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Jarkko Rautio

Jarkko Rautio

Laitoksen varajohtaja

Professori

Olen farmaseuttisen kemian professori ja farmasian laitoksen varajohtaja. Lisäksi toimin lääketutkimuksen tohtoriohjelman (DPDR) johtajana.

Farmasian laitos, Terveystieteiden tiedekunta

jarkko.rautio@uef.fi | 040 353 2791

Tiedot Julkaisut

Tutkimusaiheenani on lääkeaineiden ominaisuuksien, kuten kulkeutumisen ja kohdentamisen, parantaminen erityisesti aihiolääketeknologian avulla.
Viime aikainen tutkimuksemme on keskittynyt hyödyntämään elimistön omia kuljetinproteiineja – aminohappotransportteria (LAT1) ja glukoositransportteria (GLUT1) – lääkeaineiden kohdennetussa kuljetuksessa veriaivoesteen läpi keskushermostoon ja solukalvon läpi syöpäsoluihin. Tutkimuksemme on keskittynyt erityisesti glioomasoluihin. Hyödynnämme laajasti eri tutkimusmenetelmiä in vitro menetelmistä ja yhdisteiden solun sisäänotosta in vivo farmakokineettisiin tutkimuksiin.

Tutkimusryhmät

Lääkeaine- ja synteesikemian laboratorio 01.01.2010 -

Avainsanat

aihiolääke farmakokinetiikka farmaseuttinen kemia farmasia kuljetinproteiini-välitteinen lääkeaineiden kuljetus ja kohdentaminen kuljetinproteiinit lääkeaineanalytiikka lääkeaineiden kuljetus ja kohdentaminen lääkeainekemia

