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List of works by Jan Konvalinka

A Reliable Docking/Scoring Scheme Based on the Semiempirical Quantum Mechanical PM6-DH2 Method Accurately Covering Dispersion and H-Bonding: HIV-1 Protease with 22 Ligands

article

A distinct binding mode of a hydroxyethylamine isostere inhibitor of HIV-1 protease

scientific article

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

scientific article

A modular approach to HIV-1 proteinase inhibitor design

scientific article published on May 1996

A novel PSMA/GCPII-deficient mouse model shows enlarged seminal vesicles upon aging

scientific article published on 05 September 2018

A novel substrate-based HIV-1 protease inhibitor drug resistance mechanism

scientific article

A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.

scientific article published in April 2004

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

scientific article

A possible regulation of negative factor (Nef) activity of human immunodeficiency virus type 1 by the viral protease.

scientific article published in July 1994

Active foamy virus proteinase is essential for virus infectivity but not for formation of a Pol polyprotein

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

An active-site mutation in the human immunodeficiency virus type 1 proteinase (PR) causes reduced PR activity and loss of PR-mediated cytotoxicity without apparent effect on virus maturation and infectivity

scientific article published on November 1995

An engineered retroviral proteinase from myeloblastosis associated virus acquires pH dependence and substrate specificity of the HIV-1 proteinase

scientific article published on March 1992

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

scientific article (publication date: 24 April 2003)

Anomalous adsorptive properties of HIV protease: Indication of two-dimensional crystallization?

article

Biochemical characterization of human glutamate carboxypeptidase III

scientific article

Capillary electrophoresis method for determination of D-serine and its application for monitoring of serine racemase activity

scientific article published in July 2006

Capturing a dynamically interacting inhibitor by paramagnetic NMR spectroscopy

scientific article published on 01 March 2019

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

scientific article

Comparison of human glutamate carboxypeptidases II and III reveals their divergent substrate specificities

scientific article

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

scientific article published on December 1997

Correction: MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

scientific article published on 16 October 2019

Current and Novel Inhibitors of HIV Protease

scientific article

Czech bibliometric system fosters mediocre research

scientific article published in Nature

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

scientific article published on 26 September 2016

DNA-linked inhibitor antibody assay (DIANA) as a new method for screening influenza neuraminidase inhibitors

scientific article published in 2018

Derivatization chemistry of the double-decker dicobalt sandwich ion targeted to design biologically active substances

Design of HIV protease inhibitors based on inorganic polyhedral metallacarboranes

scientific article

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

scientific article

Detection and quantitation of glutamate carboxypeptidase II in human blood.

scientific article published on 20 March 2014

Determining and overcoming resistance to HIV protease inhibitors.

scientific article published on June 2004

Different requirements for productive interaction between the active site of HIV-1 proteinase and substrates containing -hydrophobic*hydrophobic- or -aromatic*pro- cleavage sites

scientific article published in June 1992

Dual substrate and reaction specificity in mouse serine racemase: identification of high-affinity dicarboxylate substrate and inhibitors and analysis of the beta-eliminase activity

scientific article published in October 2005

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

Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir

scientific article

Exploiting the unique features of Zika and Dengue proteases for inhibitor design

scientific article published on 09 May 2019

Expression and distribution of 'high affinity' glutamate transporters GLT1, GLAST, EAAC1 and of GCPII in the rat peripheral nervous system

scientific article published in November 2008

From nonpeptide toward noncarbon protease inhibitors: metallacarboranes as specific and potent inhibitors of HIV protease

scientific article

GCPII and its close homolog GCPIII: from a neuropeptidase to a cancer marker and beyond

scientific article published on 01 March 2019

GCPII variants, paralogs and orthologs.

scientific article published on January 2012

GS-8374, a Prototype Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits Protease Mutants with Amino Acid Insertions

scientific article

Glutamate carboxypeptidase II does not process amyloid-β peptide.

scientific article published on 23 March 2013

HIV-1 Protease Mutations and Inhibitor Modifications Monitored on a Series of Complexes. Structural Basis for the Effect of the A71V Mutation on the Active Site†

scientific article published on 01 September 2006

HIV-1 protease inhibitor mutations affect the development of HIV-1 resistance to the maturation inhibitor bevirimat.

