Search Results - "Bařinka, Cyril"
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A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging
Published in Nature communications (15-09-2021)“…Surgery is an efficient way to treat localized prostate cancer (PCa), however, it is challenging to demarcate rapidly and accurately the tumor boundary…”
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Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models
Published in Journal of medicinal chemistry (26-09-2019)“…Isoxazole is a five-membered heterocycle that is widely used in drug discovery endeavors. Here, we report the design, synthesis, and structural and biological…”
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Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor
Published in ACS medicinal chemistry letters (14-05-2020)“…Tubastatin A, a tetrahydro-γ-carboline-capped selective HDAC6 inhibitor (HDAC6i), was rationally designed 10 years ago, and has become the best investigated…”
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Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot–Marie–Tooth Type 2A Mouse Model
Published in Journal of medicinal chemistry (22-04-2021)“…Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6…”
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Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models
Published in Journal of medicinal chemistry (24-09-2020)“…Selective inhibition of histone deacetylase 6 (HDAC6) is being recognized as a therapeutic approach for cancers. In this study, we designed a new HDAC6…”
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One-Atom Substitution Enables Direct and Continuous Monitoring of Histone Deacylase Activity
Published in Biochemistry (Easton) (03-12-2019)“…We developed a one-step direct assay for the determination of histone deacylase (HDAC) activity by substituting the carbonyl oxygen of the acyl moiety with…”
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Development of 5D3-DM1: A Novel Anti-Prostate-Specific Membrane Antigen Antibody-Drug Conjugate for PSMA-Positive Prostate Cancer Therapy
Published in Molecular pharmaceutics (08-09-2020)“…Prostate cancer (PC) is a potentially high-risk disease and the most common cancer in American men. It is a leading cause of cancer-related deaths in men in…”
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Predicting Effects of Site-Directed Mutagenesis on Enzyme Kinetics by QM/MM and QM Calculations: A Case of Glutamate Carboxypeptidase II
Published in The journal of physical chemistry. B (13-01-2022)“…Quantum and molecular mechanics (QM/MM) and QM-only (cluster model) modeling techniques represent the two workhorses in mechanistic understanding of enzyme…”
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Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome
Published in ACS chemical neuroscience (20-03-2019)“…Disease-modifying therapies are needed for Fragile X Syndrome (FXS), as at present there are no effective treatments or cures. Herein, we report on a…”
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Uncovering Robust Delactoylase and Depyruvoylase Activities of HDAC Isoforms
Published in ACS chemical biology (17-06-2022)“…Zinc-dependent histone deacetylases (HDACs) and sirtuins (SIRT) represent two different classes of enzymes which are responsible for deacylation of modified…”
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Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain
Published in Journal of medicinal chemistry (28-09-2017)“…4-Carboxy-α-[3-(hydroxyamino)-3-oxopropyl]-benzenepropanoic acid 1 is a potent hydroxamate-based inhibitor of glutamate carboxypeptidase II. In an attempt to…”
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Comprehensive Mechanistic View of the Hydrolysis of Oxadiazole-Based Inhibitors by Histone Deacetylase 6 (HDAC6)
Published in ACS chemical biology (21-07-2023)“…Histone deacetylase (HDAC) inhibitors used in the clinic typically contain a hydroxamate zinc-binding group (ZBG). However, more recent work has shown that the…”
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Carboxy-terminal polyglutamylation regulates signaling and phase separation of the Dishevelled protein
Published in The EMBO journal (30-09-2024)“…Polyglutamylation is a reversible posttranslational modification that is catalyzed by enzymes of the tubulin tyrosine ligase-like (TTLL) family. Here, we found…”
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Development and therapeutic evaluation of 5D3(CC-MLN8237) 3.2 antibody-theranostic conjugates for PSMA-positive prostate cancer therapy
Published in Frontiers in pharmacology (01-05-2024)“…Prostate cancer (PC) is an aggressive cancer that can progress rapidly and eventually become castrate-resistant prostate cancer (CRPC). Stage IV metastatic…”
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The Avian Retroviral Receptor Tva Mediates the Uptake of Transcobalamin Bound Vitamin B 12 (Cobalamin)
Published in Journal of virology (01-04-2021)“…We demonstrate that the ASLV receptor Tva participates in the physiological uptake of TC-Cbl because the viral infection suppresses the uptake of Cbl and vice…”
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Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors
Published in ACS omega (26-11-2019)“…Histone deacetylase 11 (HDAC11) preferentially removes fatty acid residues from lysine side chains in a peptide or protein environment. Here, we report the…”
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Cellular Delivery of Bioorthogonal Pretargeting Therapeutics in PSMA-Positive Prostate Cancer
Published in Molecular pharmaceutics (06-01-2020)“…Prostate cancer is primarily fatal after it becomes metastatic and castration-resistant despite novel combined hormonal and chemotherapeutic regimens. Hence,…”
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Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models
Published in ACS medicinal chemistry letters (12-10-2017)“…Only a handful of therapies offer significant improvement in the overall survival in cases of melanoma, a cancer whose incidence has continued to rise in the…”
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2‑Aminoadipic Acid–C(O)–Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics
Published in ACS medicinal chemistry letters (08-11-2018)“…The design and synthesis of prostate specific membrane antigen (PSMA) ligands derived from 2-aminoadipic acid, a building block that has not previously been…”
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Structural and Biochemical Characterization of a Novel Aminopeptidase from Human Intestine
Published in The Journal of biological chemistry (01-05-2015)“…N-acetylated α-linked acidic dipeptidase-like protein (NAALADase L), encoded by the NAALADL1 gene, is a close homolog of glutamate carboxypeptidase II, a…”
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