Selected publications

Table of contents:

2016

  • Over B, Matsson P, Tyrchan C, Artursson P, Doak BC, Foley MA, Hilgendorf C, Johnston SE, Lee MD 4th, Lewis RJ, McCarren P, Muncipinto G, Norinder U, Perry MW, Duvall JR, Kihlberg J Structural and conformational determinants of macrocycle cell permeability. Nat Chem Biol. 2016 Oct 17. doi: 10.1038/nchembio.2203. [Epub ahead of print]"

  • Diwakarla S, Nylander E, Grönbladh A, Vanga SR, Khan YS, Gutiérrez-de-Terán H, Sävmarker J, Ng L, Pham V, Lundbäck T, Jenmalm-Jensen A, Svensson R, Artursson P, Zelleroth S, Engen K, Rosenström U, Larhed M, Åqvist J, Chai SY, Hallberg M Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures ACS Chem Neurosci. 2016 Aug 8. [Epubahead of print]

  • Alskär LC, Porter CJ, Bergström CA. Tools for Early Prediction of Drug Loading in Lipid-Based Formulations Mol Pharm. 2016 Jan 4;13(1):251-61.

  • Jacek R. Wisniewski , Christine Wegler, Per Artursson Subcellular fractionation of human liver reveals limits in global proteomic quantification from isolated fractions Analytical Biochemistry 509 (2016) 82-88

  • Matsson P, Lundquist P, Artursson P. The Need for Speed-Kinetic Limits of Drug Transporters Trends Pharmacol Sci. 2016 Apr;37(4):243-5

  • Pellegrini P, Dyczynski M, Sbrana FV, Karlgren M, Buoncervello M, Hägg-Olofsson M, Ma R, Hartman J, Bajalica-Lagercrantz S, Grander D, Kharaziha P, De Milito A. Tumor acidosis enhances cytotoxic effects and autophagy inhibition by salinomycin on cancer cell lines and cancer stem cells Oncotarget. 2016 May 27. doi: 10.18632/oncotarget.9601. [Epub ahead of print]

  • Almqvist H, Axelsson H, Jafari R, Dan C, Mateus A, Haraldsson M, Larsson A, Martinez Molina D, Artursson P, Lundbäck T, Nordlund P. CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil Nat Commun. 2016 Mar 24;7:11040. doi: 10.1038/ncomms11040.

  • Good JA, Silver J, Núñez-Otero C, Bahnan W, Krishnan KS, Salin O, Engström P,Svensson R, Artursson P, Gylfe Å, Bergström S, Almqvist F Thiazolino 2-PyridoneAmide Inhibitors of Chlamydia trachomatis Infectivity J Med Chem. 2016 Mar 10;59(5):2094-108

  • Anna Vildhede, André Mateus, Elin K. Khan, Yurong Lai, Maria Karlgren, Per Artursson, and Maria C. Kjellsson Mechanistic Modeling of Pitavastatin Disposition in Sandwich-Cultured Human Hepatocytes: A Proteomics-Informed Bottom-Up Approach Drug Metab Dispos 44:505–516, April 2016

  • Wisniewski JR, Vildhede A, Norén A, Artursson P In-depth quantitative analysis and comparison of the human hepatocyte and hepatoma cell line HepG2 proteomes J Proteomics. 2016 Mar 16;136:234-47

  • Sabin Llona-Minguez, Andreas Hö glund, Sylvain A. Jacques, Lars Johansson, JoséManuel Calderon-Montan ́ , Magnus Claesson,∞ Olga Loseva, Nicholas C. K. Valerie, Thomas Lundback, Javier Piedrafita, Giovanni Maga,Emmanuele Crespan,Laurent Meijer, Estefanía Burgos Moron, ́ Pawel Baranczewski, Ann-Louise Hagbjö rk, Richard Svensson,Elisee Wiita,Ingrid Almlöf, Torkild Visnes, Fredrik Jeppsson, Kristmundur Sigmundsson, Annika Jenmalm Jensen,Per Artursson, Ann-Sofie Jemth, Pal Stenmark, ̊ Ulrika Warpman Berglund, Martin Scobie, and Thomas Helleday Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1 J Med Chem

  • Simoff Ivailo, Karlgren Maria, Backlund Maria, Lindström Anne-Christine, Gaugaz Fabienne Z., Matsson Pär, Artursson Per Complete Knockout of Endogenous Mdr1 (Abcb1) in MDCK cells by CRISPR-Cas9 J Pharm Sci. 2016 Feb;105(2):1017-2

  • Ölander M, Wiśniewski JR, Matsson P, Lundquist P, Artursson P. The proteome of filter-grown Caco-2 cells with a focus on proteins involved in drug disposition. J Pharm Sci. 2016 Feb;105(2):817-27.

