Trevor M Penning

Trevor M Penning

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Trevor M Penning

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Aldo-keto reductase 1C3-Assessment as a new target for the treatment of endometriosis.

Pharmacol Res 2020 Feb 20;152:104446. Epub 2019 Sep 20.

Center of Excellence in Environmental Toxicology & Department of Systems Pharmacology & Translational Therapeutics, University of Pennsylvania Perelman School of Medicine, 421 Curie Boulevard, PA 19104-6160, Philadelphia, USA.

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http://dx.doi.org/10.1016/j.phrs.2019.104446DOI Listing
February 2020

Intracrinology-revisited and prostate cancer.

J Steroid Biochem Mol Biol 2020 Feb 12;196:105499. Epub 2019 Oct 12.

Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania School Philadelphia, PA, United States.

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http://dx.doi.org/10.1016/j.jsbmb.2019.105499DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6954292PMC
February 2020

Induction of the Antioxidant Response by the Transcription Factor NRF2 Increases Bioactivation of the Mutagenic Air Pollutant 3-Nitrobenzanthrone in Human Lung Cells.

Chem Res Toxicol 2019 Dec 20;32(12):2538-2551. Epub 2019 Nov 20.

Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine , University of Pennsylvania , Philadelphia , Pennsylvania 19104 , United States.

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http://dx.doi.org/10.1021/acs.chemrestox.9b00399DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6934363PMC
December 2019

A 3-(4-nitronaphthen-1-yl) amino-benzoate analog as a bifunctional AKR1C3 inhibitor and AR antagonist: Head to head comparison with other advanced AKR1C3 targeted therapeutics.

J Steroid Biochem Mol Biol 2019 09 11;192:105283. Epub 2019 Jan 11.

Department of Systems Pharmacology and Translational Therapeutics and the Center for Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, 1315 BRBII/III, 421 Curie Boulevard, Philadelphia, PA 19104-6160, USA. Electronic address:

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http://dx.doi.org/10.1016/j.jsbmb.2019.01.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6625945PMC
September 2019

AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase): Roles in malignancy and endocrine disorders.

Authors:
Trevor M Penning

Mol Cell Endocrinol 2019 06 19;489:82-91. Epub 2018 Sep 19.

Department of Systems Pharmacology and Translational Therapeutics and Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, 1315 BRBII/III 421 Curie Blvd, Philadelphia, PA, 19104, USA. Electronic address:

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http://dx.doi.org/10.1016/j.mce.2018.07.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6422768PMC
June 2019

Biology and clinical relevance of Hydroxysteroid (17beta) dehydrogenase enzymes.

Mol Cell Endocrinol 2019 06 13;489:1-2. Epub 2019 Apr 13.

Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S03037207193010
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http://dx.doi.org/10.1016/j.mce.2019.04.008DOI Listing
June 2019

AKR1D1 regulates glucocorticoid availability and glucocorticoid receptor activation in human hepatoma cells.

J Steroid Biochem Mol Biol 2019 05 12;189:218-227. Epub 2019 Feb 12.

Oxford Centre for Diabetes, Endocrinology and Metabolism, NIHR Oxford Biomedical Research Centre, University of Oxford, Churchill Hospital, Oxford, OX3 7LE, UK. Electronic address:

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http://dx.doi.org/10.1016/j.jsbmb.2019.02.002DOI Listing
May 2019

Human and murine steroid 5β-reductases (AKR1D1 and AKR1D4): insights into the role of the catalytic glutamic acid.

Chem Biol Interact 2019 May 28;305:163-170. Epub 2019 Mar 28.

Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, 19104, USA; Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, 19104, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cbi.2019.03.025DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6500757PMC
May 2019

Structural and Functional Biology of Aldo-Keto Reductase Steroid-Transforming Enzymes.

Endocr Rev 2019 04;40(2):447-475

Division of Metabolism, Endocrinology, and Diabetes, Department of Internal Medicine and Department of Pharmacology, University of Michigan School of Medicine, Ann Arbor, Michigan.

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http://dx.doi.org/10.1210/er.2018-00089DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6405412PMC
April 2019

Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia.