scientific article published on 24 August 2011

High-level expression of enzymatically active bovine leukemia virus proteinase in E. coli

scientific article published in August 1991

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 DNA-Damage-Inducible 2 Protein Is Structurally and Functionally Distinct from Its Yeast Ortholog.

scientific article

Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.

scientific article published in October 2009

Hydroxyethylamine isostere of an HIV-1 protease inhibitor prefers its amine to the hydroxy group in binding to catalytic aspartates. A synchrotron study of HIV-1 protease in complex with a peptidomimetic inhibitor

scientific article

Identification of Novel Carbonic Anhydrase IX Inhibitors Using High-Throughput Screening of Pooled Compound Libraries by DNA-Linked Inhibitor Antibody Assay (DIANA)

scientific article published on 26 May 2020

Identification of Protein Targets of Bioactive Small Molecules Using Randomly Photomodified Probes

scientific article published on 07 December 2018

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

scientific article

Induced maturation of human immunodeficiency virus.

scientific article published on 17 September 2014

Inhibition of the precursor and mature forms of HIV-1 protease as a tool for drug evaluation.

scientific article published on 11 July 2018

Inhibitor and substrate binding induced stability of HIV-1 protease against sequential dissociation and unfolding revealed by high pressure spectroscopy and kinetics

scientific article

Inhibitor binding at the protein interface in crystals of a HIV-1 protease complex

article

Inhibitor-Decorated Polymer Conjugates Targeting Fibroblast Activation Protein

scientific article published on 27 September 2017

Inhibitor-GCPII interaction: selective and robust system for targeting cancer cells with structurally diverse nanoparticles.

scientific article published in February 2018

Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance

scientific article published on 4 July 2008

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

scientific article published on 17 May 2019

Ion specific effects of alkali cations on the catalytic activity of HIV-1 protease

scientific article published on January 2013

Ion specific effects of sodium and potassium on the catalytic activity of HIV-1 protease

article

Kinetic, Thermodynamic, and Structural Analysis of Drug Resistance Mutations in Neuraminidase from the 2009 Pandemic Influenza Virus

scientific article published on 21 June 2018

Kinetic, thermodynamic and structural analysis of tamiphosphor binding to neuraminidase of H1N1 (2009) pandemic influenza

scientific article

Kinetics of the dimerization of retroviral proteases: the "fireman's grip" and dimerization.

scientific article published on October 2003

Label-free determination of prostate specific membrane antigen in human whole blood at nanomolar levels by magnetically assisted surface enhanced Raman spectroscopy

scientific article published on 17 October 2017

MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

scientific article published on 16 September 2019

Malonate-based inhibitors of mammalian serine racemase: kinetic characterization and structure-based computational study.

scientific article published on 16 October 2014

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

scientific article published on 21 August 2007

Molecular Characterization of Clinical Isolates of Human Immunodeficiency Virus Resistant to the Protease Inhibitor Darunavir

scientific article

Molecular analysis of the HIV-1 resistance development: enzymatic activities, crystal structures, and thermodynamics of nelfinavir-resistant HIV protease mutants

scientific article

Molecular recognition of fibroblast activation protein for diagnostic and therapeutic applications

scientific article published on 06 April 2020

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

scientific article (publication date: 30 January 2003)

Mouse glutamate carboxypeptidase II (GCPII) has a similar enzyme activity and inhibition profile but a different tissue distribution to human GCPII.

scientific article published on 29 August 2017

Mutations in HIV-1 gag and pol Compensate for the Loss of Viral Fitness Caused by a Highly Mutated Protease

scientific article

Ninety-Nine Is Not Enough: Molecular Characterization of Inhibitor-Resistant Human Immunodeficiency Virus Type 1 Protease Mutants with Insertions in the Flap Region

scientific article

Non-infectious fluorimetric assay for phenotyping of drug-resistant HIV proteinase mutants

scientific article published on 9 March 2006

Novel Substrate-Based Inhibitors of Human Glutamate Carboxypeptidase II with Enhanced Lipophilicity

scientific article

On the role of theRconfiguration of the reaction-intermediate isostere in HIV-1 protease-inhibitor binding: X-ray structure at 2.0 Å resolution

article

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

scientific article

Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies

article

Prostate-specific membrane antigen and its truncated form PSM'.

