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Items: 1 to 50 of 89

1.

Investigation of flexibility of neuraminidase 150-loop using tamiflu derivatives in influenza A viruses H1N1 and H5N1.

Zima V, Albiñana CB, Rojíková K, Pokorná J, Pachl P, Řezáčová P, Hudlicky J, Navrátil V, Majer P, Konvalinka J, Kožíšek M, Machara A.

Bioorg Med Chem. 2019 Jul 1;27(13):2935-2947. doi: 10.1016/j.bmc.2019.05.024. Epub 2019 May 17.

PMID:
31128993
2.

Tumor-Targeted Delivery of 6-Diazo-5-oxo-l-norleucine (DON) Using Substituted Acetylated Lysine Prodrugs.

Tenora L, Alt J, Dash RP, Gadiano AJ, Novotná K, Veeravalli V, Lam J, Kirkpatrick QR, Lemberg KM, Majer P, Rais R, Slusher BS.

J Med Chem. 2019 Apr 11;62(7):3524-3538. doi: 10.1021/acs.jmedchem.8b02009. Epub 2019 Mar 29.

PMID:
30892035
3.

Correction: 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.

Neuropsychopharmacology. 2019 May;44(6):1178. doi: 10.1038/s41386-019-0354-3. Epub 2019 Mar 13.

4.

The unraveling of substrate specificity of histone deacetylase 6 domains using acetylome peptide microarrays and peptide libraries.

Kutil Z, Skultetyova L, Rauh D, Meleshin M, Snajdr I, Novakova Z, Mikesova J, Pavlicek J, Hadzima M, Baranova P, Havlinova B, Majer P, Schutkowski M, Barinka C.

FASEB J. 2019 Mar;33(3):4035-4045. doi: 10.1096/fj.201801680R. Epub 2018 Nov 29.

PMID:
30496698
5.

Identification and Enantiodivergent Synthesis of (5 Z,9 S)-Tetradec-5-en-9-olide, a Queen-Specific Volatile of the Termite Silvestritermes minutus.

Machara A, Křivánek J, Dolejšová K, Havlíčková J, Bednárová L, Hanus R, Majer P, Kyjaková P.

J Nat Prod. 2018 Oct 26;81(10):2266-2274. doi: 10.1021/acs.jnatprod.8b00632. Epub 2018 Oct 9.

PMID:
30299957
6.

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.

Neuropsychopharmacology. 2019 Mar;44(4):683-694. doi: 10.1038/s41386-018-0177-7. Epub 2018 Aug 13. Erratum in: Neuropsychopharmacology. 2019 May;44(6):1178.

PMID:
30127344
7.

Metabolomic and transcriptomic data on major metabolic/biosynthetic pathways in workers and soldiers of the termite Prorhinotermes simplex (Isoptera: Rhinotermitidae) and chemical synthesis of intermediates of defensive (E)-nitropentadec-1-ene biosynthesis.

Jirošová A, Jančařík A, Menezes RC, Bazalová O, Dolejšová K, Vogel H, Jedlička P, Buček A, Brabcová J, Majer P, Hanus R, Svatoš A.

Data Brief. 2018 May 2;18:1614-1627. doi: 10.1016/j.dib.2018.04.052. eCollection 2018 Jun.

8.

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.

J Med Chem. 2018 May 10;61(9):3918-3929. doi: 10.1021/acs.jmedchem.7b01792. Epub 2018 Apr 19.

PMID:
29648826
9.

Ranking Power of the SQM/COSMO Scoring Function on Carbonic Anhydrase II-Inhibitor Complexes.

Pecina A, Brynda J, Vrzal L, Gnanasekaran R, Hořejší M, Eyrilmez SM, Řezáč J, Lepšík M, Řezáčová P, Hobza P, Majer P, Veverka V, Fanfrlík J.

Chemphyschem. 2018 Apr 5;19(7):873-879. doi: 10.1002/cphc.201701104. Epub 2018 Feb 19.

PMID:
29316128
10.

Shared CaM- and S100A1-binding epitopes in the distal TRPM4 N terminus.

Bousova K, Herman P, Vecer J, Bednarova L, Monincova L, Majer P, Vyklicky L, Vondrasek J, Teisinger J.

FEBS J. 2018 Feb;285(3):599-613. doi: 10.1111/febs.14362. Epub 2017 Dec 29.

11.

General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases.

Tichá A, Stanchev S, Vinothkumar KR, Mikles DC, Pachl P, Began J, Škerle J, Švehlová K, Nguyen MTN, Verhelst SHL, Johnson DC, Bachovchin DA, Lepšík M, Majer P, Strisovsky K.