J Med Chem 2019 04 25;62(7):3590-3616. Epub 2019 Mar 25.

Department of Pharmaceutical Sciences , Texas Tech University Health Sciences Center, School of Pharmacy , Amarillo , Texas 79106 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00090DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6528660PMC
April 2019

Dehydroepiandrosterone (DHEA)-SO Depot and Castration-Resistant Prostate Cancer.

Authors:
Trevor M Penning

Vitam Horm 2018 24;108:309-331. Epub 2018 Feb 24.

Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, United States. Electronic address:

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http://dx.doi.org/10.1016/bs.vh.2018.01.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6226251PMC
November 2018

Role of Human Aldo-Keto Reductases in the Metabolic Activation of the Carcinogenic Air Pollutant 3-Nitrobenzanthrone.

Chem Res Toxicol 2018 11 8;31(11):1277-1288. Epub 2018 Nov 8.

Biochemical Institute for Environmental Carcinogens, Prof. Dr. Gernot Grimmer-Foundation , Grosshansdorf 22927 , Germany.

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http://dx.doi.org/10.1021/acs.chemrestox.8b00250DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6319660PMC
November 2018

AKR1C3 Inhibitor KV-37 Exhibits Antineoplastic Effects and Potentiates Enzalutamide in Combination Therapy in Prostate Adenocarcinoma Cells.

Mol Cancer Ther 2018 09 11;17(9):1833-1845. Epub 2018 Jun 11.

Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, Texas.

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http://dx.doi.org/10.1158/1535-7163.MCT-17-1023DOI Listing
September 2018

Aldo-Keto Reductase (AKR) 1C3 inhibitors: a patent review.

Authors:
Trevor M Penning

Expert Opin Ther Pat 2017 Dec 19;27(12):1329-1340. Epub 2017 Sep 19.

a Center of Excellence in Environmental Toxicology & Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine , University of Pennsylvania , Philadelphia , PA , USA.

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http://dx.doi.org/10.1080/13543776.2017.1379503DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5724044PMC
December 2017

Potential Metabolic Activation of Representative Alkylated Polycyclic Aromatic Hydrocarbons 1-Methylphenanthrene and 9-Ethylphenanthrene Associated with the Deepwater Horizon Oil Spill in Human Hepatoma (HepG2) Cells.

Chem Res Toxicol 2017 12 27;30(12):2140-2150. Epub 2017 Oct 27.

Synthetic Organic Chemistry Core, Center in Environmental Toxicology, University of Texas Medical Branch at Galveston , Galveston, Texas 77555-1110, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.7b00232DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734992PMC
December 2017

On meta- and mega-analyses for gene-environment interactions.

Genet Epidemiol 2017 12 7;41(8):876-886. Epub 2017 Nov 7.

Department of Biostatistics, Epidemiology and Informatics, University of Pennsylvania, Philadelphia, Pennsylvania, United States of America.

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http://dx.doi.org/10.1002/gepi.22085DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5775907PMC
December 2017

Genotoxicity of -quinones: reactive oxygen species covalent modification.

Authors:
Trevor M Penning

Toxicol Res (Camb) 2017 6;6(6):740-754. Epub 2017 Sep 6.

Center of Excellence in Environmental Toxicology and Department of Systems Pharmacology & Translational Therapeutics, University of Pennsylvania, Philadelphia, PA 19104-6160, USA.

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http://xlink.rsc.org/?DOI=C7TX00223H
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http://dx.doi.org/10.1039/C7TX00223HDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5842949PMC
September 2017

Testicular vs adrenal sources of hydroxy-androgens in prostate cancer.

Endocr Relat Cancer 2017 08 29;24(8):393-404. Epub 2017 Jun 29.

Department of Systems Pharmacology & Translational TherapeuticsPerelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA

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http://dx.doi.org/10.1530/ERC-17-0107DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5593253PMC
August 2017

Potential Metabolic Activation of a Representative C4-Alkylated Polycyclic Aromatic Hydrocarbon Retene (1-Methyl-7-isopropyl-phenanthrene) Associated with the Deepwater Horizon Oil Spill in Human Hepatoma (HepG2) Cells.