Julkaisut

106/106 kappaletta

A technological comparison of freeze-dried poly-ɛ-caprolactone (PCL) and poly (lactic-co-glycolic acid) (PLGA) nanoparticles loaded with clozapine for nose-to-brain delivery
Lombardo, Rosamaria; Ruponen, Marika; Rautio, Jarkko; Lampinen, Riikka; Kanninen, Katja M.; Koivisto, Anne M.; Penttilä, Elina; Löppönen, Heikki; Demartis, Sara; Giunchedi, Paolo; Rassu, Giovanna; Fragalà, Maria Elena; Pignatello, Rosario. 2024. Journal of drug delivery science and technology. 93: . 105419
Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments
Zingale, Elide; Bonaccorso, Angela; D’Amico, Agata Grazia; Lombardo, Rosamaria; D’Agata, Velia; Rautio, Jarkko; Pignatello, Rosario. 2024. Pharmaceutics. 16:
Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates
Subbaiah, Murugaiah A M; Rautio, Jarkko; Meanwell, Nicholas A. 2024. Chemical society reviews. 53: 2099-2210
Specific Transport of Temozolomide Does Not Override DNA Repair-mediated Chemoresistance
Bahrami, Katayan; Kärkkäinen, Jussi; Bibi, Sania; Huttunen, Johanna; Tampio, Janne; Montaser, Ahmed B.; Moody, Catherine L; Lehtonen, Marko; Rautio, Jarkko; Wheelhouse, Richard T; Huttunen, Kristiina M. 2024. European journal of pharmaceutical sciences. 195:
Altering distribution profile of palbociclib by its prodrugs
Järvinen, Juulia; Montaser, Ahmed B; Adla, Santosh Kumar; Leppänen, Jukka; Lehtonen, Marko; Vellonen, Kati-Sisko; Laitinen, Tuomo; Jalkanen, Aaro; Elmquist, William F; Timonen, Juri; Huttunen, Kristiina M; Rautio, Jarkko. 2023. European journal of pharmaceutical sciences. 2024; 192:
Amino Acid-Based Boron Carriers in Boron Neutron Capture Therapy (BNCT)
Järvinen, Juulia; Pulkkinen, Herkko; Rautio, Jarkko; Timonen, Juri M. 2023. Pharmaceutics. 15:
Development of Lyophilised Eudragit® Retard Nanoparticles for the Sustained Release of Clozapine via Intranasal Administration
Lombardo, Rosamaria; Ruponen, Marika; Rautio, Jarkko; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Calosi, Laura; Bani, Daniele; Lampinen, Riikka; Kanninen, Katja M.; Koivisto, Anne M; Penttilä, Elina; Löppönen, Heikki; Pignatello, Rosario. 2023. Pharmaceutics. 15:
Farmaseuttinen kemia
Jarho, Pekka; Lahtela-Kakkonen, Maija; Vepsäläinen, Jouko; Rautio, Jarkko; Huttunen, Kristiina; Poso, Antti; Auriola, Seppo. 2023. Publications of the University of Eastern Finland. General series. 44: 32-35
Sweet Battle of the Epimers─Continued Exploration of Monosaccharide-Derived Delivery Agents for Boron Neutron Capture Therapy
Matović, Jelena; Bahrami, Katayun; Stockmann, Philipp; Sokka, Iris K; Khng, You Cheng; Sarparanta, Mirkka; Hey-Hawkins, Evamarie; Rautio, Jarkko; Ekholm, Filip S. 2023. Molecular pharmaceutics. 20: 3127-3139
Targeting Glial Cells by Organic Anion-Transporting Polypeptide 1C1 (OATP1C1)-Utilizing l-Thyroxine-Derived Prodrugs
Tonduru, Arun Kumar; Maljaei, Seyed Hamed; Adla, Santosh Kumar; Anamea, Landry; Tampio, Janne; Králová, Adéla; Jalkanen, Aaro J; Espada, Catarina; Santos, Inês Falcato; Montaser, Ahmed B; Rautio, Jarkko; Kronenberger, Thales; Poso, Antti; Huttunen, Kristiina M. 2023. Journal of medicinal chemistry. 66: 15094-15114
Tetrazine Glycoconjugate for Pretargeted Positron Emission Tomography Imaging of trans-Cyclooctene-Functionalized Molecular Spherical Nucleic Acids
Auchynnikava, Tatsiana; Aarela, Antti; Liljenback, Heidi; Jarvinen, Juulia; Andriana, Putri; Kovacs, Luciana; Rautio, Jarkko; Rajander, Johan; Virta, Pasi; Roivainen, Anne; Li, Xiang-Guo; Airaksinen, Anu J.. 2023. ACS omega. 8: 45326-45336
Development of Sesamol Carbamate-L-Phenylalanine Prodrug Targeting L-Type Amino Acid Transporter1 (LAT1) as a Potential Antiproliferative Agent against Melanoma
Srisongkram, Tarapong; Bahrami, Katayun; Järvinen, Juulia; Timonen, Juri; Rautio, Jarkko; Weerapreeyakul, Natthida. 2022. International journal of molecular sciences. 23: . 8446
In-vitro dynamic dissolution/bioconversion/permeation of fosamprenavir using a novel tool with an artificial biomimetic permeation barrier and microdialysis-sampling
Eriksen, Jonas Borregaard; Christiansen, Jeppe Juhl; Bauer-Brandl, Annette; Ruponen, Marika; Rautio, Jarkko; Brandl, Martin. 2022. European journal of pharmaceutical sciences. 2023; 181:
Structural Features Affecting the Interactions and Transportability of LAT1-Targeted Phenylalanine Drug Conjugates
Bahrami, Katayun; Järvinen, Juulia; Laitinen, Tuomo; Reinisalo, Mika; Honkakoski, Paavo; Poso, Antti; Huttunen, Kristiina M.; Rautio, Jarkko. 2022. Molecular pharmaceutics. 2023; 20: 206-218
Synthesis and In Vitro Evaluation of a Set of 6-Deoxy-6-thio-carboranyl d-Glucoconjugates Shed Light on the Substrate Specificity of the GLUT1 Transporter
Matović, Jelena; Järvinen, Juulia; Sokka, Iris K; Stockmann, Philipp; Kellert, Martin; Imlimthan, Surachet; Sarparanta, Mirkka; Johansson, Mikael P; Hey-Hawkins, Evamarie; Rautio, Jarkko; Ekholm, Filip S. 2022. ACS omega. 7: 30376-30388
Molecular characteristics supporting L-Type amino acid transporter 1 (LAT1)-mediated translocation
Kärkkäinen, Jussi; Laitinen, Tuomo; Markowicz-Piasecka, Magdalena; Montaser, Ahmed; Lehtonen, Marko; Rautio, Jarkko; Gynther, Mikko; Poso, Antti; Huttunen, Kristiina M. 2021. Bioorganic chemistry. 112: 104921
Species differences in the intra-brain distribution of an L-type amino acid transporter 1 (LAT1) -utilizing compound between mice and rats
