List of works - Cyril Barinka

2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics

scientific article published on 24 October 2018

A high-affinity [(18)F]-labeled phosphoramidate peptidomimetic PSMA-targeted inhibitor for PET imaging of prostate cancer

scientific article

A high-resolution structure of ligand-free human glutamate carboxypeptidase II

scientific article

A picomolar inhibitor of resistant strains of human immunodeficiency virus protease identified by a combinatorial approach.

scientific article

A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging

scientific article published in 2021

A remote arene-binding site on prostate specific membrane antigen revealed by antibody-recruiting small molecules

scientific article

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

scientific article

Biochemical characterization of human glutamate carboxypeptidase III

scientific article

Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure–activity relationship studies

scientific article

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome

scientific article published on 14 December 2018

Calcium-Driven Folding of RTX Domain β-Rolls Ratchets Translocation of RTX Proteins through Type I Secretion Ducts

scientific article

Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization.

scientific article published on 26 September 2015

Cellular Delivery of Bioorthogonal Pretargeting Therapeutics in PSMA-Positive Prostate Cancer

scientific article published on 16 December 2019

Comparative analysis of monoclonal antibodies against prostate-specific membrane antigen (PSMA).

scientific article

Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.

scientific article published on 7 April 2017

Design of composite inhibitors targeting glutamate carboxypeptidase II: the importance of effector functionalities

scientific article

Development of 5D3-DM1: A Novel Anti-Prostate-Specific Membrane Antigen Antibody-Drug Conjugate for PSMA-Positive Prostate Cancer Therapy

scientific article published on 17 August 2020

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

scientific article published on 17 July 2019

Development of a High-Throughput Fluorescence Polarization Assay to Identify Novel Ligands of Glutamate Carboxypeptidase II ⬇️

scientific article published on June 29, 2012

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models

scientific article published on 04 September 2019

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

scientific article published on 31 July 2017

Efficient and versatile one-step affinity purification of in vivo biotinylated proteins: Expression, characterization and structure analysis of recombinant human glutamate carboxypeptidase II

scientific article

Engineered Fragments of the PSMA-Specific 5D3 Antibody and Their Functional Characterization

scientific article published on 12 September 2020

Evaluation of 111In-DOTA-5D3, a Surrogate SPECT Imaging Agent for Radioimmunotherapy of Prostate-Specific Membrane Antigen

scientific article published on 20 September 2018

Glu-Ureido-Based Inhibitors of Prostate-Specific Membrane Antigen: Lessons Learned During the Development of a Novel Class of Low-Molecular-Weight Theranostic Radiotracers

scientific article published in September 2017

Glutamate Carboxypeptidase II in Diagnosis and Treatment of Neurologic Disorders and Prostate Cancer ⬇️

scientific article published on January 1, 2012

Histone Deacetylase 11 Is a Fatty-Acid Deacylase

scientific article published on 16 January 2018

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.

scientific article published in April 2005

Human histone deacetylase 6 shows strong preference for tubulin dimers over assembled microtubules

scientific article

Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity

scientific article

Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization

scientific article

In‐solution structure and oligomerization of human histone deacetylase 6 – an integrative approach

scientific article published in 2022

Mapping of the active site of glutamate carboxypeptidase II by site-directed mutagenesis

scientific article published on 21 August 2007

Mitochondria-adaptor TRAK1 promotes kinesin-1 driven transport in crowded environments

scientific article published on 19 June 2020

Molecular Design of <sup>68</sup>Ga- and <sup>89</sup>Zr-Labeled Anticalin Radioligands for PET-Imaging of PSMA-Positive Tumors

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

scientific article (publication date: 30 January 2003)

Novel Monoclonal Antibodies Recognizing Human Prostate-Specific Membrane Antigen (PSMA) as Research and Theranostic Tools.

scientific article published in March 2017

Novel β- and γ-Amino Acid-Derived Inhibitors of Prostate-Specific Membrane Antigen

scientific article published on 09 March 2020

One-Atom Substitution Enables Direct and Continuous Monitoring of Histone Deacylase Activity

scientific article published on 14 November 2019

Prostate-specific membrane antigen (PSMA)-mediated laminin proteolysis generates a pro-angiogenic peptide

scientific article published on 8 July 2016

Reaction mechanism of glutamate carboxypeptidase II revealed by mutagenesis, X-ray crystallography, and computational methods

scientific article

Resonance Assignment and Three-Dimensional Structure Determination of a Human α-Defensin, HNP-1, by Solid-State NMR

scientific article

Selection and characterization of Anticalins targeting human prostate-specific membrane antigen (PSMA).