Chem Res Toxicol 2017 04 22;30(4):1093-1101. Epub 2017 Mar 22.

Synthetic Organic Chemistry Core, Center in Environmental Toxicology, University of Texas Medical Branch at Galveston , Galveston, Texas 77555-1110, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.6b00457DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5593134PMC
April 2017

Simultaneous quantitation of nine hydroxy-androgens and their conjugates in human serum by stable isotope dilution liquid chromatography electrospray ionization tandem mass spectrometry.

J Steroid Biochem Mol Biol 2017 01 12;165(Pt B):342-355. Epub 2016 Aug 12.

Center for Excellence in Environmental Toxicology, Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, United States; Center for Cancer Pharmacology, Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, United States. Electronic address:

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http://dx.doi.org/10.1016/j.jsbmb.2016.08.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5146996PMC
January 2017

Aldo-Keto Reductase Regulation by the Nrf2 System: Implications for Stress Response, Chemotherapy Drug Resistance, and Carcinogenesis.

Authors:
Trevor M Penning

Chem Res Toxicol 2017 01 16;30(1):162-176. Epub 2016 Nov 16.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.6b00319DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5241174PMC
January 2017

Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.

J Med Chem 2016 08 12;59(16):7431-44. Epub 2016 Aug 12.

Department of Systems Pharmacology and Translational Therapeutics and the Center for Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania , 1315 BRBII/III, 421 Curie Boulevard, Philadelphia, Pennsylvania 19104-6160, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b00160DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5149398PMC
August 2016

Selective AKR1C3 Inhibitors Potentiate Chemotherapeutic Activity in Multiple Acute Myeloid Leukemia (AML) Cell Lines.

ACS Med Chem Lett 2016 Aug 22;7(8):774-9. Epub 2016 Jun 22.

Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, Texas 79106, United States; Center for Chemical Biology, Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, Texas 79409-1061, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00163DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4983729PMC
August 2016

Single-molecule enzymology of steroid transforming enzymes: Transient kinetic studies and what they tell us.

Authors:
Trevor M Penning

J Steroid Biochem Mol Biol 2016 07 24;161:5-12. Epub 2015 Oct 24.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, United States. Electronic address:

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http://dx.doi.org/10.1016/j.jsbmb.2015.10.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4842339PMC
July 2016

Potential Metabolic Activation of a Representative C2-Alkylated Polycyclic Aromatic Hydrocarbon 6-Ethylchrysene Associated with the Deepwater Horizon Oil Spill in Human Hepatoma (HepG2) Cells.

Chem Res Toxicol 2016 06 1;29(6):991-1002. Epub 2016 May 1.

Center of Excellence in Environmental Toxicology and ‡Center for Cancer Pharmacology, Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6160, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.6b00036DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4916485PMC
June 2016

Current advances in intratumoral androgen metabolism in castration-resistant prostate cancer.

Curr Opin Endocrinol Diabetes Obes 2016 06;23(3):264-70

Department of Systems Pharmacology and Translational Therapeutics, Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA.

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http://dx.doi.org/10.1097/MED.0000000000000253DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4893781PMC
June 2016

Unconventional Gas and Oil Drilling Is Associated with Increased Hospital Utilization Rates.

PLoS One 2015 15;10(7):e0131093. Epub 2015 Jul 15.

Center of Excellence in Environmental Toxicology (CEET), Airways Biology Initiative, University of Pennsylvania Perelman School of Medicine, Philadelphia, Pennsylvania, United States of America.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0131093PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4503720PMC
April 2016

Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates degenerative disease.

Free Radic Biol Med 2015 Nov 27;88(Pt B):108-146. Epub 2015 Jun 27.

Jacqui Wood Cancer Centre, Division of Cancer Research, Ninewells Hospital and Medical School, University of Dundee, Dundee DD1 9SY, Scotland, UK. Electronic address:

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http://dx.doi.org/10.1016/j.freeradbiomed.2015.06.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4659505PMC
November 2015

Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities.

Bioorg Med Chem Lett 2015 Oct 8;25(20):4437-40. Epub 2015 Sep 8.

Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, D-52056 Aachen, Germany.

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http://dx.doi.org/10.1016/j.bmcl.2015.09.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4599580PMC
October 2015

Metabolism of an Alkylated Polycyclic Aromatic Hydrocarbon 5-Methylchrysene in Human Hepatoma (HepG2) Cells.

Chem Res Toxicol 2015 Oct 5;28(10):2045-58. Epub 2015 Oct 5.

Synthetic Organic Chemistry Core, Center in Environmental Toxicology, University of Texas Medical Branch at Galveston , Galveston, Texas 77555-1110, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.5b00256DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4709222PMC
October 2015

In-Depth Dissection of the P133R Mutation in Steroid 5β-Reductase (AKR1D1): A Molecular Basis of Bile Acid Deficiency.

Biochemistry 2015 Oct 6;54(41):6343-51. Epub 2015 Oct 6.

Center of Excellence in Environmental Toxicology and Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine University of Pennsylvania , Philadelphia, Philadelphia, United States.

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http://dx.doi.org/10.1021/acs.biochem.5b00816DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4696769PMC
October 2015

Mechanisms of drug resistance that target the androgen axis in castration resistant prostate cancer (CRPC).

Authors:
Trevor M Penning

J Steroid Biochem Mol Biol 2015 Sep 29;153:105-13. Epub 2015 May 29.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, USA. Electronic address:

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http://dx.doi.org/10.1016/j.jsbmb.2015.05.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4568163PMC
September 2015

Promiscuity and diversity in 3-ketosteroid reductases.

J Steroid Biochem Mol Biol 2015 Jul 10;151:93-101. Epub 2014 Dec 10.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, USA.

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https://linkinghub.elsevier.com/retrieve/pii/S09600760140030
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http://dx.doi.org/10.1016/j.jsbmb.2014.12.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4458445PMC
July 2015

The aldo-keto reductases (AKRs): Overview.

Authors:
Trevor M Penning

Chem Biol Interact 2015 Jun 7;234:236-46. Epub 2014 Oct 7.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cbi.2014.09.024DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4388799PMC
June 2015

The rate-determining steps of aldo-keto reductases (AKRs), a study on human steroid 5β-reductase (AKR1D1).

Chem Biol Interact 2015 Jun 11;234:360-5. Epub 2014 Dec 11.

Center of Excellence in Environmental Toxicology and Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cbi.2014.12.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4414691PMC
June 2015

The DHEA-sulfate depot following P450c17 inhibition supports the case for AKR1C3 inhibition in high risk localized and advanced castration resistant prostate cancer.

Chem Biol Interact 2015 Jun 13;234:332-8. Epub 2014 Dec 13.

Centers for Cancer Pharmacology and Excellence of Environmental Toxicology (CEET), Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00092797140039
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http://dx.doi.org/10.1016/j.cbi.2014.12.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4414681PMC
June 2015

Screening baccharin analogs as selective inhibitors against type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).

Chem Biol Interact 2015 Jun 31;234:339-48. Epub 2014 Dec 31.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology & Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, United States. Electronic address:

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http://dx.doi.org/10.1016/j.cbi.2014.12.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4414711PMC
June 2015

Editorial. 17th International Workshop on the Enzymology and Molecular Biology of Carbonyl Metabolism.

Authors:
Trevor M Penning

Chem Biol Interact 2015 Jun;234:1-3

University of Pennsylvania, Dept. of Pharmacol, Sch of Med, 3620 Hamilton Walk, Philadelphia, PA 19104, United States. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00092797150016
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http://dx.doi.org/10.1016/j.cbi.2015.04.014DOI Listing
June 2015

Electron transfer by human wild-type and A287P mutant P450 oxidoreductase assessed by transient kinetics: functional basis of P450 oxidoreductase deficiency.

Biochem J 2015 May;468(1):25-31

‡Department of Pediatrics, University of California, San Francisco, San Francisco, California, CA 94143, U.S.A.

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http://dx.doi.org/10.1042/BJ20141410DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4692368PMC
May 2015

Environmental health research recommendations from the Inter-Environmental Health Sciences Core Center Working Group on unconventional natural gas drilling operations.