Cell Chem Biol. 2017 Dec 21;24(12):1523-1536.e4. doi: 10.1016/j.chembiol.2017.09.007. Epub 2017 Oct 26.

12.

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.

Mol Pharm. 2017 Oct 2;14(10):3248-3257. doi: 10.1021/acs.molpharmaceut.7b00231. Epub 2017 Aug 31.

13.

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.

J Med Chem. 2017 Aug 24;60(16):7186-7198. doi: 10.1021/acs.jmedchem.7b00966. Epub 2017 Aug 14.

14.

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.

J Med Chem. 2017 Sep 28;60(18):7799-7809. doi: 10.1021/acs.jmedchem.7b00825. Epub 2017 Sep 18.

15.

ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles.

Řezníčková E, Tenora L, Pospíšilová P, Galeta J, Jorda R, Berka K, Majer P, Potáček M, Kryštof V.

Eur J Med Chem. 2017 Feb 15;127:632-642. doi: 10.1016/j.ejmech.2017.01.018. Epub 2017 Jan 12.

PMID:
28135685
16.

Co-option of the sphingolipid metabolism for the production of nitroalkene defensive chemicals in termite soldiers.

Jirošová A, Jančařík A, Menezes RC, Bazalová O, Dolejšová K, Vogel H, Jedlička P, Buček A, Brabcová J, Majer P, Hanus R, Svatoš A.

Insect Biochem Mol Biol. 2017 Mar;82:52-61. doi: 10.1016/j.ibmb.2017.01.008. Epub 2017 Jan 23.

PMID:
28126587
17.

Sensitive Versatile Fluorogenic Transmembrane Peptide Substrates for Rhomboid Intramembrane Proteases.

Tichá A, Stanchev S, Škerle J, Began J, Ingr M, Švehlová K, Polovinkin L, Růžička M, Bednárová L, Hadravová R, Poláchová E, Rampírová P, Březinová J, Kašička V, Majer P, Strisovsky K.

J Biol Chem. 2017 Feb 17;292(7):2703-2713. doi: 10.1074/jbc.M116.762849. Epub 2017 Jan 9.

18.

Integrated Activity and Genetic Profiling of Secreted Peptidases in Cryptococcus neoformans Reveals an Aspartyl Peptidase Required for Low pH Survival and Virulence.

Clarke SC, Dumesic PA, Homer CM, O'Donoghue AJ, La Greca F, Pallova L, Majer P, Madhani HD, Craik CS.

PLoS Pathog. 2016 Dec 15;12(12):e1006051. doi: 10.1371/journal.ppat.1006051. eCollection 2016 Dec.

19.

DNA-linked Inhibitor Antibody Assay (DIANA) for sensitive and selective enzyme detection and inhibitor screening.

Navrátil V, Schimer J, Tykvart J, Knedlík T, Vik V, Majer P, Konvalinka J, Šácha P.

Nucleic Acids Res. 2017 Jan 25;45(2):e10. doi: 10.1093/nar/gkw853. Epub 2016 Sep 26.

20.

Smells Like Home: Chemically Mediated Co-Habitation of Two Termite Species in a Single Nest.

Jirošová A, Sillam-Dussès D, Kyjaková P, Kalinová B, Dolejšová K, Jančařík A, Majer P, Cristaldo PF, Hanus R.

J Chem Ecol. 2016 Oct;42(10):1070-1081. Epub 2016 Sep 17.

PMID:
27639394
21.

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.

J Med Chem. 2016 Sep 22;59(18):8621-33. doi: 10.1021/acs.jmedchem.6b01069. Epub 2016 Sep 6.

PMID:
27560860
22.

Stress tolerance of transgenic barley accumulating the alfalfa aldose reductase in the cytoplasm and the chloroplast.

Nagy B, Majer P, Mihály R, Pauk J, Horváth GV.

Phytochemistry. 2016 Sep;129:14-23. doi: 10.1016/j.phytochem.2016.07.007. Epub 2016 Jul 25.

PMID:
27469099
23.

The characterization of a novel S100A1 binding site in the N-terminus of TRPM1.

Jirku M, Lansky Z, Bednarova L, Sulc M, Monincova L, Majer P, Vyklicky L, Vondrasek J, Teisinger J, Bousova K.

Int J Biochem Cell Biol. 2016 Sep;78:186-193. doi: 10.1016/j.biocel.2016.07.014. Epub 2016 Jul 17.

PMID:
27435061
24.

Still NAAG'ing After All These Years: The Continuing Pursuit of GCPII Inhibitors.

Vornov JJ, Hollinger KR, Jackson PF, Wozniak KM, Farah MH, Majer P, Rais R, Slusher BS.

