008 Nov 14;36(11):2393-403. Epub 2008 Aug 14.

Department of Biological Sciences, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Rd., La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1124/dmd.108.021642DOI Listing
November 2008

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

J Med Chem 2008 Nov;51(22):7075-93

Departments of Medicinal Chemistry and Biosciences, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/jm800824dDOI Listing
November 2008

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

J Med Chem 2008 Jul 21;51(14):4331-9. Epub 2008 Jun 21.

Department of Medicinal Chemistry, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/jm8001235DOI Listing
July 2008

Prodrugs of phosphates and phosphonates.

J Med Chem 2008 Apr 1;51(8):2328-45. Epub 2008 Feb 1.

Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/jm701260bDOI Listing
April 2008

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

J Med Chem 2008 Feb 4;51(3):666-76. Epub 2008 Jan 4.

Department of Chemistry and Biochemistry, Metabasis Therapeutics Inc, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1021/jm7012216DOI Listing
February 2008

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

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

Department of Medicinal Chemistry, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/ja074869uDOI Listing
December 2007

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

J Am Chem Soc 2007 Aug 7;129(30):9296-7. Epub 2007 Jul 7.

Metabasis Therapeutics Inc, La Jolla, CA 92037, USA.

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http://pubs.acs.org/doi/abs/10.1021/ja072905j
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http://dx.doi.org/10.1021/ja072905jDOI Listing
August 2007

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

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

Departments of Biochemistry and Medicinal Chemistry, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1021/jm0701021DOI Listing
August 2007

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

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

Department of Biological Sciences, Metabasis Therapeutics Inc, 11119 North Torrey Pines Road, La Jolla, CA 92037, USA.

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July 2007

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

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

Department of Chemistry, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1016/j.bmcl.2007.03.089DOI Listing
June 2007

Ab initio quantum mechanics-based free energy perturbation method for calculating relative solvation free energies.

J Comput Chem 2007 Jan;28(2):491-4

Metabasis Therapeutics, 11119 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1002/jcc.20510DOI Listing
January 2007

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

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

Departments of Medicinal Chemistry and Biosciences, Metabasis Therapeutics, Inc., 11119 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1021/jm0607449DOI Listing
December 2006

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

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

Department of Biochemistry, Metabasis Therapeutics, 11119 North Torrey Pines Rd., La Jolla, CA 92037, USA.

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http://dx.doi.org/10.2337/db05-1443DOI Listing
June 2006

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

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

Metabasis Therapeutics Inc, La Jolla, CA 92037, USA.

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February 2006

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

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

Department of Chemistry, Metabasis Therapeutics, Inc., 9390 Towne Centre Drive, Building 300, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1081/ncn-200059781DOI Listing
December 2005

Computer-aided drug design strategies used in the discovery of fructose 1, 6-bisphosphatase inhibitors.

Curr Pharm Des 2005 ;11(3):283-94

Metabasis Therapeutics, Inc, 9390 Towne Centre Drive, San Diego, CA 92121, USA. E-mail:

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http://dx.doi.org/10.2174/1381612053382160DOI Listing
October 2005

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

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

Department of Biochemistry, Metabasis Therapeutics, Inc., 9390 Towne Centre Drive, Building 300, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1073/pnas.0502983102DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1138262PMC
May 2005

Liver-targeted drug delivery using HepDirect prodrugs.

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

Research and Development, Metabasis Therapeutics, Inc., 9390 Towne Centre Drive, Building 300, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1124/jpet.104.075903DOI Listing
February 2005

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

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

Valeant Pharmaceuticals International, Costa Mesa, Calif., USA.

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http://dx.doi.org/10.1177/095632020401500603DOI Listing
November 2004

Development of a quantum mechanics-based free-energy perturbation method: use in the calculation of relative solvation free energies.

J Am Chem Soc 2004 May;126(20):6224-5

Metabasis Therapeutics, Inc., 9390 Towne Centre Drive, Building 300, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/ja049281rDOI Listing
May 2004

Adenosine kinase inhibitors. 3. Synthesis, SAR, and antiinflammatory activity of a series of l-lyxofuranosyl nucleosides.

J Med Chem 2003 Oct;46(22):4750-60

Metabasis Therapeutics, Inc., 9390 Towne Centre Drive, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/jm030230zDOI Listing
October 2003

Modulation of cardiac remodeling by adenosine: in vitro and in vivo effects.

Mol Cell Biochem 2003 Sep;251(1-2):17-26

Department of Medicine, University of California, San Diego 92103-8412, USA.

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September 2003