Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA) (English)
- New search for: Majer, Pavel
- New search for: Majer, Pavel
- New search for: Jančařík, Andrej
- New search for: Krečmerová, Marcela
- New search for: Tichý, Tomáš
- New search for: Tenora, Lukáš
- New search for: Wozniak, Krystyna
- New search for: Wu, Ying
- New search for: Pommier, Elie
- New search for: Ferraris, Dana
- New search for: Rais, Rana
- New search for: Slusher, Barbara S
In:
Journal of medicinal chemistry
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59
, 6
; 2810
;
2016
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ISSN:
- Article (Journal) / Print
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Title:Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA)
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Contributors:Majer, Pavel ( author ) / Jančařík, Andrej / Krečmerová, Marcela / Tichý, Tomáš / Tenora, Lukáš / Wozniak, Krystyna / Wu, Ying / Pommier, Elie / Ferraris, Dana / Rais, Rana
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Published in:Journal of medicinal chemistry ; 59, 6 ; 2810
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Publisher:
- New search for: American Chemical Society
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Place of publication:Easton, Pa.
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Publication date:2016
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 770/4230
- New search for: 44.42 / 44.42
- Further information on Basic classification
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Keywords:
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Source:
Table of contents – Volume 59, Issue 6
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 2269
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Rho Kinase (ROCK) Inhibitors and Their Therapeutic PotentialFeng, Yangbo / LoGrasso, Philip V. / Defert, Olivier / Li, Rongshi et al. | 2016
- 2301
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C‑Nucleosides To Be RevisitedDe Clercq, Erik et al. | 2016
- 2312
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How Beyond Rule of 5 Drugs and Clinical Candidates Bind to Their TargetsDoak, Bradley C. / Zheng, Jie / Dobritzsch, Doreen / Kihlberg, Jan et al. | 2016
- 2328
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Discovery of (R)‑6-(1-(8-Fluoro-6-(1-methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)‑one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor ActivityBoezio, Alessandro A. / Copeland, Katrina W. / Rex, Karen / K. Albrecht, Brian / Bauer, David / Bellon, Steven F. / Boezio, Christiane / Broome, Martin A. / Choquette, Deborah / Coxon, Angela et al. | 2016
- 2343
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MutT Homolog 1 (MTH1): The Silencing of a TargetPapeo, Gianluca et al. | 2016
- 2346
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Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell SurvivalKettle, Jason G. / Alwan, Husam / Bista, Michal / Breed, Jason / Davies, Nichola L. / Eckersley, Kay / Fillery, Shaun / Foote, Kevin M. / Goodwin, Louise / Jones, David R. et al. | 2016
- 2362
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Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosisKarabanovich, Galina / Zemanová, Júlia / Smutný, Tomáš / Székely, Rita / Šarkan, Michal / Centárová, Ivana / Vocat, Anthony / Pávková, Ivona / Čonka, Patrik / Němeček, Jan et al. | 2016
- 2381
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Conopeptide-Derived κ‑Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive PropertiesBrust, Andreas / Croker, Daniel E. / Colless, Barbara / Ragnarsson, Lotten / Andersson, Åsa / Jain, Kapil / Garcia-Caraballo, Sonia / Castro, Joel / Brierley, Stuart M / Alewood, Paul F. et al. | 2016
- 2396
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Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction SitesWong, Michael H. L. / Bryan, Holly K. / Copple, Ian M. / Jenkins, Rosalind E. / Chiu, Pak Him / Bibby, Jaclyn / Berry, Neil G. / Kitteringham, Neil R. / Goldring, Christopher E. / O’Neill, Paul M. et al. | 2016
- 2410
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Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51Gaali, Steffen / Feng, Xixi / Hähle, Andreas / Sippel, Claudia / Bracher, Andreas / Hausch, Felix et al. | 2016
- 2423
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Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of SchistosomiasisHeimburg, Tino / Chakrabarti, Alokta / Lancelot, Julien / Marek, Martin / Melesina, Jelena / Hauser, Alexander-Thomas / Shaik, Tajith B. / Duclaud, Sylvie / Robaa, Dina / Erdmann, Frank et al. | 2016
- 2436
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Discovery of a New Inhibitor of Myeloid Differentiation 2 from Cinnamamide Derivatives with Anti-Inflammatory Activity in Sepsis and Acute Lung InjuryChen, Gaozhi / Zhang, Yali / Liu, Xing / Fang, Qilu / Wang, Zhe / Fu, Lili / Liu, Zhiguo / Wang, Yi / Zhao, Yunjie / Li, Xiaokun et al. | 2016
- 2452