Adv Pharmacol. 2016;76:215-55. doi: 10.1016/bs.apha.2016.01.007. Epub 2016 Mar 18. Review.

PMID:
27288079
25.

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.

J Med Chem. 2016 May 26;59(10):4539-50. doi: 10.1021/acs.jmedchem.5b01806. Epub 2016 Apr 25.

PMID:
27074627
26.

Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).

Majer P, Jančařík A, Krečmerová M, Tichý T, Tenora L, Wozniak K, Wu Y, Pommier E, Ferraris D, Rais R, Slusher BS.

J Med Chem. 2016 Mar 24;59(6):2810-9. doi: 10.1021/acs.jmedchem.6b00062. Epub 2016 Mar 10.

PMID:
26930119
27.

iBodies: Modular Synthetic Antibody Mimetics Based on Hydrophilic Polymers Decorated with Functional Moieties.

Šácha P, Knedlík T, Schimer J, Tykvart J, Parolek J, Navrátil V, Dvořáková P, Sedlák F, Ulbrich K, Strohalm J, Majer P, Šubr V, Konvalinka J.

Angew Chem Int Ed Engl. 2016 Feb 12;55(7):2356-60. doi: 10.1002/anie.201508642. Epub 2016 Jan 8.

28.

Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.

Tykvart J, Schimer J, Jančařík A, Bařinková J, Navrátil V, Starková J, Šrámková K, Konvalinka J, Majer P, Šácha P.

J Med Chem. 2015 May 28;58(10):4357-63. doi: 10.1021/acs.jmedchem.5b00278. Epub 2015 May 7.

PMID:
25923815
29.

The Effect of Halogen-to-Hydrogen Bond Substitution on Human Aldose Reductase Inhibition.

Fanfrlík J, Ruiz FX, Kadlčíková A, Řezáč J, Cousido-Siah A, Mitschler A, Haldar S, Lepšík M, Kolář MH, Majer P, Podjarny AD, Hobza P.

ACS Chem Biol. 2015 Jul 17;10(7):1637-42. doi: 10.1021/acschembio.5b00151. Epub 2015 May 6.

PMID:
25919404
30.

Triggering HIV polyprotein processing by light using rapid photodegradation of a tight-binding protease inhibitor.

Schimer J, Pávová M, Anders M, Pachl P, Šácha P, Cígler P, Weber J, Majer P, Řezáčová P, Kräusslich HG, Müller B, Konvalinka J.

Nat Commun. 2015 Mar 9;6:6461. doi: 10.1038/ncomms7461.

31.

Portfolio Decisions and Brain Reactions via the CEAD method.

Majer P, Mohr PN, Heekeren HR, Härdle WK.

Psychometrika. 2016 Sep;81(3):881-903. doi: 10.1007/s11336-015-9441-5. Epub 2015 Feb 11.

PMID:
25670029
32.

Substrate binding and specificity of rhomboid intramembrane protease revealed by substrate-peptide complex structures.

Zoll S, Stanchev S, Began J, Skerle J, Lepšík M, Peclinovská L, Majer P, Strisovsky K.

EMBO J. 2014 Oct 16;33(20):2408-21. doi: 10.15252/embj.201489367. Epub 2014 Sep 12.

33.

Risk patterns and correlated brain activities. Multidimensional statistical analysis of FMRI data in economic decision making study.

van Bömmel A, Song S, Majer P, Mohr PN, Heekeren HR, Härdle WK.

Psychometrika. 2014 Jul;79(3):489-514. doi: 10.1007/s11336-013-9352-2. Epub 2013 Jul 20.

PMID:
25205006
34.

Antioxidant defence in UV-irradiated tobacco leaves is centred on hydrogen-peroxide neutralization.

Majer P, Czégény G, Sándor G, Dix PJ, Hideg E.

Plant Physiol Biochem. 2014 Sep;82:239-43. doi: 10.1016/j.plaphy.2014.06.011. Epub 2014 Jun 25.

PMID:
25000557
35.

Rational design of urea-based glutamate carboxypeptidase II (GCPII) inhibitors as versatile tools for specific drug targeting and delivery.

Tykvart J, Schimer J, Bařinková J, Pachl P, Poštová-Slavětínská L, Majer P, Konvalinka J, Šácha P.

Bioorg Med Chem. 2014 Aug 1;22(15):4099-108. doi: 10.1016/j.bmc.2014.05.061. Epub 2014 Jun 5.

PMID:
24954515
36.

Sphinganine-like biogenesis of (E)-1-nitropentadec-1-ene in termite soldiers of the genus Prorhinotermes.

Jirošová A, Majer P, Jančařík A, Dolejšová K, Tykva R, Sobotník J, Jiroš P, Hanus R.