Jalkanen, Aaro J.; Ihalainen, Jouni; Lehtonen, Marko; Forsberg, Markus M.; Rautio, Jarkko; Huttunen, Kristiina M.; Gynther, Mikko. 2021. International journal of pharmaceutics. 596: 120300
Addressing the biochemical foundations of a glucose-based "Trojan horse"-stradegy to boron neutron capture therephy: from chemical synthesis to in vitro assesment
Matovic, Jelena; Järvinen, Juulia; Bland, Helena C; Sokka, Iris K; Imlimthan, Surachet; Ferrando, Ruth Mateu; Huttunen, Kristiina M; Timonen, Juri; Peräniemi, Sirpa; Aitio, Olli; Airaksinen, Anu J; Sarparanta, Mirkka; Johansson, Mikael P; Rautio, Jarkko; Ekholm, Filip S. 2020. Molecular pharmaceutics. 17: 3885-3899
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7
Gütschow, Michael; Eynde, Jean Jacques Vanden; Jampilek, Josef; Kang, CongBao; Mangoni, Arduino A; Fossa, Paola; Karaman, Rafik; Trabocchi, Andrea; Scott, Peter JH; Reynisson, Jóhannes; Rapposelli, Simona; Galdiero, Stefania; Winum, Jean-Yves; Brullo, Chiara; Prokai-Tatrai, Katalin; Sharma, Arun K; Schapira, Matthieu; Azuma, Yasu-Taka; Cerchia, Laura; Spetea, Mariana; et al. [incl. Rautio, J]. 2020. Molecules. 25: E2968
Exploring the Biochemical Foundations of a Successful GLUT1-Targeting Strategy to BNCT: Chemical Synthesis and In Vitro Evaluation of the Entire Positional Isomer Library of ortho-Carboranylmethyl-Bearing Glucoconjugates
Matovic, Jelena; Järvinen, Juulia; Sokka, Iris K; Imlimthan, Surachet; Raitanen, Jan-Erik; Montaser, Ahmed; Maaheimo, Hannu; Huttunen, Kristiina M; Peräniemi, Sirpa; Airaksinen, Anu J; Sarparanta, Mirkka; Johansson, Mikael P; Rautio, Jarkko; Ekholm, Filip S. 2020. Molecular pharmaceutics. 2021; 18: 285-304
Intranasal Nanoemulsions for Direct Nose-to-Brain Delivery of Actives for CNS Disorders
Bahadur, Shiv; Pardhi, Dinesh M; Rautio, Jarkko; Rosenholm, Jessica M; Pathak, Kamla. 2020. Pharmaceutics. 12: 1230
Prodrug Approach for Posterior Eye Drug Delivery: Synthesis of Novel Ganciclovir Prodrugs and in Vitro Screening with Cassette Dosing
Heikkinen, Emma M; Ruponen, Marika; Jasper, Lisa-Marie; Leppänen, Jukka; Hellinen, Laura; Urtti, Arto; Auriola, Seppo; Rautio, Jarkko; Vellonen, Kati-Sisko. 2020. Molecular pharmaceutics. 17: 1945-1953
Tyrosine-chlorambucil conjugates facilitate cellular uptake through L-type amino acid transporter 1 (LAT1) in human breast cancer cell line MCF-7
Pocasap, P; Weerapreeyakul, N; Timonen, J; Järvinen, J; Leppänen, J; Kärkkäinen, J; Rautio, J. 2020. International journal of molecular sciences. 21: 2132
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5
Mangoni, AA; Eynde, JJV; Jampilek, J; Hadjipavlou-Litina, D; Liu, H; Reynisson, J; Sousa, ME; Gomes, PAC; Prokai-Tatrai, K; Tuccinardi, T; Sabatier, JM; Luque, FJ; Rautio, J; Karaman, R; Vasconcelos, MH; Gemma, S; Galdiero, S; Hulme, C; Collina, S; Gütschow, M; et al.. 2019. Molecules. 24: 2415
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6
Vanden Eynde, JJ; Mangoni, AA; Rautio, J; Leprince, J; Azuma, YT; García-Sosa, AT; Hulme, C; Jampilek, J; Karaman, R; Li, W; Gomes, PAC; Hadjipavlou-Litina, D; Capasso, R; Geronikaki, A; Cerchia, L; Sabatier, JM; Ragno, R; Tuccinardi, T; Trabocchi, A; Winum, JY et al.. 2019. Molecules. 2020; 25: 1-24
Role of L-Type Amino Acid Transporter 1 (LAT1) for the Selective Cytotoxicity of Sesamol in Human Melanoma Cells
Srisongkram, T; Weerapreeyakul, N; Kärkkäinen, J; Rautio, J. 2019. Molecules. 24: 3869
Aihiolääkkeet
Rautio, Jarkko. Teoksessa: Koulu, Markku; Mervaala, Eero(toim.) , 2018. Farmakologia ja toksikologia. s. 109. Kustannusosakeyhtiö Medicina
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3
Mangoni, AA; Tuccanardi, T; Collina, S; Vanden Eynde, JJ; Muñoz-Torrero, D; Karaman, R; Siciliano, C; de Sousa, ME; Prokai-Tatrai, K; Rautio, J; Guillou, C; Gütschow, M; Galdiero, S; Liu, H; Agrofoglio, LA; Sabatier, JM; Hulme, C; Kokotos, G; You, Q; Gomes, PAC. 2018. Molecules. 23: 1596
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-4
Mangoni, AA; Guillou, C; Vanden Eynde, JJ; Hulme, C; Jampilek, J; Li, W; Prokai-Tatrai, K; Rautio, J; Collina, S; Tuccinardi, T; Sousa, ME; Sabatier, JM; Galdiero, S; Karaman, R; Kokotos, G; Torri, G; Luque, FJ; Vasconcelos, MH; Hadjipavlou-Litina, D; Siciliano, C; et al. 2018. Molecules. 24: 130
Discovery of Polar Spirocyclic Orally Bioavailable Urea Inhibitors of Soluble Epoxide Hydrolase
Lukin, Alexey; Kramer, Jan; Hartmann, Markus; Weizel, Lilia; Hernandez- Olmos, Victor; Falahati, Konstantin; Burghardt, Irene; Kalinchenkova, Natalia; Bagnyukova, Darya; Zhurilo, Nikolay; Rautio, Jarkko; Forsberg, Markus; Ihalainen, Jouni; Auriola, Seppo; Leppänen, Jukka; Konstantinov, Igor; Pogoryelov, Denys; Proschak, Ewgenij; Dar'in, Dmitry; Krasavin, Mikhail. 2018. Bioorganic chemistry. 80: 655-667
Secondary carbamate linker can facilitate the sustained release of dopamine from brain-targeted prodrug
Thiele, Nikki A; Kärkkäinen, Jussi; Sloan, Kenneth B; Rautio, Jarkko; Huttunen, Kristiina M. 2018. Bioorganic and medicinal chemistry letters. 28: 2856-2860
Structural properties for selective and efficient L-type amino acid transporter 1 (LAT1) mediated cellular uptake
Kärkkäinen, J; Gynther, M; Kokkola, T; Petsalo, A; Auriola, S; Lahtela-Kakkonen, M; Laine, K; Rautio, J; Huttunen, KM. 2018. International journal of pharmaceutics. 544: 91-99