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Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment ScreeningBorthwick, Jennifer A. / Ancellin, Nicolas / Bertrand, Sophie M. / Bingham, Ryan P. / Carter, Paul S. / Chung, Chun-wa / Churcher, Ian / Dodic, Nerina / Fournier, Charlène / Francis, Peter L. et al. | 2016
- 2468
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Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid BiosynthesisGobbi, Silvia / Hu, Qingzhong / Zimmer, Christina / Engel, Matthias / Belluti, Federica / Rampa, Angela / Hartmann, Rolf W. / Bisi, Alessandra et al. | 2016
- 2478
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Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)Getlik, Matthäus / Smil, David / Zepeda-Velázquez, Carlos / Bolshan, Yuri / Poda, Gennady / Wu, Hong / Dong, Aiping / Kuznetsova, Ekaterina / Marcellus, Richard / Senisterra, Guillermo et al. | 2016
- 2497
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Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical PropertiesJohansson, Anders / Löfberg, Christian / Antonsson, Madeleine / von Unge, Sverker / Hayes, Martin A. / Judkins, Robert / Ploj, Karolina / Benthem, Lambertus / Lindén, Daniel / Brodin, Peter et al. | 2016
- 2512
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Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3‑Kinase (PI3K)Van Dort, Marcian E. / Hong, Hao / Wang, Hanxiao / Nino, Charles A. / Lombardi, Rachel L. / Blanks, Avery E. / Galbán, Stefanie / Ross, Brian D. et al. | 2016
- 2523
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Investigations of Enantiopure Nicotine Haptens Using an Adjuvanting Carrier in Anti-Nicotine Vaccine DevelopmentJacob, Nicholas T. / Lockner, Jonathan W. / Schlosburg, Joel E. / Ellis, Beverly A. / Eubanks, Lisa M. / Janda, Kim D. et al. | 2016
- 2530
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Repositioning Antitubercular 6‑Nitro-2,3-dihydroimidazo[2,1‑b][1,3]oxazoles for Neglected Tropical Diseases: Structure–Activity Studies on a Preclinical Candidate for Visceral LeishmaniasisThompson, Andrew M. / O’Connor, Patrick D. / Blaser, Adrian / Yardley, Vanessa / Maes, Louis / Gupta, Suman / Launay, Delphine / Martin, Denis / Franzblau, Scott G. / Wan, Baojie et al. | 2016
- 2551
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Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor AntagonistsMochizuki, Michiyo / Kori, Masakuni / Kobayashi, Katsumi / Yano, Takahiko / Sako, Yuu / Tanaka, Maiko / Kanzaki, Naoyuki / Gyorkos, Albert C. / Corrette, Christopher P. / Cho, Suk Young et al. | 2016
- 2567
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Rational Design, Synthesis, and Preliminary Structure–Activity Relationships of α‑Substituted-2-Phenylcyclopropane Carboxylic Acids as Inhibitors of Salmonella typhimurium O‑Acetylserine SulfhydrylasePieroni, Marco / Annunziato, Giannamaria / Beato, Claudia / Wouters, Randy / Benoni, Roberto / Campanini, Barbara / Pertinhez, Thelma A. / Bettati, Stefano / Mozzarelli, Andrea / Costantino, Gabriele et al. | 2016
- 2579
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Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid HydroxylaseDiaz, Philippe / Huang, Weize / Keyari, Charles M. / Buttrick, Brian / Price, Lauren / Guilloteau, Nicolas / Tripathy, Sasmita / Sperandio, Vanessa G. / Fronczek, Frank R. / Astruc-Diaz, Fanny et al. | 2016
- 2596
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Small Molecule Inhibitors of Cyclophilin D To Protect Mitochondrial Function as a Potential Treatment for Acute PancreatitisShore, Emma R. / Awais, Muhammad / Kershaw, Neil M. / Gibson, Robert R. / Pandalaneni, Sravan / Latawiec, Diane / Wen, Li / Javed, Muhammad A. / Criddle, David N. / Berry, Neil et al. | 2016
- 2612
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Development and Pharmacological Characterization of Selective Blockers of 2‑Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and PainBrindisi, Margherita / Maramai, Samuele / Gemma, Sandra / Brogi, Simone / Grillo, Alessandro / Di Cesare Mannelli, Lorenzo / Gabellieri, Emanuele / Lamponi, Stefania / Saponara, Simona / Gorelli, Beatrice et al. | 2016
- 2633
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Tuning Side Arm Electronics in Unsymmetrical Cyclotriazadisulfonamide (CADA) Endoplasmic Reticulum (ER) Translocation Inhibitors to Improve their Human Cluster of Differentiation 4 (CD4) Receptor Down-Modulating PotenciesChawla, Reena / Van Puyenbroeck, Victor / Pflug, Nicholas C. / Sama, Alekhya / Ali, Rameez / Schols, Dominique / Vermeire, Kurt / Bell, Thomas W. et al. | 2016
- 2648
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3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical EvaluationsTang, Jing / Liu, Feng / Nagy, Eva / Miller, Lena / Kirby, Karen A. / Wilson, Daniel J. / Wu, Bulan / Sarafianos, Stefan G. / Parniak, Michael A. / Wang, Zhengqiang et al. | 2016
- 2660