Environ Health Perspect 2014 Nov 18;122(11):1155-9. Epub 2014 Jul 18.

Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA.

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http://ehp.niehs.nih.gov/wp-content/uploads/advpub/2014/7/eh
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http://ehp.niehs.nih.gov/1408207
Publisher Site
http://dx.doi.org/10.1289/ehp.1408207DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4216169PMC
November 2014

Human aldo-keto reductases and the metabolic activation of polycyclic aromatic hydrocarbons.

Authors:
Trevor M Penning

Chem Res Toxicol 2014 Nov 16;27(11):1901-17. Epub 2014 Oct 16.

Center of Excellence in Environmental Toxicology, Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6061, United States.

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http://pubs.acs.org/doi/10.1021/tx500298n
Publisher Site
http://dx.doi.org/10.1021/tx500298nDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4237494PMC
November 2014

Intense androgen-deprivation therapy with abiraterone acetate plus leuprolide acetate in patients with localized high-risk prostate cancer: results of a randomized phase II neoadjuvant study.

J Clin Oncol 2014 Nov 13;32(33):3705-15. Epub 2014 Oct 13.

Mary-Ellen Taplin, Massimo Loda, Rosina T. Lis, Wanling Xie, Zhenyang Jiang, and Philip W. Kantoff, Dana-Farber Cancer Institute, Harvard Medical School; Glenn J. Bubley, Huihui Ye, and Steven P. Balk, Beth Israel Deaconess Medical Center; Jerome P. Richie, Massimo Loda, and Rosina T. Lis, Brigham and Women's Hospital, Boston, MA; Bruce Montgomery, Bruce L. Dalkin, Lawrence D. True, and Alvin M. Matsumoto, University of Washington; Brett T. Marck and Alvin M. Matsumoto, Geriatric Research, Education and Clinical Center, Veterans' Affairs Puget Sound Health Care System; Elahe A. Mostaghel and Peter S. Nelson, Fred Hutchinson Cancer Research Center, Seattle, WA; Christopher J. Logothetis, John W. Davis, and Patricia Troncoso, University of Texas MD Anderson Cancer Center, Houston, TX; Martin G. Sanda, Emory University School of Medicine, Atlanta, GA; Massimo Loda, King's College London, London, United Kingdom; Trevor M. Penning and Daniel Tamae, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA; and Christopher M. Haqq, NamPhuong Tran, Weimin Peng, Thian Kheoh, and Arturo Molina, Janssen Research and Development, Los Angeles, CA.

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http://dx.doi.org/10.1200/JCO.2013.53.4578DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4226804PMC
November 2014

Androgen biosynthesis in castration-resistant prostate cancer.

Authors:
Trevor M Penning

Endocr Relat Cancer 2014 Aug 14;21(4):T67-78. Epub 2014 May 14.

Perelman School of MedicineCenter of Excellence in Environmental Toxicology, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6084, USA

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http://dx.doi.org/10.1530/ERC-14-0109DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4167409PMC
August 2014

Rate of steroid double-bond reduction catalysed by the human steroid 5β-reductase (AKR1D1) is sensitive to steroid structure: implications for steroid metabolism and bile acid synthesis.

Biochem J 2014 Aug;462(1):163-71

*Center of Excellence in Environmental Toxicology and Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, U.S.A.

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http://dx.doi.org/10.1042/BJ20140220DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4163838PMC
August 2014

Quantitative detection of 8-Oxo-7,8-dihydro-2'-deoxyguanosine using chemical tagging and qPCR.

Chem Res Toxicol 2014 Jul 16;27(7):1227-35. Epub 2014 Jun 16.

Department of Chemistry, Johns Hopkins University , 3400 N. Charles Street, Baltimore, Maryland 21218, United States.

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http://dx.doi.org/10.1021/tx500120pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106692PMC
July 2014

5β-Reduced steroids and human Δ(4)-3-ketosteroid 5β-reductase (AKR1D1).

Steroids 2014 May 8;83:17-26. Epub 2014 Feb 8.

Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, United States; Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6160, United States. Electronic address:

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May 2014

Metabolism of a representative oxygenated polycyclic aromatic hydrocarbon (PAH) phenanthrene-9,10-quinone in human hepatoma (HepG2) cells.

Chem Res Toxicol 2014 May 31;27(5):852-63. Epub 2014 Mar 31.

Center of Excellence in Environmental Toxicology and ‡Center for Cancer Pharmacology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6160, United States.

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May 2014

Role of aldo-keto reductase family 1 (AKR1) enzymes in human steroid metabolism.

Steroids 2014 Jan 1;79:49-63. Epub 2013 Nov 1.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA. Electronic address:

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3870468PMC
January 2014

Interception of benzo[a]pyrene-7,8-dione by UDP glucuronosyltransferases (UGTs) in human lung cells.

Chem Res Toxicol 2013 Oct 3;26(10):1570-8. Epub 2013 Oct 3.

Center of Excellence in Environmental Toxicology and ‡Center for Cancer Pharmacology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6160, United States.

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October 2013

AKR1C3 as a target in castrate resistant prostate cancer.

J Steroid Biochem Mol Biol 2013 Sep 6;137:136-49. Epub 2013 Jun 6.

Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6061, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3805777PMC
September 2013

Identification of stable benzo[a]pyrene-7,8-dione-DNA adducts in human lung cells.

Chem Res Toxicol 2013 May 26;26(5):685-92. Epub 2013 Apr 26.

Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6160, United States.

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May 2013

Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.

J Med Chem 2013 Mar 13;56(6):2429-46. Epub 2013 Mar 13.

Department of Biochemistry, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine , Nashville, Tennessee 37232-0146, USA.

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March 2013

Alternative splicing in the aldo-keto reductase superfamily: implications for protein nomenclature.

Chem Biol Interact 2013 Feb 5;202(1-3):153-8. Epub 2013 Jan 5.

Diabetes and Obesity Center, School of Medicine, University of Louisville, Louisville, KY 40202, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3758225PMC
February 2013

The Role of Human Aldo-Keto Reductases in the Metabolic Activation and Detoxication of Polycyclic Aromatic Hydrocarbons: Interconversion of PAH Catechols and PAH o-Quinones.

Front Pharmacol 2012 16;3:193. Epub 2012 Nov 16.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania Philadelphia, PA, USA.

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November 2012

Aldo-keto reductase family 1 member C3 (AKR1C3) is expressed in adenocarcinoma and squamous cell carcinoma but not small cell carcinoma.

Int J Clin Exp Pathol 2012 26;5(4):278-89. Epub 2012 Apr 26.

College of Medicine, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA.

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October 2012

p53 Mutagenesis by benzo[a]pyrene derived radical cations.

Chem Res Toxicol 2012 Oct 9;25(10):2117-26. Epub 2012 Aug 9.

Department of Pharmacology and Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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October 2012

Selective inhibitors of aldo-keto reductases AKR1C1 and AKR1C3 discovered by virtual screening of a fragment library.

J Med Chem 2012 Sep 27;55(17):7417-24. Epub 2012 Aug 27.

Institute of Biochemistry, Faculty of Medicine, University of Ljubljana , Vrazov trg 2, 1000 Ljubljana, Slovenia.

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September 2012

Synthesis of -labelled oxidized metabolites of the carcinogenic polycyclic aromatic hydrocarbon benzo[]pyrene.

Tetrahedron 2012 Sep;68(35)

The Ben May Department for Cancer Research, The University of Chicago, Chicago, IL 60637, United States.

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September 2012

Detoxication of benzo[a]pyrene-7,8-dione by sulfotransferases (SULTs) in human lung cells.

J Biol Chem 2012 Aug 9;287(35):29909-20. Epub 2012 Jul 9.

Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104-6084, USA.

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August 2012

Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5α-reductase inhibitor finasteride.

J Steroid Biochem Mol Biol 2012 May 12;130(1-2):7-15. Epub 2012 Jan 12.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, United States.

