P. Majer

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

B. Slusher, J. Vornov, K. Hollinger, 2016, Advances in pharmacology.

Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models

A. Bodner, G. Ghadge, R. Roos, 2003, Proceedings of the National Academy of Sciences of the United States of America.

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

K. Berka, V. Kryštof, R. Jorda, 2017, European journal of medicinal chemistry.

Design of sensitive fluorogenic substrates for human cathepsin D

J. Collins, S. Gulnik, L. Suvorov, 1997, FEBS letters.

A safe and efficient method for preparation of N,N'-unsymmetrically disubstituted ureas utilizing triphosgene

P. Majer, R. Randad, 1994 .

Unraveling the anti-influenza effect of flavonoids: Experimental validation of luteolin and its congeners as potent influenza endonuclease inhibitors.

J. Konvalinka, J. Hodek, J. Brynda, 2020, European journal of medicinal chemistry.

Post X‐ray crystallographic studies of chymosin: the existence of two structural forms and the regulation of activity by the interaction with the histidine‐proline cluster of κ‐casein

E. Gustchina, P. Majer, N. Andreeva, 1996, FEBS letters.

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

L. Vyklický, J. Vondrášek, P. Heřman, 2018, The FEBS journal.

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

L. Vyklický, J. Vondrášek, M. Sulc, 2016, The international journal of biochemistry & cell biology.

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

D. Ferraris, T. Tsukamoto, B. Slusher, 2014, Journal of medicinal chemistry.

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

D. Ferraris, T. Tsukamoto, B. Slusher, 2010, Bioorganic & medicinal chemistry letters.

Substrate specificity, inhibition and enzymological analysis of recombinant human glutamate carboxypeptidase II

J. Konvalinka, C. Bařinka, B. Slusher, 2002, Journal of neurochemistry.

Amino acids at the N- and C-termini of human glutamate carboxypeptidase II are required for enzymatic activity and proper folding.

J. Konvalinka, P. Mlcochova, C. Bařinka, 2004, European journal of biochemistry.

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

Ramachandran Gnanasekaran, J. Brynda, V. Veverka, 2018 .

Post X-ray crystallographic studies of chymosin specificity. The role of histidine-proline cluster of kappa-casein in catalytic reactions.

E. Gustchina, P. Majer, N. Andreeva, 1998, Advances in experimental medicine and biology.

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

J. Konvalinka, P. Majer, P. Šácha, 2014, Bioorganic & medicinal chemistry.

Targeting glutamine metabolism enhances tumor specific immunity by modulating suppressive myeloid cells.

M. Horton, J. Powell, S. Collins, 2020, The Journal of clinical investigation.

Targeting glutamine metabolism enhances tumor specific immunity by inhibiting the generation of MDSCs and reprogramming tumor associated macrophages

M. Horton, J. Powell, S. Collins, 2019, bioRxiv.

Re-emerging Aspartic Protease Targets: Examining Cryptococcus neoformans Major Aspartyl Peptidase 1 as a Target for Antifungal Drug Discovery

H. Madhani, C. Craik, J. Konvalinka, 2021, Journal of medicinal chemistry.

JHU-2545 Selectively Shields Salivary Glands and Kidneys during PSMA-Targeted Radiotherapy

C. Kratochwil, Marie-France Penet, D. Abou, 2018, bioRxiv.

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

Riya C. Menezes, R. Hanus, P. Jedlička, 2018, Data in brief.

Thermodynamic and structural characterization of an optimized peptide-based inhibitor of the influenza polymerase PA-PB1 subunit interaction.

J. Konvalinka, J. Hodek, J. Brynda, 2022, Antiviral research.

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

Qun Liu, T. Tsukamoto, B. Slusher, 2006, Journal of medicinal chemistry.

Facile synthesis of α-substituted acrylate esters

T. Tsukamoto, P. Majer, Bunda Hin, 2002 .

Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.

Qun Liu, T. Tsukamoto, B. Slusher, 2003, Journal of medicinal chemistry.