scientific article

Protein-Engineered Proteinase of Myeloblastosis Associated Virus, An Enzyme of High Activity and HIV-1 Proteinase-Like Specificity ⬇️

scientific article published on January 1, 1991

Proteolytic Processing of Particle-Associated Retroviral Polyproteins by Homologous and Heterologous Viral Proteinases

scientific article published on 01 February 1995

Random mutagenesis of human serine racemase reveals residues important for the enzymatic activity

Random protein sequences can form defined secondary structures and are well-tolerated in vivo.

scientific article published on 13 November 2017

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

scientific article

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

scientific article published on 18 May 2021

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

scientific article

Recombinant human serine racemase: enzymologic characterization and comparison with its mouse ortholog

scientific article

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

scientific article published on February 1992

Response of HIV positive patients to the long-term salvage therapy by lopinavir/ritonavir

scientific article published in August 2005

Retroviral proteases and their roles in virion maturation

scientific article published on 26 March 2015

Role of hydroxyl group and R/S configuration of isostere in binding properties of HIV-1 protease inhibitors.

scientific article published in November 2004

Sensitive, soluble chromogenic substrates for HIV-1 proteinase

scientific article

Simian Immunodeficiency Virus Retropepsin

article published in 2013

Specific Inhibitors of HIV Capsid Assembly Binding to the C-Terminal Domain of the Capsid Protein: Evaluation of 2-Arylquinazolines as Potential Antiviral Compounds.

scientific article published on 21 December 2015

Specific cleavage sites of Nef proteins from human immunodeficiency virus types 1 and 2 for the viral proteases

scientific article

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

scientific article published on July 1993

Specificity studies on retroviral proteinase from myeloblastosis-associated virus

scientific article published in April 1991

Spumapepsins

scholarly article

Stimulated Emission Depletion Nanoscopy Reveals Time-Course of Human Immunodeficiency Virus Proteolytic Maturation

scientific article

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 characterization of the interaction between the C-terminal domain of the influenza polymerase PA subunit and an optimized small peptide inhibitor

scientific article published on 06 November 2020

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

Structural studies of the yeast DNA damage-inducible protein Ddi1 reveal domain architecture of this eukaryotic protein family.

scientific article published on 20 September 2016

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

scientific article

Structure-aided design of novel inhibitors of HIV protease based on a benzodiazepine scaffold.

scientific article

Sub-site preferences of the aspartic proteinase from the human immunodeficiency virus, HIV-1.

scientific article published in July 1990

Subsite specificity of the proteinase from myeloblastosis associated virus

scientific article published in April 1991

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

scientific article published in February 2002

Synthesis and application of methyleneoxy pseudodipeptide building blocks in biologically active peptides

scientific article

Synthesis and evaluation of 2-pyridinylpyrimidines as inhibitors of HIV-1 structural protein assembly

scientific article published on 16 June 2016

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 murine endogenous retrovirus MIA14 encodes an active aspartic proteinase that is functionally similar to proteinases from D-type retroviruses

scientific article published on February 2002

The spacer peptide between human immunodeficiency virus capsid and nucleocapsid proteins is essential for ordered assembly and viral infectivity

scientific article published on June 1995

The yeast proteases Ddi1 and Wss1 are both involved in the DNA replication stress response

scientific article published on 27 June 2019

Thermodynamic and structural analysis of HIV protease resistance to darunavir - analysis of heavily mutated patient-derived HIV-1 proteases

scientific article

Thermodynamic characterization of the peptide assembly inhibitor binding to HIV-1 capsid protein

article

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

scientific article published on 01 February 2008

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

scientific article published on 9 March 2015

Unorthodox inhibitors of HIV protease: looking beyond active-site-directed peptidomimetics.

scientific article published on January 2014

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

scientific article published on 22 August 2020

Unusual binding mode of an HIV-1 protease inhibitor explains its potency against multi-drug-resistant virus strains

scientific article

Urea and Guanidinium Induced Denaturation of a Trp-Cage Miniprotein

scientific article published on 02 June 2011

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

scientific article published on 08 January 2016

Doba koronavirová ⬇️

book edition published in 2020

Spánek rozumu plodí příšery: Jan Konvalinka v rozhovoru o covidu, právu na omyl a historickém optimismu

book edition published in 2020

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