Jan Konvalinka

Author PubWeight™ 49.94‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 A novel substrate-based HIV-1 protease inhibitor drug resistance mechanism. PLoS Med 2007 1.99
2 Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer. EMBO J 2006 1.55
3 Molecular analysis of the HIV-1 resistance development: enzymatic activities, crystal structures, and thermodynamics of nelfinavir-resistant HIV protease mutants. J Mol Biol 2007 1.19
4 Substrate specificity, inhibition and enzymological analysis of recombinant human glutamate carboxypeptidase II. J Neurochem 2002 1.17
5 From nonpeptide toward noncarbon protease inhibitors: metallacarboranes as specific and potent inhibitors of HIV protease. Proc Natl Acad Sci U S A 2005 1.11
6 Current and Novel Inhibitors of HIV Protease. Viruses 2009 1.10
7 Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity. Protein Sci 2004 1.09
8 Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. J Med Chem 2007 1.08
9 Czech bibliometric system fosters mediocre research. Nature 2009 1.08
10 Ninety-nine is not enough: molecular characterization of inhibitor-resistant human immunodeficiency virus type 1 protease mutants with insertions in the flap region. J Virol 2008 1.08
11 Dual substrate and reaction specificity in mouse serine racemase: identification of high-affinity dicarboxylate substrate and inhibitors and analysis of the beta-eliminase activity. Biochemistry 2005 1.07
12 Structural basis of interactions between human glutamate carboxypeptidase II and its substrate analogs. J Mol Biol 2008 1.01
13 Inhibition of human serine racemase, an emerging target for medicinal chemistry. Curr Drug Targets 2011 1.00
14 Molecular characterization of clinical isolates of human immunodeficiency virus resistant to the protease inhibitor darunavir. J Virol 2009 0.99
15 Biochemical characterization of human glutamate carboxypeptidase III. J Neurochem 2007 0.98
16 A high-resolution structure of ligand-free human glutamate carboxypeptidase II. Acta Crystallogr Sect F Struct Biol Cryst Commun 2007 0.98
17 Unusual binding mode of an HIV-1 protease inhibitor explains its potency against multi-drug-resistant virus strains. J Mol Biol 2002 0.96
18 Inhibitor binding at the protein interface in crystals of a HIV-1 protease complex. Acta Crystallogr D Biol Crystallogr 2004 0.96
19 Design of HIV protease inhibitors based on inorganic polyhedral metallacarboranes. J Med Chem 2009 0.96
20 Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. J Med Chem 2008 0.95
21 Proteinases of betaretroviruses bind single-stranded nucleic acids through a novel interaction module, the G-patch. FEBS Lett 2004 0.94
22 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. J Phys Chem B 2010 0.93
23 Mutations in HIV-1 gag and pol compensate for the loss of viral fitness caused by a highly mutated protease. Antimicrob Agents Chemother 2012 0.93
24 Reaction mechanism of glutamate carboxypeptidase II revealed by mutagenesis, X-ray crystallography, and computational methods. Biochemistry 2009 0.90
25 Mapping of the active site of glutamate carboxypeptidase II by site-directed mutagenesis. FEBS J 2007 0.89
26 Tissue expression and enzymologic characterization of human prostate specific membrane antigen and its rat and pig orthologs. Prostate 2008 0.89
27 Expression and distribution of 'high affinity' glutamate transporters GLT1, GLAST, EAAC1 and of GCPII in the rat peripheral nervous system. J Anat 2008 0.88
28 Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir. Protein Sci 2008 0.88
29 Mouse brain serine racemase catalyzes specific elimination of L-serine to pyruvate. FEBS Lett 2003 0.88
30 Kinetics of the dimerization of retroviral proteases: the "fireman's grip" and dimerization. Protein Sci 2003 0.87
31 Amino acids at the N- and C-termini of human glutamate carboxypeptidase II are required for enzymatic activity and proper folding. Eur J Biochem 2004 0.87
32 HIV-1 protease inhibitor mutations affect the development of HIV-1 resistance to the maturation inhibitor bevirimat. Retrovirology 2011 0.86
33 Determining and overcoming resistance to HIV protease inhibitors. Curr Drug Targets Infect Disord 2004 0.86
34 Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity. J Med Chem 2011 0.84
35 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. Biol Chem 2005 0.83
36 Recombinant human serine racemase: enzymologic characterization and comparison with its mouse ortholog. Protein Expr Purif 2008 0.83
37 Structural insight into the evolutionary and pharmacologic homology of glutamate carboxypeptidases II and III. FEBS J 2009 0.83
38 Structural and biochemical characterization of the folyl-poly-γ-l-glutamate hydrolyzing activity of human glutamate carboxypeptidase II. FEBS J 2014 0.83
39 A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution. J Med Chem 2004 0.83
40 Urea and guanidinium induced denaturation of a Trp-cage miniprotein. J Phys Chem B 2011 0.82
41 Detection and quantitation of glutamate carboxypeptidase II in human blood. Prostate 2014 0.81
42 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. J Med Chem 2006 0.81
43 Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor. J Med Chem 2009 0.80
44 GS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions. J Virol 2013 0.79
45 Prostate-specific membrane antigen and its truncated form PSM'. Prostate 2009 0.79
46 Structure-aided design of novel inhibitors of HIV protease based on a benzodiazepine scaffold. J Med Chem 2012 0.79
47 Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies. Antiviral Res 2008 0.78
48 Thermodynamic and structural analysis of HIV protease resistance to darunavir - analysis of heavily mutated patient-derived HIV-1 proteases. FEBS J 2014 0.78
49 The murine endogenous retrovirus MIA14 encodes an active aspartic proteinase that is functionally similar to proteinases from D-type retroviruses. Arch Biochem Biophys 2002 0.78
50 Response of HIV positive patients to the long-term salvage therapy by lopinavir/ritonavir. J Clin Virol 2005 0.78
51 Non-infectious fluorimetric assay for phenotyping of drug-resistant HIV proteinase mutants. J Clin Virol 2006 0.77
52 An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study. J Med Chem 2003 0.76
53 Capillary electrophoresis method for determination of D-serine and its application for monitoring of serine racemase activity. Electrophoresis 2006 0.76
54 Role of hydroxyl group and R/S configuration of isostere in binding properties of HIV-1 protease inhibitors. Eur J Biochem 2004 0.75
55 Glutamate carboxypeptidase II does not process amyloid-β peptide. FASEB J 2013 0.75
56 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. J Med Chem 2002 0.75
57 Ion specific effects of alkali cations on the catalytic activity of HIV-1 protease. Faraday Discuss 2013 0.75
58 Ion specific effects of sodium and potassium on the catalytic activity of HIV-1 protease. Phys Chem Chem Phys 2009 0.75
59 On the role of the R configuration of the reaction-intermediate isostere in HIV-1 protease-inhibitor binding: X-ray structure at 2.0 A resolution. Acta Crystallogr D Biol Crystallogr 2006 0.75
60 Anomalous adsorptive properties of HIV protease: indication of two-dimensional crystallization? Colloids Surf B Biointerfaces 2008 0.75