Mouse brain serine racemase catalyzes specific elimination of L‐serine to pyruvate

J. Konvalinka, C. Bařinka, B. Slusher, 2003, FEBS letters.

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

D. Ferraris, B. Slusher, K. Wozniak, 2016, Journal of medicinal chemistry.

Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects

B. Slusher, P. Majer, R. Rais, 2022, Frontiers in Chemistry.

Discovery of DRP-104, a tumor-targeted metabolic inhibitor prodrug

Liang Zhao, T. Seiwert, A. Pal, 2022, Science advances.

Facile Stereoselective Synthesis of γ‐Substituted γ‐Amino Acids from the Corresponding α‐Amino Acids.

E. Majerová, M. Eissenstat, P. Majer, 1998 .

Facile stereoselective synthesis of ?-substituted ?-amino acids from the corresponding ?-amino acids

E. Majerová, M. Eissenstat, P. Majer, 1997 .

Cholecystokinin analogues with alkylated carboxy terminal phenylalanine

J. Slaninová, P. Majer, L. Maletínská, 1991 .

Synthesis of methylated phenylalanines via hydrogenolysis of corresponding 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids. Synthesis and biological activity of oxytocin analogs with methylated phenylalanines in position 2.

M. Lebl, J. Slaninová, P. Majer, 2009, International journal of peptide and protein research.

Structure-activity relationship and biochemical evaluation of novel fibroblast activation protein and prolyl endopeptidase inhibitors with α-ketoamide warheads.

J. Konvalinka, J. Brynda, J. Beranová, 2021, European journal of medicinal chemistry.

Enantiospecificity of glutamate carboxypeptidase II inhibition.

T. Tsukamoto, B. Slusher, K. Wozniak, 2005, Journal of medicinal chemistry.

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

R. Hanus, J. Křivánek, L. Bednárová, 2018, Journal of natural products.

Biomimetic macrocyclic inhibitors of human cathepsin D: structure-activity relationship and binding mode analysis.

J. Brynda, M. Lepšík, P. Majer, 2020, Journal of medicinal chemistry.

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

Pavel Majer, Filip Majer, I. Pichová, 2006, Biological chemistry.

Homology modeling and SAR analysis of Schistosoma japonicum cathepsin D (SjCD) with statin inhibitors identify a unique active site steric barrier with potential for the design of specific inhibitors

Pavel Majer, Jirí Vondrásek, J. Konvalinka, 2005, Biological chemistry.

Facile stereoselective synthesis of γ-amino acids from the corresponding α-amino acids

E. Majerová, M. Eissenstat, P. Majer, 2002 .

Structure‐based subsite specificity mapping of human cathepsin D using statine‐based inhibitors

J. Collins, S. Gulnik, J. Erickson, 1997, Protein science : a publication of the Protein Society.

Engineering the substrate specificity of rhizopuspepsin: The role of Asp 77 of fungal aspartic proteinases in facilitating the cleavage of oligopeptide substrates with lysine in P1

B. Dunn, P. Majer, W. Todd Lowther, 1995, Protein science : a publication of the Protein Society.

Synthesis and biological evaluation of (R)- and (S)-2-(phosphonomethyl)pentanedioic acids as inhibitors of glutamate carboxypeptidase II

T. Tsukamoto, P. Majer, D. Vitharana, 2002 .

Unprecedented Binding Mode of Hydroxamate-Based Inhibitors of Glutamate Carboxypeptidase II: Structural Characterization and Biological Activity.

J. Vávra, C. Bařinka, D. Ferraris, 2016, Journal of medicinal chemistry.

Determination of dissociation constant of picric acid and calibration of potentiometric cell in acetone

M. Foltin, P. Majer, 1978 .

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

H. Madhani, C. Craik, P. Dumesic, 2016, PLoS pathogens.

Enhanced oral bioavailability of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) from its (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (ODOL) based prodrugs.

B. Slusher, P. Majer, R. Rais, 2019, Molecular pharmaceutics.

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

K. Ulbrich, V. Šubr, J. Konvalinka, 2016, Angewandte Chemie.

Peptide inhibitors of HIV-1 and HIV-2 proteases: a comparative study.