The expanding role of prodrugs in contemporary drug design and development
Rautio, Jarkko; Meanwell, Nicholas A; Di, Li; Hageman, Michael J. 2018. Nature reviews drug discovery. 17: 559-587
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes
Muñoz-Torrero D, Mangoni AA, Guillou C, Collina S, Eynde JJV, Rautio J, Keseru GM, Hulme C, Chibale K, Luque FJ, Karaman R, Gütschow M, Liu H, Ragno R. 2017. Molecules. 22: 743
Breakthroughs in medicinal chemistry: New targets and mechanisms, new drugs, new hopes-2
Muñoz-Torrero, D; Mangoni, AA; Liu, H; Hulme, C; Rautio, J; Karaman, R; De Sousa, ME; Prokai-Tatrai, K; Sabatier, J-M; Siciliano, C; Luque, FJ; Kokotos, G; Ragno, R; Collina, S; Guillou, C; Gütschow, M; Agrofoglio, LA. 2017. Molecules. 2018; 23: 65
High-accuracy mass spectrometry for identification of sulphur-containing bioactive constituents and flavonoids in extracts of Raphanus sativus var. caudatus Alef (Thai rat-tailed radish)
Sangthonga S, Weerapreeyakulb N, Lehtonen M, Leppanen J, Rautio J. 2017. Journal of functional foods. 31: 237-247
Prodrugs : recent approvals and a glimpse of the pipeline
Rautio Jarkko, Kärkkäinen Jussi, Sloan Kenneth B. 2017. European journal of pharmaceutical sciences. 109: 146-161
Prodrugs in medicinal chemistry and enzyme prodrug therapies
Walther Raoul, Rautio Jarkko, Zelikin Alexander N. 2017. Advanced drug delivery reviews. 118: 65-77
Amino Acid Promoieties Alter Valproic Acid Pharmacokinetics and Enable Extended Brain Exposure
Gynther Mikko, Peura Lauri, Vernerová Monika, Leppänen Jukka, Kärkkäinen Jussi, Lehtonen Marko, Rautio Jarkko, Huttunen Kristiina M. 2016. Neurochemical research. 41: 2797-2809
Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835
Krasavin Mikhail, Lukin Alexey, Bagnyukova Daria, Zhurilo Nikolay, Zahanich Ihor, Zozulya Sergey, Ihalainen Jouni, Forsberg Markus M, Lehtonen Marko, Rautio Jarkko, Moore Daniel, Tikhonova Irina G. 2016. Bioorganic and medicinal chemistry. 24: 5481-5494
Aihiolääketeknologia lääkekehityksessä
Rautio Jarkko, Huttunen Kristiina, Gynther Mikko, Laine Krista, Leppänen Jukka, Kärkkäinen Jussi, Malmioja Kalle. 2014. Dosis. 30: 209
Amino acid ester prodrugs conjugated to the alpha-carboxylic acid group do not display affinity for the L-type amino acid transporter 1 (LAT1)
Rautio Jarkko, Kärkkäinen Jussi, Huttunen Kristiina, Gynther Mikko. 2014. European journal of pharmaceutical sciences. 2015; 66: 36-40
Brain Pharmacokinetics of Ganciclovir in Rats with Orthotopic BT4C Glioma
Gynther Mikko, Kääriäinen Tiina M, Hakkarainen Jenni J, Jalkanen Aaro J, Petsalo Aleksanteri, Lehtonen Marko, Peura Lauri, Kurkipuro Jere, Samaranayake Haritha, Yla-Herttuala Seppo, Rautio Jarkko, Forsberg Markus M. 2014. Drug metabolism and disposition. 2015; 43: 140-146
Evaluation of novel imidazotetrazine analogues designed to overcome temozolomide resistance and glioblastoma regrowth
Ramirez Yulian P, Mladek Ann C, Phillips Roger M, Gynther Mikko, Rautio Jarkko, Ross Alonzo H, Wheelhouse Richard T, Sakaria Jann N. 2014. Molecular cancer therapeutics. 2015; 14: 111-119
Glutathione-S-transferase selective release of metformin from its sulfonamide prodrug
Rautio Jarkko, Vernerová Monika, Aufderhaar Imke, Huttunen Kristiina M. 2014. Bioorganic and medicinal chemistry letters. 24: 5034-5036
Quantitative Insight into the Design of Compounds Recognized by the L-Type Amino Acid Transporter 1 (LAT1)
Ylikangas Henna, Malmioja Kalle, Peura Lauri, Gynther Mikko, Nwachukwu Emmanuel O, Leppänen Jukka, Laine Krista, Rautio Jarkko, Lahtela-Kakkonen Maija, Huttunen Kristiina M, Poso Antti. 2014. Chemmedchem. 9: 2699-2707
Convenient microwave-assisted synthesis of lipophilic sulfenamide prodrugs of metformin
Huttunen Kristiina M, Leppänen Jukka, Laine Krista, Vepsäläinen Jouko, Rautio Jarkko. 2013. European journal of pharmaceutical sciences. 49: 624-628
Design, synthesis and brain uptake of LAT1-targeted amino acid prodrugs of dopamine
Peura Lauri, Malmioja Kalle, Huttunen Kristiina, Leppänen Jukka, Hämäläinen Miia, Forsberg Markus M, Gynther Mikko, Rautio Jarkko, Laine Krista. 2013. Pharmaceutical research. 30: 2523-2537
Farmaseuttinen kemia - uudet haasteet Itä-Suomen yliopistossa
Nevalainen Tapio, Poso Antti, Rautio Jarkko. Teoksessa: Ahonen R, Laitinen K, Lapinjoki S, Mensalo P, Ranta V-P, Ylikangas H (toim).(toim.) , 2013. Muutosten vuosikymmen : Itä-Suomen yliopiston farmasian laitos 40 vuotta. s. 34-42.
LAT1-mediated prodrug uptake: a way to breach the blood-brain barrier?
Rautio Jarkko, Gynther Mikko, Laine Krista. 2013. Therapeutic delivery. 4: 281-284
Amino acids as promoieties in prodrug design and development
Vig Balvinder S, Huttunen Kristiina M, Laine Krista, Rautio Jarkko. 2012. Advanced drug delivery reviews. 2013:65: 1370-1385
Design, synthesis, and evaluation of novel cyclic phosphates of 5-aminosalicylic acid as cytochrome P450-activated prodrugs
Huttunen Kristiina M, Tani Niina, Juvonen Risto O, Raunio Hannu, Rautio Jarkko. 2012. Molecular pharmaceutics. 2013:10: 532-537
In vitro and in vivo evaluation of a sulfenamide prodrug of basic metformin
Huttunen Kristiina M, Leppänen Jukka, Vepsäläinen Jouko, Sirviö Jouni, Laine Krista, Rautio Jarkko. 2012. Journal of pharmaceutical sciences. 101: 2854-2860