scientific article published on 21 January 2016

Structural Basis of Interactions between Human Glutamate Carboxypeptidase II and Its Substrate Analogs

scientific article

Structural and biochemical characterization of a novel aminopeptidase from human intestine

scientific article published on 9 March 2015

Structural and biochemical characterization of the folyl-poly-γ-l-glutamate hydrolyzing activity of human glutamate carboxypeptidase II

scientific article

Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors

scientific article published on 14 November 2018

Structural basis of interaction between urokinase-type plasminogen activator and its receptor

scientific article

Structural characterization of P1′-diversified urea-based inhibitors of glutamate carboxypeptidase II

scientific article

Structural insight into the evolutionary and pharmacologic homology of glutamate carboxypeptidases II and III

scientific article

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II

scientific article

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

scientific article

Structure of human monocyte chemoattractant protein 4 (MCP-4/CCL13)

scientific article

Structure-Activity Relationship of (18)F-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer

scientific article published on 13 June 2016

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

scientific article published in February 2002

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models

scientific article published on 5 September 2017

The calcium-binding site of human glutamate carboxypeptidase II is critical for dimerization, thermal stability, and enzymatic activity

scientific article published on 01 September 2018

The disordered N-terminus of HDAC6 is a microtubule-binding domain critical for efficient tubulin deacetylation

scientific article published on 17 January 2020

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

scientific article published on 29 November 2018

Tissue expression and enzymologic characterization of human prostate specific membrane antigen and its rat and pig orthologs

scientific article published on 01 February 2008

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

scientific article

List of works by Cyril Barinka

2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics

A high-affinity [(18)F]-labeled phosphoramidate peptidomimetic PSMA-targeted inhibitor for PET imaging of prostate cancer

A high-resolution structure of ligand-free human glutamate carboxypeptidase II

A picomolar inhibitor of resistant strains of human immunodeficiency virus protease identified by a combinatorial approach.

A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging

A remote arene-binding site on prostate specific membrane antigen revealed by antibody-recruiting small molecules

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

Biochemical characterization of human glutamate carboxypeptidase III

Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure–activity relationship studies

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome

Calcium-Driven Folding of RTX Domain β-Rolls Ratchets Translocation of RTX Proteins through Type I Secretion Ducts

Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization.

Cellular Delivery of Bioorthogonal Pretargeting Therapeutics in PSMA-Positive Prostate Cancer

Comparative analysis of monoclonal antibodies against prostate-specific membrane antigen (PSMA).

Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.

Design of composite inhibitors targeting glutamate carboxypeptidase II: the importance of effector functionalities

Development of 5D3-DM1: A Novel Anti-Prostate-Specific Membrane Antigen Antibody-Drug Conjugate for PSMA-Positive Prostate Cancer Therapy

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

Development of a High-Throughput Fluorescence Polarization Assay to Identify Novel Ligands of Glutamate Carboxypeptidase II ⬇️

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models

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

Efficient and versatile one-step affinity purification of in vivo biotinylated proteins: Expression, characterization and structure analysis of recombinant human glutamate carboxypeptidase II

Engineered Fragments of the PSMA-Specific 5D3 Antibody and Their Functional Characterization

Evaluation of 111In-DOTA-5D3, a Surrogate SPECT Imaging Agent for Radioimmunotherapy of Prostate-Specific Membrane Antigen

Glu-Ureido-Based Inhibitors of Prostate-Specific Membrane Antigen: Lessons Learned During the Development of a Novel Class of Low-Molecular-Weight Theranostic Radiotracers

Glutamate Carboxypeptidase II in Diagnosis and Treatment of Neurologic Disorders and Prostate Cancer ⬇️

Histone Deacetylase 11 Is a Fatty-Acid Deacylase

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.

Human histone deacetylase 6 shows strong preference for tubulin dimers over assembled microtubules

Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity

Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization

In‐solution structure and oligomerization of human histone deacetylase 6 – an integrative approach

Mapping of the active site of glutamate carboxypeptidase II by site-directed mutagenesis

Mitochondria-adaptor TRAK1 promotes kinesin-1 driven transport in crowded environments

Molecular Design of <sup>68</sup>Ga- and <sup>89</sup>Zr-Labeled Anticalin Radioligands for PET-Imaging of PSMA-Positive Tumors

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

Novel Monoclonal Antibodies Recognizing Human Prostate-Specific Membrane Antigen (PSMA) as Research and Theranostic Tools.

Novel β- and γ-Amino Acid-Derived Inhibitors of Prostate-Specific Membrane Antigen

One-Atom Substitution Enables Direct and Continuous Monitoring of Histone Deacylase Activity

Prostate-specific membrane antigen (PSMA)-mediated laminin proteolysis generates a pro-angiogenic peptide

Reaction mechanism of glutamate carboxypeptidase II revealed by mutagenesis, X-ray crystallography, and computational methods

Resonance Assignment and Three-Dimensional Structure Determination of a Human α-Defensin, HNP-1, by Solid-State NMR

Selection and characterization of Anticalins targeting human prostate-specific membrane antigen (PSMA).

Structural Basis of Interactions between Human Glutamate Carboxypeptidase II and Its Substrate Analogs

Structural and biochemical characterization of a novel aminopeptidase from human intestine

Structural and biochemical characterization of the folyl-poly-γ-l-glutamate hydrolyzing activity of human glutamate carboxypeptidase II

Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors

Structural basis of interaction between urokinase-type plasminogen activator and its receptor

Structural characterization of P1′-diversified urea-based inhibitors of glutamate carboxypeptidase II

Structural insight into the evolutionary and pharmacologic homology of glutamate carboxypeptidases II and III

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II

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

Structure of human monocyte chemoattractant protein 4 (MCP-4/CCL13)

Structure-Activity Relationship of (18)F-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer

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

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models

The calcium-binding site of human glutamate carboxypeptidase II is critical for dimerization, thermal stability, and enzymatic activity

The disordered N-terminus of HDAC6 is a microtubule-binding domain critical for efficient tubulin deacetylation

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

Tissue expression and enzymologic characterization of human prostate specific membrane antigen and its rat and pig orthologs

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