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May 2012

Conversion of human steroid 5β-reductase (AKR1D1) into 3β-hydroxysteroid dehydrogenase by single point mutation E120H: example of perfect enzyme engineering.

J Biol Chem 2012 May 20;287(20):16609-22. Epub 2012 Mar 20.

Department of Pharmacology and Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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May 2012

Metabolism and distribution of benzo[a]pyrene-7,8-dione (B[a]P-7,8-dione) in human lung cells by liquid chromatography tandem mass spectrometry: detection of an adenine B[a]P-7,8-dione adduct.

Chem Res Toxicol 2012 May 1;25(5):993-1003. Epub 2012 May 1.

Center of Excellence in Environmental Toxicology and Center for Cancer Pharmacology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, United States.

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May 2012

Metabolism of the synthetic progestogen norethynodrel by human ketosteroid reductases of the aldo-keto reductase superfamily.

J Steroid Biochem Mol Biol 2012 Apr 28;129(3-5):139-44. Epub 2011 Dec 28.

Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA.

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April 2012

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.

J Med Chem 2012 Mar 15;55(5):2311-23. Epub 2012 Feb 15.

Department of Pharmacology and Center of Excellence in Environmental Toxicology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6084, USA.

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March 2012

Multidrug resistance protein (MRP) 4 attenuates benzo[a]pyrene-mediated DNA-adduct formation in human bronchoalveolar H358 cells.

Toxicol Lett 2012 Feb 30;209(1):58-66. Epub 2011 Nov 30.

Center for Cancer Pharmacology, 421 Curie Boulevard, BRB II/III Room 841, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.

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http://dx.doi.org/10.1016/j.toxlet.2011.11.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3256298PMC
February 2012

Specificity of human aldo-keto reductases, NAD(P)H:quinone oxidoreductase, and carbonyl reductases to redox-cycle polycyclic aromatic hydrocarbon diones and 4-hydroxyequilenin-o-quinone.

Chem Res Toxicol 2011 Dec 29;24(12):2153-66. Epub 2011 Sep 29.

Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3251162PMC
December 2011

Quantitation of benzo[a]pyrene metabolic profiles in human bronchoalveolar (H358) cells by stable isotope dilution liquid chromatography-atmospheric pressure chemical ionization mass spectrometry.

Chem Res Toxicol 2011 Nov 7;24(11):1905-14. Epub 2011 Nov 7.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6084, USA.

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November 2011

Stereospecific reduction of 5β-reduced steroids by human ketosteroid reductases of the AKR (aldo-keto reductase) superfamily: role of AKR1C1-AKR1C4 in the metabolism of testosterone and progesterone via the 5β-reductase pathway.

Biochem J 2011 Jul;437(1):53-61

Department of Pharmacology and Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104-6084, USA.

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July 2011

Detoxication of structurally diverse polycyclic aromatic hydrocarbon (PAH) o-quinones by human recombinant catechol-O-methyltransferase (COMT) via O-methylation of PAH catechols.

J Biol Chem 2011 Jul 27;286(29):25644-54. Epub 2011 May 27.

Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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http://www.jbc.org/lookup/doi/10.1074/jbc.M111.240739
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3138279PMC
July 2011

Inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3): overview and structural insights.

J Steroid Biochem Mol Biol 2011 May 16;125(1-2):95-104. Epub 2010 Nov 16.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, University of Pennsylvania School of Medicine, 130C John Morgan Bldg, 3620 Hamilton Walk, Philadelphia, PA 19104-6084, United States.

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May 2011

The effect of disease associated point mutations on 5β-reductase (AKR1D1) enzyme function.

Chem Biol Interact 2011 May 24;191(1-3):250-4. Epub 2010 Dec 24.

University of Pennsylvania, School of Medicine, Department of Pharmacology, Philadelphia, PA 19104-6084, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3101292PMC
May 2011

Human hydroxysteroid dehydrogenases and pre-receptor regulation: insights into inhibitor design and evaluation.

Authors:
Trevor M Penning

J Steroid Biochem Mol Biol 2011 May 25;125(1-2):46-56. Epub 2011 Jan 25.

