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Discovery of tert-Butyl Ester Based 6-Diazo-5-oxo-l-norleucine Prodrugs for Enhanced Metabolic Stability and Tumor Delivery.
Novotná K, Tenora L, Prchalová E, Paule J, Alt J, Veeravalli V, Lam J, Wu Y, Šnajdr I, Gori S, Mettu VS, Tsukamoto T, Majer P, Slusher BS, Rais R. Novotná K, et al. Among authors: majer p. J Med Chem. 2023 Nov 23;66(22):15493-15510. doi: 10.1021/acs.jmedchem.3c01681. Epub 2023 Nov 10. J Med Chem. 2023. PMID: 37949450 Free PMC article.
Discovery of 6-Diazo-5-oxo-l-norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma.
Rais R, Jančařík A, Tenora L, Nedelcovych M, Alt J, Englert J, Rojas C, Le A, Elgogary A, Tan J, Monincová L, Pate K, Adams R, Ferraris D, Powell J, Majer P, Slusher BS. Rais R, et al. Among authors: majer p. J Med Chem. 2016 Sep 22;59(18):8621-33. doi: 10.1021/acs.jmedchem.6b01069. Epub 2016 Sep 6. J Med Chem. 2016. PMID: 27560860
Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain.
Rais R, Vávra J, Tichý T, Dash RP, Gadiano AJ, Tenora L, Monincová L, Bařinka C, Alt J, Zimmermann SC, Slusher CE, Wu Y, Wozniak K, Majer P, Tsukamoto T, Slusher BS. Rais R, et al. Among authors: majer p. J Med Chem. 2017 Sep 28;60(18):7799-7809. doi: 10.1021/acs.jmedchem.7b00825. Epub 2017 Sep 18. J Med Chem. 2017. PMID: 28759215 Free PMC article.
N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.
Nedelcovych MT, Tenora L, Kim BH, Kelschenbach J, Chao W, Hadas E, Jančařík A, Prchalová E, Zimmermann SC, Dash RP, Gadiano AJ, Garrett C, Furtmüller G, Oh B, Brandacher G, Alt J, Majer P, Volsky DJ, Rais R, Slusher BS. Nedelcovych MT, et al. Among authors: majer p. J Med Chem. 2017 Aug 24;60(16):7186-7198. doi: 10.1021/acs.jmedchem.7b00966. Epub 2017 Aug 14. J Med Chem. 2017. PMID: 28759224 Free PMC article.
N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs.
Zimmermann SC, Tichý T, Vávra J, Dash RP, Slusher CE, Gadiano AJ, Wu Y, Jančařík A, Tenora L, Monincová L, Prchalová E, Riggins GJ, Majer P, Slusher BS, Rais R. Zimmermann SC, et al. Among authors: majer p. J Med Chem. 2018 May 10;61(9):3918-3929. doi: 10.1021/acs.jmedchem.7b01792. Epub 2018 Apr 19. J Med Chem. 2018. PMID: 29648826
Unprecedented Binding Mode of Hydroxamate-Based Inhibitors of Glutamate Carboxypeptidase II: Structural Characterization and Biological Activity.
Novakova Z, Wozniak K, Jancarik A, Rais R, Wu Y, Pavlicek J, Ferraris D, Havlinova B, Ptacek J, Vavra J, Hin N, Rojas C, Majer P, Slusher BS, Tsukamoto T, Barinka C. Novakova Z, et al. Among authors: majer p. J Med Chem. 2016 May 26;59(10):4539-50. doi: 10.1021/acs.jmedchem.5b01806. Epub 2016 Apr 25. J Med Chem. 2016. PMID: 27074627
Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs.
Nedelcovych M, Dash RP, Tenora L, Zimmermann SC, Gadiano AJ, Garrett C, Alt J, Hollinger KR, Pommier E, Jančařík A, Rojas C, Thomas AG, Wu Y, Wozniak K, Majer P, Slusher BS, Rais R. Nedelcovych M, et al. Among authors: majer p. Mol Pharm. 2017 Oct 2;14(10):3248-3257. doi: 10.1021/acs.molpharmaceut.7b00231. Epub 2017 Aug 31. Mol Pharm. 2017. PMID: 28763226 Free PMC article.
JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.
Zhu X, Nedelcovych MT, Thomas AG, Hasegawa Y, Moreno-Megui A, Coomer W, Vohra V, Saito A, Perez G, Wu Y, Alt J, Prchalova E, Tenora L, Majer P, Rais R, Rojas C, Slusher BS, Kamiya A. Zhu X, et al. Among authors: majer p. Neuropsychopharmacology. 2019 Mar;44(4):683-694. doi: 10.1038/s41386-018-0177-7. Epub 2018 Aug 13. Neuropsychopharmacology. 2019. PMID: 30127344 Free PMC article.
116 results