I. Pichová, J. Konvalinka, P. Štrop, 1997, Leukemia.

Synthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors

J. Konvalinka, J. Brynda, M. Kožíšek, 2021, International journal of molecular sciences.

Configurations of diastereomeric hydroxyethylene isosteres strongly affect biological activities of a series of specific inhibitors of human-immunodeficiency-virus proteinase.

I. Pichová, J. Konvalinka, P. Štrop, 1997, European journal of biochemistry.

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

J. Konvalinka, M. Kožíšek, P. Řezáčová, 2019, Bioorganic & medicinal chemistry.

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

M. Schutkowski, D. Rauh, C. Bařinka, 2018, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress

Yuto Hasegawa, Xiaolei Zhu, A. Kamiya, 2018, Neuropsychopharmacology.

Discovery of 6-Diazo-5-oxo-l-norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma.

A. Le, D. Ferraris, L. Monincová, 2016, Journal of medicinal chemistry.

Potency comparison of peptidomimetic inhibitors against HIV-1 and HIV-2 proteinases: design of equipotent lead compounds.

I. Pichová, J. Urban, J. Konvalinka, 1997, Archives of biochemistry and biophysics.

Mapping of CaM, S100A1 and PIP2-Binding Epitopes in the Intracellular N- and C-Termini of TRPM4

J. Vondrášek, I. Barvík, P. Heřman, 2020, International journal of molecular sciences.

N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs.

G. Riggins, J. Vávra, L. Monincová, 2018, Journal of medicinal chemistry.

The Novel Glutamine Antagonist Prodrug JHU395 Has Antitumor Activity in Malignant Peripheral Nerve Sheath Tumor

C. Brayton, J. Blakeley, K. Lemberg, 2019, Molecular Cancer Therapeutics.

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

K. Lemberg, K. Novotná, B. Slusher, 2019, Journal of medicinal chemistry.

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.

D. Volsky, W. Chao, G. Brandacher, 2017, Journal of medicinal chemistry.

Structure and inhibition of plasmepsin II, a hemoglobin-degrading enzyme from P. Falciparum

Jack R. Collins, Pavel Majer, Raul E. Cachau, 1996 .

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

J. Konvalinka, P. Majer, P. Šácha, 2016, Nucleic acids research.

Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells

A. Kozikowski, C. Bařinka, P. Majer, 2023, International journal of molecular sciences.

High-affinity Near-infrared Fluorescent Small-molecule Contrast Agents for In Vivo Imaging of Prostate-specific Membrane Antigen

Takashi Tsukamoto, John V. Frangioni, Pavel Majer, 2005, Molecular imaging.

An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study.

Pavel Majer, Jan Dohnálek, Tereza Skálová, 2003, Journal of medicinal chemistry.

Glutamate carboxypeptidase II inhibition as a novel therapeutic target.

T. Tsukamoto, B. Slusher, J. Vornov, 2003, Advances in experimental medicine and biology.

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

J. Konvalinka, J. Lubkowski, P. Mlcochova, 2007, Journal of medicinal chemistry.

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

J. Konvalinka, J. Lubkowski, M. Dauter, 2008, Journal of molecular biology.

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

J. Konvalinka, R. Hilgenfeld, J. Mesters, 2006, The EMBO journal.

Rational design and synthesis of conformationally constrained inhibitors of human cathepsin D

J. Collins, S. Gulnik, J. Erickson, 2002 .

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

Riya C. Menezes, R. Hanus, P. Jedlička, 2017, Insect biochemistry and molecular biology.

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

J. Konvalinka, H. Kräusslich, B. Müller, 2015, Nature Communications.

Chemical Blockage of the Mitochondrial Rhomboid Protease PARL by Novel Ketoamide Inhibitors Reveals Its Role in PINK1/Parkin-Dependent Mitophagy

T. Langer, P. Majer, M. K. Lemberg, 2022, Journal of medicinal chemistry.

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

David C. Mikles, K. Vinothkumar, M. Lepšík, 2017, Cell chemical biology.

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

Martin Lepšík, Pavel Majer, M. Lepšík, 2014, The EMBO journal.

Sensitive Versatile Fluorogenic Transmembrane Peptide Substrates for Rhomboid Intramembrane Proteases*

J. Březinová, Kateřina Švehlová, L. Bednárová, 2017, The Journal of Biological Chemistry.

Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs.