2015

  • Caraballo R, Larsson M, Nilsson SK, Ericsson M, Qian W, Nguyen Tran NP, Kindahl T, Svensson R, Saar V, Artursson P, Olivecrona G, Enquist PA, Elofsson M. Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.Eur J Med Chem 2015 Oct 20;103:191-209

  • Gordon LJ, Allen M, Artursson P, Hann MM, Leavens BJ, Mateus A, Readshaw S, Valko K, Wayne GJ, West A. Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability J Biomol Screen. 2016 Feb;21(2):156-64

  • Matsson P and Bergström CA Computational modeling to predict the functions and impact of drug transporters In Silico Pharmacology (2015) 3:8

  • Vildhede A, Wiśniewski JR, Norén A, Karlgren M, Artursson P Comparative Proteomic Analysis of Human Liver Tissue and Isolated Hepatocytes with a Focus on Proteins Determining Drug Exposure J Proteome Res. 2015 Aug 7;14(8):3305-14

  • Matsson P, Fenu LA, Lundquist P, Wiśniewski JR, Kansy M, Artursson P Quantifying the impact of transporters on cellular drug permeability Trends Pharmacol Sci. 2015 May;36(5):255-62

  • Artursson P, Knight SD.Structural biology. Breaking the intestinal barrier to deliver drugs. Science. 2015 Feb 13;347(6223):716-7

  • Borhade SR, Svensson R, Brandt P, Artursson P, Arvidsson PI, Sandström A. Preclinical characterization of acyl sulfonimidamides: potential carboxylic acid bioisosteres with tunable properties Chem Med Chem. 2015 Mar;10(3):455-60

2014

  • Fransson R, Nordvall G, Bylund J, Carlsson-Jonsson A, Kratz JM, Svensson R, Artursson P, Hallberg M, Sandström A. Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues ACS Med Chem Lett. 2014 Oct 29;5(12):1272-7

  • Lampa, Anna;Alogheli, Hiba; Ehrenberg, Angelica; Åkerblom, Eva; Svensson, Richard; Artursson, Per; Danielson, U. Helena; Karlén, Anders; Sandström, Anja Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles Bioorganic & Medicinal Chemistry

  • Anna Vildhede, Maria Karlgren, Elin K. Svedberg, Jacek R. Wisniewski, Yurong Lai, Agneta Norén, and Per Artursson Hepatic Uptake of Atorvastatin: Influence of Variability in Transporter Expression on Uptake Clearance and Drug-Drug Interactionss Drug Metab Dispos 42:1210–1218, July 2014

  • Mateus A, Matsson P, Artursson P A high-throughput cell-based method to predict the unbound drug fraction in the brain.J. Med. Chem. 2014 (57)7: 3005-3010.

  • Helge Gad, Tobias Koolmeister, Ann-Sofie Jemth, Saeed Eshtad, Sylvain A. Jacques,Cecilia E. Ström, Linda M. Svensson, Niklas Schultz, Thomas Lundbäck, Berglind Osk Einarsdottir, Aljona Saleh, Camilla Göktürk, Pawel Baranczewski, Richard Svensson, Ronnie P.-A. Berntsson, Robert Gustafsson, Kia Strömberg, Kumar Sanjiv, Marie-Caroline Jacques-Cordonnier, Matthieu Desroses, Anna-Lena Gustavsson, Roger Olofsson, Fredrik Johansson, Evert J. Homan, Olga Loseva, Lars Bräutigam, Lars Johansson, Andreas Höglund, Anna Hagenkort, Therese Pham, Mikael Altun, Fabienne Z. Gaugaz, Svante Vikingsson, Bastiaan Evers, Martin Henriksson, Karl S. A. Vallin, Olov A. Wallner, Lars G. J. Hammarström, Elisee Wiita, Ingrid Almlöf, Christina Kalderén, Hanna Axelsson, Tatjana Djureinovic, Jordi Carreras Puigvert, Maria Häggblad, Fredrik Jeppsson, Ulf Martens, Cecilia Lundin, Bo Lundgren, Ingrid Granelli, Annika Jenmalm Jensen, Per Artursson, Jonas A. Nilsson, Pål Stenmark, Martin Scobie, Ulrika Warpman Berglund & Thomas Helleday MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool Nature, 2014, April 10 , 508, 215–221

