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Lista de obras de 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

artículo científico publicado en 2001

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

artículo científico publicado en 2007

A modular approach to HIV-1 proteinase inhibitor design

artículo científico publicado en 1996

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

artículo científico publicado en 2018

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

artículo científico publicado en 2007

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

artículo científico publicado en 2004

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

artículo científico publicado en 2000

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

artículo científico publicado en 1994

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

artículo científico publicado en 1995

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

artículo científico publicado en 2004

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

artículo científico publicado en 1995

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

artículo científico publicado en 1992

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

artículo científico publicado en 2003

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

article

Biochemical characterization of human glutamate carboxypeptidase III

artículo científico publicado en 2007

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

artículo científico publicado en 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).

artículo científico publicado en 2014

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

artículo científico publicado en 2016

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

artículo científico publicado en 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

artículo científico publicado en 2009

Czech bibliometric system fosters mediocre research

artículo científico publicado en 2009

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

artículo científico publicado en 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

artículo científico publicado en 2009

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

artículo científico publicado en 2015

Detection and quantitation of glutamate carboxypeptidase II in human blood.

artículo científico publicado en 2014

Determining and overcoming resistance to HIV protease inhibitors.

artículo científico publicado en 2004

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

artículo científico publicado en 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

artículo científico publicado en 2005

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

artículo científico publicado en 2012

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

artículo científico publicado en 2008

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

artículo científico publicado en 2008

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

artículo científico publicado en 2005

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.

artículo científico publicado en 2012

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

artículo científico publicado en 2014

Glutamate carboxypeptidase II does not process amyloid-β peptide.

artículo científico publicado en 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†

artículo científico publicado en 2006

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

artículo científico

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

artículo científico publicado en 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.

artículo científico publicado en 2005

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

artículo científico publicado en 2016

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

artículo científico publicado en 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

artículo científico publicado en 2002

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

artículo científico publicado en 2020

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

artículo científico publicado en 2018

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

artículo científico publicado en 2004

Induced maturation of human immunodeficiency virus.

artículo científico publicado en 2014

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

artículo científico publicado en 2018

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

artículo científico publicado en 2015

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

article

Inhibitor-Decorated Polymer Conjugates Targeting Fibroblast Activation Protein

artículo científico publicado en 2017

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

artículo científico publicado en 2018

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

artículo científico publicado en 2008

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

artículo científico publicado en 2019

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

artículo científico publicado en 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

artículo científico publicado en 2018

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

artículo científico publicado en 2016

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

artículo científico publicado en 2003

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

artículo científico publicado en 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.

artículo científico publicado en 2014

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

artículo científico publicado en 2007

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

artículo científico publicado en 2009

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

artículo científico publicado en 2007

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

artículo científico publicado en 2003

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

artículo científico publicado en 2017

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

artículo científico publicado en 2012

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

artículo científico publicado en 2008

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

artículo científico publicado en 2006

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

artículo científico publicado en 2011

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

artículo científico publicado en 1997

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

article

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

artículo científico publicado en 2009

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

artículo científico publicado el 1 de enero de 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.

artículo científico publicado en 2017

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

artículo científico publicado en 2014

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

artículo científico publicado en 2021

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

artículo científico publicado en 2009

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

artículo científico publicado en 2009

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

artículo científico publicado en 1992

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

artículo científico publicado en 2005

Retroviral proteases and their roles in virion maturation

artículo científico

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

artículo científico publicado en 2004

Sensitive, soluble chromogenic substrates for HIV-1 proteinase

artículo científico publicado en 1990

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.

artículo científico publicado en 2015

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

artículo científico publicado en 1996

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

artículo científico publicado en 1993

Specificity studies on retroviral proteinase from myeloblastosis-associated virus

artículo científico publicado en 1991

Spumapepsins

scholarly article

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

artículo científico publicado en 2016

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

artículo científico publicado en 2008

Structural and biochemical characterization of a novel aminopeptidase from human intestine

artículo científico publicado en 2015

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

artículo científico publicado en 2014

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

artículo científico publicado en 2009

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II

artículo científico publicado en 2007

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

artículo científico publicado en 2016

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

artículo científico publicado en 2006

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

artículo científico publicado en 2012

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

artículo científico publicado en 1990

Subsite specificity of the proteinase from myeloblastosis associated virus

artículo científico publicado en 1991

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

artículo científico publicado en 2002

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

artículo científico publicado en 2004

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

artículo científico publicado en 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

artículo científico publicado en 2002

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

artículo científico publicado en 1995

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

artículo científico publicado en 2019

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

artículo científico publicado en 2014

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

artículo científico publicado en 2015

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

artículo científico

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

artículo científico publicado en 2020

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

artículo científico publicado en 2002

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.

artículo científico

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