Inhibitors of LRRK2 kinase activity to probe the treatment option in Parkinson's disease
Rautio Jarkko. 2012. Journal of medicinal chemistry. 55: 9414-9415
Structure-activity relationship study of compounds binding to large amino acid transporter 1 (LAT1) based on pharmacophore modeling and in situ rat brain perfusion
Ylikangas Henna, Peura Lauri, Malmioja Kalle, Leppänen Jukka, Laine Krista, Poso Antti, Lahtela-Kakkonen Maija, Rautio Jarkko. 2012. European journal of pharmaceutical sciences. 2013:48: 523-531
Aihiolääketeknologia lääkekehityksessä. [Summary: Prodrug technology in the development of medicinal agents]
Peura Lauri, Malmioja Kalle, Rautio Jarkko. 2011. Duodecim. 127: 263-272
Amino acid prodrugs for oral delivery: challenges and opportunities
Vig Balvinder, Rautio Jarkko. 2011. Therapeutic delivery. 2: 959-962
Large amino acid transporter 1 (LAT1) prodrugs of valproic acid: new prodrug design ideas for central nervous system delivery
Peura Lauri, Malmioja Kalle, Laine Krista, Leppänen Jukka, Gynther Mikko, Isotalo Antti, Rautio Jarkko. 2011. Molecular pharmaceutics. 8: 1857-1866
New Prodrug Design Ideas for Transporter-Mediated CNS Drug Delivery
Kalle Malmioja, Lauri Peura, Krista Laine, Jukka Leppänen, Mikko Gynther, Jarkko Rautio. 2011.
New Prodrug Desing Ideas for Large Amino Acid Transporter 1 -Mediated Drug Brain Delivery
Peura L, Malmioja K, Laine K, Leppänen J, Gynther M & Rautio J. 2011.
Prodrug strategies in drug design
Rautio Jarkko. Teoksessa: Rautio Jarkko(toim.) , 2011. Prodrugs and Targeted Delivery. s. 3-30. Wiley-VCH Verlag
Prodrugs - an efficient way to breach delivery and targeting barriers
Huttunen Kristiina M, Rautio Jarkko. 2011. Current topics in medicinal chemistry. 11: 2265-2287
Prodrugs - from serendipity to rational design
Huttunen Kristiina, Raunio Hannu, Rautio Jarkko. 2011. Pharmacological reviews. 63: 750 - 771
Prodrugs and Targeted Delivery: Towards Better ADME Properties
Rautio Jarkko. 2011. Methods and Principles in Medicinal Chemistry. . WILEY-VCH Verlag GmbH & Co. KCaA
Prodrugs designed to target transporters for oral drug delivery
Warren Mark S, Rautio Jarkko. Teoksessa: Rautio Jarkko(toim.) , 2011. Prodrugs and Targeted Delivery. s. 231-252. Wiley-VCH Verlag
Brain uptake of ketoprofen-lysine prodrug in rats
Gynther M, Jalkanen A, Lehtonen M, Forsberg M, Laine K, Ropponen J, Leppänen J, Knuuti J & Rautio J. 2010. International journal of pharmaceutics. 399: 121-128
Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor
Rautio J, Leppänen J, Lehtonen M, Laine K, Koskinen M, Pystynen J, Savolainen J & Sairanen M. 2010. Bioorganic and medicinal chemistry letters. 20: 2614 - 2616
Enzyme-activated prodrug strategies for targeted drug action
Rautio Jarkko, Laine Krista, Fang Lanyan, Han Bing, Huttunen Kristiina, Sun Duxin. Teoksessa: Ram I. Mahato and Ajit S. Narang(toim.) , 2010. Targeted Delivery of Small and Macromolecular Drugs. s. 311-348. CRC Press, Taylor& Francis Group
Determination of metformin and its prodrugs in human and rat blood by hydrophilic interaction liquid chromatography
Huttunen KM, Rautio J, Leppänen J, Vepsäläinen J, Keski-Rahkonen P. 2009. Journal of pharmaceutical and biomedical analysis. 50: 469-474
Glucose promoiety enables glucose transporter mediated brain uptake of ketoprofen and indomethacin prodrugs in rats
Gynther M, Ropponen J, Laine K, Leppänen J, Haapakoski P, Peura L, Järvinen T, Rautio J. 2009. Journal of medicinal chemistry. 52: 3348-3353
The first bioreversible prodrug of metformin with improved lipophilicity and enhanced intestinal absorption
Huttunen KM, Mannila A, Laine K, Kemppainen E, Leppänen J, Vepsäläinen J, Järvinen T, Rautio J. 2009. Journal of medicinal chemistry. 52: 4142-4148
Cytochrome P450-activated prodrugs: targeted drug delivery
Huttunen KM, Mähönen N, Raunio H, Rautio J. 2008. Current medicinal chemistry. 15: 2346-2365
Diclofenac readily penetrates the cerebrospinal fluid in children
Kokki H, Kumpulainen E, Laisalmi M, Savolainen J, Rautio J, Lehtonen M. 2008. British journal of clinical pharmacology. 65: 879-884
Enhanced brain drug delivery and targeting
Rautio J, Laine K, Gynther M. 2008. PHARMACEUTICAL TECHNOLOGY EUROPE. 20: 27-33
How readily does ketorolac penetrate cerebrospinal fluid in children?
Kumpulainen E, Kokki H, Laisalmi M, Heikkinen M, Savolainen J, Rautio J, Lehtonen M. 2008. Journal of clinical pharmacology. 48: 495-501
Large neutral amino acid transporter enables brain drug delivery via prodrugs
Gynther M, Laine K, Ropponen J, Leppänen J, Mannila A, Nevalainen T, Savolainen J, Järvinen T, Rautio J. 2008. Journal of medicinal chemistry. 51: 932-936
Prodrug approaches for CNS delivery
Rautio Jarkko, Laine Krista, Gynther Mikko, Savolainen Jouko. 2008. AAPS journal. 10: 92-102
Prodrugs: design and clinical applications
Rautio J, Kumpulainen H, Heimbach T, Oliyai R, Oh D, Järvinen T, Savolainen J. 2008. Nature reviews drug discovery. 7: 255-270
Synthesis, in vitro and in vivo characterization of novel ethyl dioxy phosphate prodrug of propofol
Kumpulainen H, Järvinen T, Mannila A, Leppänen J, Nevalainen T, Mäntylä A, Vepsäläinen J, Rautio J. 2008. European journal of pharmaceutical sciences. 34: 110-117
Aminocarbonyloxymethyl ester prodrugs of flufenamic acid and diclofenac: suppressing the rearrangement pathway in aqueous media