Center of Excellence in Environmental Toxicology, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104-6084, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3104102PMC
May 2011

Substrate specificity and inhibitor analyses of human steroid 5β-reductase (AKR1D1).

Steroids 2011 Apr 19;76(5):484-90. Epub 2011 Jan 19.

Department of Pharmacology, University of Pennsylvania, Philadelphia, PA 19104-6084, USA.

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http://dx.doi.org/10.1016/j.steroids.2011.01.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3056882PMC
April 2011

Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).

Bioorg Med Chem Lett 2011 Mar 7;21(5):1464-8. Epub 2011 Jan 7.

Department of Pharmacology, University of Pennsylvania, School of Medicine, Philadelphia, PA 19104-6084, USA.

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http://dx.doi.org/10.1016/j.bmcl.2011.01.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3057412PMC
March 2011

Regulation of benzo[a]pyrene-mediated DNA- and glutathione-adduct formation by 2,3,7,8-tetrachlorodibenzo-p-dioxin in human lung cells.

Chem Res Toxicol 2011 Jan 28;24(1):89-98. Epub 2010 Oct 28.

Center for Cancer Pharmacology, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6610, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3021323PMC
January 2011

Liquid chromatography-mass spectrometry (LC-MS) of steroid hormone metabolites and its applications.

J Steroid Biochem Mol Biol 2010 Aug 18;121(3-5):546-55. Epub 2010 Jan 18.

Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104-6084, USA.

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http://dx.doi.org/10.1016/j.jsbmb.2010.01.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2894289PMC
August 2010

Characterization of disease-related 5beta-reductase (AKR1D1) mutations reveals their potential to cause bile acid deficiency.

J Biol Chem 2010 Aug 3;285(32):24529-37. Epub 2010 Jun 3.

Department of Pharmacology, University of PennsylvaniaSchool of Medicine, Center of Excellence in Environmental Toxicology, Philadelphia, Pennsylvania 19104-6084, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2915689PMC
August 2010

Suppressed expression of type 2 3alpha/type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3) in endometrial hyperplasia and carcinoma.

Int J Clin Exp Pathol 2010 Jul 5;3(6):608-17. Epub 2010 Jul 5.

Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA.

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July 2010

New frontiers in androgen biosynthesis and metabolism.

Authors:
Trevor M Penning

Curr Opin Endocrinol Diabetes Obes 2010 Jun;17(3):233-9

University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104-6084, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3206266PMC
June 2010

Partners in crime: deregulation of AR activity and androgen synthesis in prostate cancer.

Trends Endocrinol Metab 2010 May 6;21(5):315-24. Epub 2010 Feb 6.

Kimmel Cancer Center, Department of Cancer Biology and Department of Urology, Thomas Jefferson University, Philadelphia, PA 19107, USA.

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http://dx.doi.org/10.1016/j.tem.2010.01.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2862880PMC
May 2010

Regiospecific oxidation of polycyclic aromatic phenols to quinones by hypervalent iodine reagents.

Tetrahedron 2010 Mar;66(12):2111-2118

Ben May Department for Cancer Research, Gordon Center for Integrative Sciences, University of Chicago, 929 East 57th Street, Room W308, Chicago, IL 60637, USA.

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http://dx.doi.org/10.1016/j.tet.2009.12.022DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3762479PMC
March 2010

Aldo-keto reductase 1C3 expression in MCF-7 cells reveals roles in steroid hormone and prostaglandin metabolism that may explain its over-expression in breast cancer.

J Steroid Biochem Mol Biol 2010 Feb 28;118(3):177-87. Epub 2009 Dec 28.

Centers of Excellence in Environmental Toxicology and Cancer Pharmacology, Department of Pharmacology, University of Pennsylvania School of Medicine, 130C John Morgan Bldg, 3620 Hamilton Walk, Philadelphia, PA 19104-6084, United States.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2819162PMC
February 2010

Expression of AKR1C3 in renal cell carcinoma, papillary urothelial carcinoma, and Wilms' tumor.

Int J Clin Exp Pathol 2009 Nov 15;3(2):147-55. Epub 2009 Nov 15.

Department of Urology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA.

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November 2009