  • Satish Srinivas Kitambi, Enrique M. Toledo, Dmitry Usoskin, Shimei Wee, Aditya Harisankar, Richard Svensson, Kristmundur Sigmundsson, Christina Kalderen, Mia Niklasson, Soumi Kundu, Sergi Aranda, Bengt Westermark, Lene Uhrbom, Michael Andäng, Peter Damberg, Sven Nelander, Ernest Arenas, Per Artursson, Julian Walfridsson, Karin Forsberg Nilsson, Lars G.J. Hammarström and Patrik Ernfors Vulnerability of Glioblastoma Cells to Catastrophic Vacuolization and Death Induced by a Small Molecule Cell. 2014 Apr 10;157(2):313-28.

  • Over B, McCarren P, Artursson P, Foley M, Giordanetto F, Grönberg G, Hilgendorf C, Lee MD 4th, Matsson P, Muncipinto G, Pellisson M, Perry MW, Svensson R, Duvall JR, Kihlberg J. Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties. J. Med. Chem., 2014, 57 (6), pp 2746–2754

  • Gising J, Belfrage AK, Alogheli H, Ehrenberg A, Akerblom E, Svensson R, Artursson P, Karlén A, Danielson UH, Larhed M, Sandström A Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket J. Med. Chem., 2014, 57 (5), pp 1790–1801

2013

  • Matsson EM, Eriksson UG, Palm JE, Artursson P, Karlgren M, Lazorova L, Brännström M, Ekdahl A, Dunér K, Knutson L, Johansson S, Schützer KM,Lennernäs H. Combined in vitro-in vivo approach to assess the hepatobiliary disposition of a novel oral thrombin inhibitor. Mol Pharm. 2013 Nov 4;10(11):4252-62

  • Pedersen JM, Matsson P, Bergström CAS, Hoogstraate J,  Norén A, LeCluyse EL, and Artursson P Early Identification of Clinically Relevant Drug Interactions With the Human Bile Salt Export Pump (BSEP/ABCB11) Toxicol Sci. Dec 2013; 136(2): 328–343.

  • Persson LC, Charman WN, Porter CJH, Bergström CAS.Computational prediction of drug solubility in lipid based formulation excipients.Pharmaceutical Research, 2013 Dec;30(12):3225-37.

  • Vodnala SK, Lundbäck T, Yeheskieli E, Sjöberg B, Gustavsson A-L, Svensson R, Olivera GC, Eze AA, de Koning HP, Hammarström LGJ, and Rottenberg, ME Structure-Activity Relationships of Synthetic Cordycepin Analogues as Experimental Therapeutics for African Trypanosomiasis J. Med. Chem., 2013, 56 (24), pp 9861–9873

  • Lampa, Anna; Bergman, Sara; Svahn Gustafsson, Sofia; Alogheli, Hiba; Åkerblom, Eva; Lindeberg, Gunnar; Svensson, Richard; Artursson, Per; Danielson, U. Helena; Karlén, Anders; Sandström, Anja Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1´ Region ACS Med. Chem. Lett., 2014, 5 (3), pp 249–254

  • Neve EP, Artursson P, Ingelman-Sundberg M, Karlgren M An integrated in vitro model for simultaneous assessment of drug uptake, metabolism, and efflux Molecular Pharmacology 2013 Aug 5;10(8):3152-63

  • Matsson P, Artursson P Computational prospecting for drug-transporter interactions Clinical Pharmacology & Therapeutics 2013 Jul;94(1):30-2