Ribeiro L, Silva N, Iley J, Rautio J, Järvinen T, Hélder M-F, Moreira R, Mendes E. 2007. Archiv der pharmazie. 340: 32-40
Cerebrospinal fluid distribution of ibuprofen after intravenous administration in children
Kokki H, Kumpulainen E, Lehtonen M, Laisalmi M, Heikkinen M, Savolainen J, Rautio J. 2007. Pediatrics. 120: e1002-e1008
Novel cyclic phosphate prodrug approach for cytochrome P450-activated drugs containing an alcohol functionality
Huttunen KM, Mähönen N, Leppänen J, Vepsäläinen J, Juvonen RO, Raunio H, Kumpulainen H, Järvinen T, Rautio J. 2007. Pharmaceutical research. 24: 679-687
Plasma and cerebrospinal fluid concentrations of indomethacin in children after intravenous administration
Mannila A, Kumpulainen E, Lehtonen M, Heikkinen M, Laisalmi M, Salo T, Rautio J, Savolainen J, Kokki H. 2007. Journal of clinical pharmacology. 47: 94-100
Convenient microwave-assisted synthesis of 1-chloroethyl phosphates
Kumpulainen H, Saari R, Lehtonen M, Rautio J, Järvinen T, Vepsäläinen J. 2006. Tetrahedron letters. 47: 2003-2004
Design for optimized topical delivery: prodrugs and a paradigm change
Sloan KB, Wasdo SC, Rautio J. 2006. Pharmaceutical research. 23: 2729-2747
Efficient strategy to prepare water-soluble prodrugs of ketones
Huttunen KM, Kumpulainen H, Leppänen J, Rautio J, Järvinen T, Vepsäläinen J. 2006. Synlett. : 701-704
Evaluation of hydroxyimine as cytochrome P450-selective prodrug structure
Kumpulainen H, Mähönen N, Laitinen M-L, Jaurakkajärvi M, Raunio H, Juvonen RO, Vepsäläinen J, Järvinen T, Rautio J. 2006. Journal of medicinal chemistry. 49: 1207-1211
In vitro P-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates
Rautio J, Humphreys JE, Webster LO, Balakrishnan A, Keogh JP, Kunta JR, Serabjit-Singh CJ, Polli JW. 2006. Drug metabolism and disposition. 34: 786-792
Inefficient central nervous system delivery limits the use of ibuprofen in neurodegenerative diseases
Mannila A, Rautio J, Lehtonen M, Järvinen T, Savolainen J. 2005. European journal of pharmaceutical sciences. 24: 101-105
Design, synthesis and in vitro evaluation of novel water-soluble prodrugs of buparvaquone
Mäntylä A, Rautio J, Nevalainen T, Keski-Rahkonen P, Vepsäläinen J, Järvinen T. 2004. European journal of pharmaceutical sciences. : 151-158
Drug delivery systems for brain tumor therapy
Rautio J, Chikhale PJ. 2004. Current pharmaceutical design. 10: 1341-1353
Lääkeaineiden ihonläpäisevyyttä parantavat menetelmät
Näsi E, Rautio J. 2004. Dosis. 20: 209-222
Synthesis and antileishmanial activity of novel buparvaquone oxime derivatives
Mäntylä A, Rautio J, Nevalainen T, Vepsälainen J, Juvonen R, Kendrick H, Garnier T, Croft SL, Järvinen T. 2004. Bioorganic and medicinal chemistry. 12: 3497-3502
Synthesis, in vitro evaluation, and antileishmanial activity of water-soluble prodrugs of buparvaquone
Mäntylä A, Garnier T, Rautio J, Nevalainen T, Vepsäläinen J, Koskinen A, Croft SL, Järvinen T. 2004. Journal of medicinal chemistry. 47: 188-195
A novel D2-dopaminergic and alfa2-adrenoceptor receptor agonist induces substantial and prolonged IOP decrease in normotensive rabbits
Savolainen J, Rautio J, Razzetti R, Järvinen T. 2003. Journal of pharmacy and pharmacology. 55: 789-794
Ei-steroidaalisten anti-inflammatoristen karboksyylihappojen aihiolääkkeitä sisältävät farmaseuttiset koostumukset topikaaliseen käyttöön
Järvinen T, Rautio J, Nevalainen T, Taipale H, Vepsäläinen J, Gynther J. 2003.
Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate
Tolle-Sander S, Rautio J, Wring S, Polli JW, Polli JE. 2003. Pharmaceutical research. 20: 757-764
Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents
Mendes E, Furtado T, Neres J, Iley J, Jarvinen T, Rautio J, Moreira R. 2002. Bioorganic and medicinal chemistry. 10: 809-816
Aihiolääkkeet parantavat lääkeaineen ihonläpäisevyyttä
Rautio J. 2000. Dosis. 16: 314-317
Piperazinylalkyl prodrugs of naproxen improve in vitro skin permeation
Rautio J, Nevalainen T, Taipale H, Vepsäläinen J, Gynther J, Laine K, Järvinen T. 2000. European journal of pharmaceutical sciences. 11: 157-163
Synthesis and in Vitro Evaluation of Novel Naproxen and Ketoprofen Prodrugs for Topical Drug Delivery
Rautio J. 2000. Kuopion yliopiston julkaisuja A. Farmaseuttiset tieteet
Synthesis and in vitro evaluation of novel morpholinyl- and methylpiperazinylacyloxyalkyl prodrugs of 2-(6-methoxy-2-naphthyl)propionic acid (naproxen) for topical drug delivery
Rautio J, Nevalainen T, Taipale H, Vepsäläinen J, Gynther J, Laine K, Järvinen T. 2000. Journal of medicinal chemistry. 43: 1489-1494
Synthesis and in vitro evaluation of aminoacyloxyalkyl esters of 2-(6-methoxy-2-naphthyl) propionic acid as novel naproxen prodrugs for dermal drug delivery
Rautio J, Nevalainen T, Taipale H, Vepsäläinen J, Gynther J, Pedersen T, Järvinen T. 1999. Pharmaceutical research. 16: 1172-1178
In vitro evaluation of acyloxyalkyl esters as dermal prodrugs of ketoprofen and naproxen
Rautio J, Taipale H, Gynther J, Vepsäläinen J, Nevalainen T, Järvinen T. 1998. Journal of pharmaceutical sciences. 87: 1622-1628
Aihiolääkkeet
Järvinen T, Rautio J, Niemi R. 1997. Duodecim. 113: 2564-2568
Voidaanko aihiolääkkeillä parantaa lääkeaineen ihonläpäisyä?
Rautio J, Taipale H, Järvinen T. 1997. Dosis. 13: 11-21