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Preparation and Evaluation of Radiolabeled Antibody Recruiting Small Molecules That Target Prostate-Specific Membrane Antigen for Combined Radiotherapy and ImmunotherapyGenady, Afaf R. / Janzen, Nancy / Banevicius, Laura / El-Gamal, Mahmoud / El-Zaria, Mohamed E. / Valliant, John F. et al. | 2016
- 2674
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Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular EdemaChen, Xinde / Wang, Kai / Xu, Wenwei / Ma, Quanxin / Chen, Minli / Du, Lili / Mo, Mingguang / Wang, Yiping / Shen, Jianhua et al. | 2016
- 2688
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4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA–PB1 Protein–Protein Interaction: Structure–Activity Relationships Exploration with the Aid of Molecular ModelingTrist, Iuni M. L. / Nannetti, Giulio / Tintori, Cristina / Fallacara, Anna Lucia / Deodato, Davide / Mercorelli, Beatrice / Palù, Giorgio / Wijtmans, Maikel / Gospodova, Tzveta / Edink, Ewald et al. | 2016
- 2704
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Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx‑1Murray, Justin K. / Long, Jason / Zou, Anruo / Ligutti, Joseph / Andrews, Kristin L. / Poppe, Leszek / Biswas, Kaustav / Moyer, Bryan D. / McDonough, Stefan I. / Miranda, Les P. et al. | 2016
- 2718
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Comprehensive Structure–Activity Relationship of Triantennary N‑Acetylgalactosamine Conjugated Antisense Oligonucleotides for Targeted Delivery to HepatocytesPrakash, Thazha P. / Yu, Jinghua / Migawa, Michael T. / Kinberger, Garth A. / Wan, W. Brad / Østergaard, Michael E. / Carty, Recaldo L. / Vasquez, Guillermo / Low, Audrey / Chappell, Alfred et al. | 2016
- 2734
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Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2)Kankanala, Jayakanth / Marchand, Christophe / Abdelmalak, Monica / Aihara, Hideki / Pommier, Yves / Wang, Zhengqiang et al. | 2016
- 2747
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Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N‑Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) FamilyTintori, Cristina / Brai, Annalaura / Dasso Lang, Maria Chiara / Deodato, Davide / Greco, Antonia Michela / Bizzarri, Bruno Mattia / Cascone, Lorena / Casian, Alexandru / Zamperini, Claudio / Dreassi, Elena et al. | 2016
- 2760
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Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based DesignVolgraf, Matthew / Sellers, Benjamin D. / Jiang, Yu / Wu, Guosheng / Ly, Cuong Q. / Villemure, Elisia / Pastor, Richard M. / Yuen, Po-wai / Lu, Aijun / Luo, Xifeng et al. | 2016
- 2780
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Design and Synthesis of 1‑((1,5-Bis(4-chlorophenyl)-2-methyl‑1H‑pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N‑Adamantan-2-yl‑N′‑((E)‑3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercular Agents Effective against Multidrug-Resistant MycobacteriaBhakta, Sanjib / Scalacci, Nicolò / Maitra, Arundhati / Brown, Alistair K. / Dasugari, Saiprasad / Evangelopoulos, Dimitrios / McHugh, Timothy D. / Mortazavi, Parisa N. / Twist, Alexander / Petricci, Elena et al. | 2016
- 2794
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Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo ActivitySchenkel, Laurie B. / Olivieri, Philip R. / Boezio, Alessandro A. / Deak, Holly L. / Emkey, Renee / Graceffa, Russell F. / Gunaydin, Hakan / Guzman-Perez, Angel / Lee, Josie H. / Teffera, Yohannes et al. | 2016
- 2810
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Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2‑Phosphonomethylpentanedioic Acid (2-PMPA)Majer, Pavel / Jančařík, Andrej / Krečmerová, Marcela / Tichý, Tomáš / Tenora, Lukáš / Wozniak, Krystyna / Wu, Ying / Pommier, Elie / Ferraris, Dana / Rais, Rana et al. | 2016
- 2820
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Potent and Selective Agonists of Sphingosine 1‑Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based SeriesWatterson, Scott H. / Guo, Junqing / Spergel, Steve H. / Langevine, Charles M. / Moquin, Robert V. / Shen, Ding Ren / Yarde, Melissa / Cvijic, Mary Ellen / Banas, Dana / Liu, Richard et al. | 2016
- 2841
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Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo EfficacyHansen, Steffen V. F. / Christiansen, Elisabeth / Urban, Christian / Hudson, Brian D. / Stocker, Claire J. / Due-Hansen, Maria E. / Wargent, Ed T. / Shimpukade, Bharat / Almeida, Reinaldo / Ejsing, Christer S. et al. | 2016
- 2847
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Correction to A Continuous, Fluorogenic Sirtuin 2 Deacylase Assay: Substrate Screening and Inhibitor EvaluationGalleano, Iacopo / Schiedel, Matthias / Jung, Manfred / Madsen, Andreas S. / Olsen, Christian A. et al. | 2016
- 2848
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Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case StudyHeald, Robert / Bowman, Krista K. / Bryan, Marian C. / Burdick, Daniel / Chan, Bryan / Chan, Emily / Chen, Yuan / Clausen, Saundra / Dominguez-Fernandez, Belen / Eigenbrot, Charles et al. | 2016