  • Prieto P, Kinsner-Ovaskainen A, Stanzel S, Albella B, Artursson P, Campillo N, Cecchelli R, Cerrato L, Díaz L, Di Consiglio E, Guerra A, Gombau L, Herrera G, Honegger P, Landry C, O'Connor JE, Páez JA, Quintas G, Svensson R, Turco L, Zurich MG, Zurbano MJ, Kopp-Schneider A The value of selected in vitro and in silico methods to predict acute oral toxicity in a regulatory context: results from the European Project ACuteTox Toxicology In Vitro 2013 Jun;27(4):1357-76

  • Fransson R, Sköld C, Kratz JM, Svensson R, Artursson P, Nyberg F, Hallberg M, Sandström A Constrained H-Phe-Phe-NH2 Analogues with High Affinity to the Substance P 1-7 Binding Site and with Improved Metabolic Stability and Cell Permeability Journal of Medicinal Chemistry 2013 56(12):4953-65

  • Mateus A, Matsson P, Artursson P Rapid measurement of intracellular unbound drug concentrations Molecular Pharmacology 2013 10(6):2467-78

  • Warren DB, Bergström CAS, Benameur H, Porter CJ, Pouton CW Evaluation of the structural determinants of polymeric precipitation inhibitors using solvent shift methods and principle component analysis.Molecular Pharmaceutics, 2013 Aug 5;10(8):2823-48.

  • Tehler U, Fagerberg JH, Svensson R, Larhed M, Artursson P, Bergström CA Optimizing solubility and permeability of a biopharmaceutics classification system (BCS) class 4 antibiotic drug using lipophilic fragments disturbing the crystal lattice Journal of Medicinal Chemistry 2013, 56(6):2690-4

  • Vodnala S, Lundbäck T, Sjöberg B, Svensson R, Rottenberg ME, Hammarström LGJ In vitro and In vivo Activity of 2-Aminopyrazines/2-Aminopyridines in Experimental Models of Human African Trypanosomiasis Antimicrobial Agents And Chemotherapy 2013, 57(2), 1012-101

  • Artursson P, Matsson P and Karlgren M In vitro characterization of interactions with drug transporting proteins Transporters in Drug Discovery, Development and Use. Eds: Sugiyama Y, Steffansen B. Springer,  2011 Volume 7, 2013, pp 37-65

2012

  • Karlgren, M., Vildhede, A., Norinder, U., Wisniewski, J., Lai, Yurong., Haglund, U. and Artursson, P. Classification of inhibitors of liver specific organic anion transporting polypeptides – influence of protein expression on drug-drug interactions Journal of Medicinal Chemistry 2012 May 24;55(10):4740-63

  • Di, L., Artursson, P., Avdeef, A., Ecker, G.F., Faller, B., Fischer, H., Kansy, M., Krämer, S., Lennernäs, H., Sugano, K Evidence-based approach to assess passive diffusion and carrier-mediated drug transport Drug Discov Today. 2012 Aug;17(15-16):905-12

  • Bergström CAS, Charman SA, Nicolazzo JA.

  • Fagerberg JH, Al-Tikriti Y, Ragnarsson G, Bergström CAS.Ethanol Effects on Apparent Solubility of Poorly Soluble Drugs in Simulated Intestinal Fluid.Molecular Pharmaceutics, 2012 Jul 2;9(7):1942-52

  • Karlgren M, Ahlin G, Bergström C.A., Svensson R, Palm J, Artursson P In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug-Drug Interactions Pharmaceutical Research 2012 Feb;29(2):411-26

2011

  • Lazorova, L, Hubatsch, I, Ekegren, J.K., Gising, J, Nakai, D, Zaki, N.M., Bergström, CAS, Norinder, U, Larhed, M, Artursson, P Structural features determining the intestinal epithelial permeability and efflux of novel HIV-1 protease inhibitors Journal Of Pharmacological Sciences 100 (9), 3763-72, 2011

2010

  • Fagerberg JH, Tsinman O, Sun N, Tsinman K, Avdeef A and Bergström CAS.Dissolution Rate and Apparent Solubility of Poorly Soluble Compounds in Biorelevant Dissolution Media.Molecular Pharmaceutics, 2010, 7, 1419-1430.

  • Zaki N, Artursson P and Bergström CAS.A Modified Physiological BCS for Prediction of Intestinal Absorption in Drug Discovery.Molecular Pharmaceutics, 2010, 7(5), 1478–1487.

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