University of Eastern Finland Joensuu, Kuopio © University of Eastern Finland

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Näytä asetukset

{title} {title} {title}

Tarkenna hakuasi

Jarkko Rautio

Tutkimusryhmät

Avainsanat

A technological comparison of freeze-dried poly-ɛ-caprolactone (PCL) and poly (lactic-co-glycolic acid) (PLGA) nanoparticles loaded with clozapine for nose-to-brain delivery

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

Specific Transport of Temozolomide Does Not Override DNA Repair-mediated Chemoresistance

Altering distribution profile of palbociclib by its prodrugs

Amino Acid-Based Boron Carriers in Boron Neutron Capture Therapy (BNCT)

Development of Lyophilised Eudragit® Retard Nanoparticles for the Sustained Release of Clozapine via Intranasal Administration

Farmaseuttinen kemia

Sweet Battle of the Epimers─Continued Exploration of Monosaccharide-Derived Delivery Agents for Boron Neutron Capture Therapy

Targeting Glial Cells by Organic Anion-Transporting Polypeptide 1C1 (OATP1C1)-Utilizing l-Thyroxine-Derived Prodrugs

Tetrazine Glycoconjugate for Pretargeted Positron Emission Tomography Imaging of trans-Cyclooctene-Functionalized Molecular Spherical Nucleic Acids

Development of Sesamol Carbamate-L-Phenylalanine Prodrug Targeting L-Type Amino Acid Transporter1 (LAT1) as a Potential Antiproliferative Agent against Melanoma

In-vitro dynamic dissolution/bioconversion/permeation of fosamprenavir using a novel tool with an artificial biomimetic permeation barrier and microdialysis-sampling