Chembiochem. 2014 Mar 3;15(4):533-6. doi: 10.1002/cbic.201300665. Epub 2014 Jan 23.

PMID:
24458870
37.

δ-Thiolactones as prodrugs of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors.

Ferraris DV, Majer P, Ni C, Slusher CE, Rais R, Wu Y, Wozniak KM, Alt J, Rojas C, Slusher BS, Tsukamoto T.

J Med Chem. 2014 Jan 9;57(1):243-7. doi: 10.1021/jm401703a. Epub 2013 Dec 27.

38.

Leaf hue measurements: a high-throughput screening of chlorophyll content.

Sass L, Majer P, Hideg E.

Methods Mol Biol. 2012;918:61-9. doi: 10.1007/978-1-61779-995-2_6.

PMID:
22893286
39.

Developmental stage is an important factor that determines the antioxidant responses of young and old grapevine leaves under UV irradiation in a green-house.

Majer P, Hideg E.

Plant Physiol Biochem. 2012 Jan;50(1):15-23. doi: 10.1016/j.plaphy.2011.09.018. Epub 2011 Oct 6.

PMID:
22099515
40.

The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.

Grella B, Adams J, Berry JF, Delahanty G, Ferraris DV, Majer P, Ni C, Shukla K, Shuler SA, Slusher BS, Stathis M, Tsukamoto T.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7222-5. doi: 10.1016/j.bmcl.2010.10.109. Epub 2010 Oct 26.

PMID:
21074428
41.

Do leaf total antioxidant capacities (TAC) reflect specific antioxidant potentials? - A comparison of TAC and reactive oxygen scavenging in tobacco leaf extracts.

Majer P, Stoyanova S, Hideg E.

J Photochem Photobiol B. 2010 Jul 2;100(1):38-43. doi: 10.1016/j.jphotobiol.2010.04.007. Epub 2010 May 6.

PMID:
20547070
42.
43.

Leaf hue measurements offer a fast, high-throughput initial screening of photosynthesis in leaves.

Majer P, Sass L, Horváth GV, Hideg E.

J Plant Physiol. 2010 Jan 1;167(1):74-6. doi: 10.1016/j.jplph.2009.06.015. Epub 2009 Jul 23.

PMID:
19631406
44.

Synthesis and biological evaluation of D-amino acid oxidase inhibitors.

Ferraris D, Duvall B, Ko YS, Thomas AG, Rojas C, Majer P, Hashimoto K, Tsukamoto T.

J Med Chem. 2008 Jun 26;51(12):3357-9. doi: 10.1021/jm800200u. Epub 2008 May 29.

PMID:
18507366
45.

Structural basis of interactions between human glutamate carboxypeptidase II and its substrate analogs.

Barinka C, Hlouchova K, Rovenska M, Majer P, Dauter M, Hin N, Ko YS, Tsukamoto T, Slusher BS, Konvalinka J, Lubkowski J.

J Mol Biol. 2008 Mar 7;376(5):1438-50. doi: 10.1016/j.jmb.2007.12.066. Epub 2008 Jan 5.

46.

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.

Barinka C, Rovenská M, Mlcochová P, Hlouchová K, Plechanovová A, Majer P, Tsukamoto T, Slusher BS, Konvalinka J, Lubkowski J.

J Med Chem. 2007 Jul 12;50(14):3267-73. Epub 2007 Jun 14.

PMID:
17567119
47.

Biochemical characterization of human glutamate carboxypeptidase III.

Hlouchová K, Barinka C, Klusák V, Sácha P, Mlcochová P, Majer P, Rulísek L, Konvalinka J.

J Neurochem. 2007 May;101(3):682-96. Epub 2007 Jan 4.

48.

Structure-based specificity mapping of secreted aspartic proteases of Candida parapsilosis, Candida albicans, and Candida tropicalis using peptidomimetic inhibitors and homology modeling.

Majer F, Pavlícková L, Majer P, Hradilek M, Dolejsí E, Hrusková-Heidingsfeldová O, Pichová I.

Biol Chem. 2006 Sep;387(9):1247-54.

PMID:
16972793
49.

Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.

Majer P, Hin B, Stoermer D, Adams J, Xu W, Duvall BR, Delahanty G, Liu Q, Stathis MJ, Wozniak KM, Slusher BS, Tsukamoto T.

J Med Chem. 2006 May 18;49(10):2876-85.

PMID:
16686531
50.

Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer.

Mesters JR, Barinka C, Li W, Tsukamoto T, Majer P, Slusher BS, Konvalinka J, Hilgenfeld R.

EMBO J. 2006 Mar 22;25(6):1375-84. Epub 2006 Feb 9.

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