B. Slusher, K. Hollinger, K. Wozniak, 2017, Molecular pharmaceutics.

Facile synthesis of alpha-substituted acrylate esters.

T. Tsukamoto, P. Majer, Bunda Hin, 2002, Journal of Organic Chemistry.

Biochemical characterization of human glutamate carboxypeptidase III

J. Konvalinka, P. Mlcochova, L. Rulíšek, 2006, Journal of neurochemistry.

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

J. Konvalinka, P. Majer, P. Šácha, 2015, Journal of medicinal chemistry.

Plasmodium falciparum, P. vivax, and P. malariae: a comparison of the active site properties of plasmepsins cloned and expressed from three different species of the malaria parasite.

J. Dame, C. Yowell, B. Dunn, 1997, Experimental parasitology.

Specificity mapping of HIV-1 protease by reduced bond inhibitors.

J. Urban, J. Konvalinka, P. Štrop, 1993, Archives of biochemistry and biophysics.

Reduced‐bond tight‐binding inhibitors of HIV‐1 protease Fine tuning of the enzyme subsite specificity

J. Urban, J. Konvalinka, P. Štrop, 1992, FEBS letters.

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

K. Hashimoto, D. Ferraris, T. Tsukamoto, 2008, Journal of medicinal chemistry.

Comprehensive Mechanistic View of the Hydrolysis of Oxadiazole-Based Inhibitors by Histone Deacetylase 6 (HDAC6)

M. Schutkowski, A. Kozikowski, L. Rulíšek, 2023, ACS chemical biology.

The combination of immunotherapy and a glutamine metabolism inhibitor represents an effective therapeutic strategy for advanced and metastatic murine pancreatic adenocarcinoma.

K. Pacak, J. Ženka, J. Chmelař, 2023, International immunopharmacology.

Selectivity in inhibition of proteolytic enzymes from Plasmodium falciparum

J. Dame, B. Dunn, J. Erickson, 2002 .

Topical SCD-153, a 4-methyl itaconate prodrug, for the treatment of alopecia areata

B. Slusher, P. Majer, R. Rais, 2022, PNAS nexus.

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

R. Hanus, P. F. Cristaldo, D. Sillam-Dussès, 2016, Journal of Chemical Ecology.

Design, synthesis, and resistance patterns of MP-134 and MP-167, two novel inhibitors of HIV type 1 protease.

D. Ho, M. Markowitz, S. Gulnik, 1996, AIDS research and human retroviruses.

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

Martin Lepšík, Jindřich Fanfrlík, Pavel Hobza, 2015, ACS chemical biology.

Unique peptidic agonists of a juvenile hormone receptor with species-specific effects on insect development and reproduction

R. Tuma, P. Jedlička, D. Řeha, 2022, Proceedings of the National Academy of Sciences of the United States of America.

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

Ramachandran Gnanasekaran, J. Brynda, V. Veverka, 2018, Chemphyschem : a European journal of chemical physics and physical chemistry.

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

J. Konvalinka, P. Majer, P. Šácha, 2015, Journal of medicinal chemistry.

A gut-restricted glutamate carboxypeptidase II inhibitor reduces monocytic inflammation and improves preclinical colitis

B. Slusher, P. Majer, R. Rais, 2023, Science Translational Medicine.

Pro-905, a Novel Purine Antimetabolite, Combines with Glutamine Amidotransferase Inhibition to Suppress Growth of Malignant Peripheral Nerve Sheath Tumor

Liang Zhao, C. Pratilas, J. Asara, 2023, Molecular cancer therapeutics.

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

J. Konvalinka, H. Kräusslich, B. Müller, 2015, Nature Communications.

Formation of gadolinium–ferritin from clinical magnetic resonance contrast agents

A. Rulseh, J. Vymazal, J. Tarábek, 2020, Nanoscale advances.

Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain.

J. Vávra, C. Bařinka, T. Tsukamoto, 2017, Journal of medicinal chemistry.

Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs.

B. Slusher, K. Wozniak, P. Majer, 2017, Molecular pharmaceutics.