Structural Features Affecting the Interactions and Transportability of LAT1-Targeted Phenylalanine Drug Conjugates

Synthesis and In Vitro Evaluation of a Set of 6-Deoxy-6-thio-carboranyl d-Glucoconjugates Shed Light on the Substrate Specificity of the GLUT1 Transporter

Molecular characteristics supporting L-Type amino acid transporter 1 (LAT1)-mediated translocation

Species differences in the intra-brain distribution of an L-type amino acid transporter 1 (LAT1) -utilizing compound between mice and rats

Addressing the biochemical foundations of a glucose-based "Trojan horse"-stradegy to boron neutron capture therephy: from chemical synthesis to in vitro assesment

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7

Exploring the Biochemical Foundations of a Successful GLUT1-Targeting Strategy to BNCT: Chemical Synthesis and In Vitro Evaluation of the Entire Positional Isomer Library of ortho-Carboranylmethyl-Bearing Glucoconjugates

Intranasal Nanoemulsions for Direct Nose-to-Brain Delivery of Actives for CNS Disorders

Prodrug Approach for Posterior Eye Drug Delivery: Synthesis of Novel Ganciclovir Prodrugs and in Vitro Screening with Cassette Dosing

Tyrosine-chlorambucil conjugates facilitate cellular uptake through L-type amino acid transporter 1 (LAT1) in human breast cancer cell line MCF-7

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6

Role of L-Type Amino Acid Transporter 1 (LAT1) for the Selective Cytotoxicity of Sesamol in Human Melanoma Cells

Aihiolääkkeet

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-4

Discovery of Polar Spirocyclic Orally Bioavailable Urea Inhibitors of Soluble Epoxide Hydrolase

Secondary carbamate linker can facilitate the sustained release of dopamine from brain-targeted prodrug

Structural properties for selective and efficient L-type amino acid transporter 1 (LAT1) mediated cellular uptake

The expanding role of prodrugs in contemporary drug design and development

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes

Breakthroughs in medicinal chemistry: New targets and mechanisms, new drugs, new hopes-2

High-accuracy mass spectrometry for identification of sulphur-containing bioactive constituents and flavonoids in extracts of Raphanus sativus var. caudatus Alef (Thai rat-tailed radish)

Prodrugs : recent approvals and a glimpse of the pipeline

Prodrugs in medicinal chemistry and enzyme prodrug therapies

Amino Acid Promoieties Alter Valproic Acid Pharmacokinetics and Enable Extended Brain Exposure

Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835

Aihiolääketeknologia lääkekehityksessä

Amino acid ester prodrugs conjugated to the alpha-carboxylic acid group do not display affinity for the L-type amino acid transporter 1 (LAT1)

Brain Pharmacokinetics of Ganciclovir in Rats with Orthotopic BT4C Glioma

Evaluation of novel imidazotetrazine analogues designed to overcome temozolomide resistance and glioblastoma regrowth

Glutathione-S-transferase selective release of metformin from its sulfonamide prodrug

Quantitative Insight into the Design of Compounds Recognized by the L-Type Amino Acid Transporter 1 (LAT1)

Convenient microwave-assisted synthesis of lipophilic sulfenamide prodrugs of metformin

Design, synthesis and brain uptake of LAT1-targeted amino acid prodrugs of dopamine

Farmaseuttinen kemia - uudet haasteet Itä-Suomen yliopistossa

LAT1-mediated prodrug uptake: a way to breach the blood-brain barrier?

Amino acids as promoieties in prodrug design and development

Design, synthesis, and evaluation of novel cyclic phosphates of 5-aminosalicylic acid as cytochrome P450-activated prodrugs

In vitro and in vivo evaluation of a sulfenamide prodrug of basic metformin

Inhibitors of LRRK2 kinase activity to probe the treatment option in Parkinson's disease

Structure-activity relationship study of compounds binding to large amino acid transporter 1 (LAT1) based on pharmacophore modeling and in situ rat brain perfusion

Aihiolääketeknologia lääkekehityksessä. [Summary: Prodrug technology in the development of medicinal agents]

Amino acid prodrugs for oral delivery: challenges and opportunities

Large amino acid transporter 1 (LAT1) prodrugs of valproic acid: new prodrug design ideas for central nervous system delivery

New Prodrug Design Ideas for Transporter-Mediated CNS Drug Delivery

New Prodrug Desing Ideas for Large Amino Acid Transporter 1 -Mediated Drug Brain Delivery

Prodrug strategies in drug design

Prodrugs - an efficient way to breach delivery and targeting barriers

Prodrugs - from serendipity to rational design

Prodrugs and Targeted Delivery: Towards Better ADME Properties

Prodrugs designed to target transporters for oral drug delivery

Brain uptake of ketoprofen-lysine prodrug in rats

Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor

Enzyme-activated prodrug strategies for targeted drug action

Determination of metformin and its prodrugs in human and rat blood by hydrophilic interaction liquid chromatography

Glucose promoiety enables glucose transporter mediated brain uptake of ketoprofen and indomethacin prodrugs in rats

The first bioreversible prodrug of metformin with improved lipophilicity and enhanced intestinal absorption

Cytochrome P450-activated prodrugs: targeted drug delivery

Diclofenac readily penetrates the cerebrospinal fluid in children

Enhanced brain drug delivery and targeting

How readily does ketorolac penetrate cerebrospinal fluid in children?

Large neutral amino acid transporter enables brain drug delivery via prodrugs