Published in Viruses on December 03, 2009
HIV-1 protease with 20 mutations exhibits extreme resistance to clinical inhibitors through coordinated structural rearrangements. Biochemistry (2012) 1.20
Autocatalytic maturation, physical/chemical properties, and crystal structure of group N HIV-1 protease: relevance to drug resistance. Protein Sci (2010) 1.01
Joint X-ray/neutron crystallographic study of HIV-1 protease with clinical inhibitor amprenavir: insights for drug design. J Med Chem (2013) 0.99
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease. J Med Chem (2013) 0.96
Terminal interface conformations modulate dimer stability prior to amino terminal autoprocessing of HIV-1 protease. Biochemistry (2012) 0.95
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Structures of darunavir-resistant HIV-1 protease mutant reveal atypical binding of darunavir to wide open flaps. ACS Chem Biol (2014) 0.81
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring. J Med Chem (2012) 0.80
Defective hydrophobic sliding mechanism and active site expansion in HIV-1 protease drug resistant variant Gly48Thr/Leu89Met: mechanisms for the loss of saquinavir binding potency. Biochemistry (2015) 0.79
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Capturing the reaction pathway in near-atomic-resolution crystal structures of HIV-1 protease. Biochemistry (2012) 0.79
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors. J Med Chem (2012) 0.78
Binding of Clinical Inhibitors to a Model Precursor of a Rationally Selected Multidrug Resistant HIV-1 Protease Is Significantly Weaker Than That to the Released Mature Enzyme. Biochemistry (2016) 0.78
Enhanced stability of monomer fold correlates with extreme drug resistance of HIV-1 protease. Biochemistry (2013) 0.78
Evolution under Drug Pressure Remodels the Folding Free-Energy Landscape of Mature HIV-1 Protease. J Mol Biol (2016) 0.77
Room Temperature Neutron Crystallography of Drug Resistant HIV-1 Protease Uncovers Limitations of X-ray Structural Analysis at 100 K. J Med Chem (2017) 0.76
Pulsed EPR characterization of HIV-1 protease conformational sampling and inhibitor-induced population shifts. Phys Chem Chem Phys (2016) 0.76
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Structural Studies of a Rationally Selected Multi-Drug Resistant HIV-1 Protease Reveal Synergistic Effect of Distal Mutations on Flap Dynamics. PLoS One (2016) 0.75
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Effect of the active site D25N mutation on the structure, stability, and ligand binding of the mature HIV-1 protease. J Biol Chem (2008) 1.44
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Crystal structures of a multidrug-resistant human immunodeficiency virus type 1 protease reveal an expanded active-site cavity. J Virol (2004) 1.40
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Atomic resolution crystal structures of HIV-1 protease and mutants V82A and I84V with saquinavir. Proteins (2007) 1.28
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease. Biochemistry (2004) 1.28
Crystal structures of HIV protease V82A and L90M mutants reveal changes in the indinavir-binding site. Eur J Biochem (2004) 1.27
Energy calculations and analysis of HIV-1 protease-inhibitor crystal structures. Protein Eng (1994) 1.25
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol (2005) 1.22
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Evaluation of the substrate envelope hypothesis for inhibitors of HIV-1 protease. Proteins (2007) 1.17
Darunavir: a review of its use in the management of HIV infection in adults. Drugs (2009) 1.16
Mechanism of drug resistance revealed by the crystal structure of the unliganded HIV-1 protease with F53L mutation. J Mol Biol (2006) 1.14
Effect of flap mutations on structure of HIV-1 protease and inhibition by saquinavir and darunavir. J Mol Biol (2008) 1.09
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Caught in the Act: the 1.5 A resolution crystal structures of the HIV-1 protease and the I54V mutant reveal a tetrahedral reaction intermediate. Biochemistry (2007) 1.03
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Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies. J Med Chem (2008) 1.02
Targeting the open-flap conformation of HIV-1 protease with pyrrolidine-based inhibitors. ChemMedChem (2008) 0.99
Molecular characterization of clinical isolates of human immunodeficiency virus resistant to the protease inhibitor darunavir. J Virol (2009) 0.99
Isolated lopinavir resistance after virological rebound of a ritonavir/lopinavir-based regimen. AIDS (2004) 0.97
Structural evidence for effectiveness of darunavir and two related antiviral inhibitors against HIV-2 protease. J Mol Biol (2008) 0.95
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. J Med Chem (2008) 0.95
Defining HIV-1 protease substrate selectivity. Curr Drug Targets Infect Disord (2002) 0.91
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir. J Med Chem (2008) 0.90
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. J Med Chem (2009) 0.90
Opportunities for structure-based design of protease-directed drugs. Curr Opin Struct Biol (2006) 0.89
Structural and thermodynamic basis of resistance to HIV-1 protease inhibition: implications for inhibitor design. Curr Drug Targets Infect Disord (2003) 0.88
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Resistant mechanism against nelfinavir of human immunodeficiency virus type 1 proteases. J Phys Chem B (2005) 0.87
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Potent HIV-1 protease inhibitors incorporating meso-bicyclic urethanes as P2-ligands: structure-based design, synthesis, biological evaluation and protein-ligand X-ray studies. Org Biomol Chem (2008) 0.85
Comparative studies on retroviral proteases: substrate specificity. Viruses (2010) 0.85
Tipranavir: a novel non-peptidic protease inhibitor for the treatment of HIV infection. Expert Opin Investig Drugs (2003) 0.84
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Detection of the protease codon 35 amino acid insertion in sequences from treatment-naïve HIV-1 subtype C infected individuals in the Central Region of Portugal. J Clin Virol (2009) 0.80
Drug-resistant HIV infection among drug-naive patients in Israel. Clin Infect Dis (2004) 0.79
Detection of a new 3-base pair insertion mutation in the protease gene of human immunodeficiency virus type 1 during highly active antiretroviral therapy (HAART). AIDS Res Hum Retroviruses (2005) 0.79
Probing multidrug-resistance and protein-ligand interactions with oxatricyclic designed ligands in HIV-1 protease inhibitors. ChemMedChem (2010) 1.11
Autocatalytic maturation, physical/chemical properties, and crystal structure of group N HIV-1 protease: relevance to drug resistance. Protein Sci (2010) 1.01
Structural basis for executioner caspase recognition of P5 position in substrates. Apoptosis (2008) 0.99
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease. J Med Chem (2013) 0.96
Design of HIV-1 protease inhibitors with C3-substituted hexahydrocyclopentafuranyl urethanes as P2-ligands: synthesis, biological evaluation, and protein-ligand X-ray crystal structure. J Med Chem (2011) 0.96
Design of substituted bis-Tetrahydrofuran (bis-THF)-derived Potent HIV-1 Protease Inhibitors, Protein-ligand X-ray Structure, and Convenient Syntheses of bis-THF and Substituted bis-THF Ligands. ACS Med Chem Lett (2011) 0.91
Role of valine 464 in the flavin oxidation reaction catalyzed by choline oxidase. Biochemistry (2010) 0.87
Highly potent HIV-1 protease inhibitors with novel tricyclic P2 ligands: design, synthesis, and protein-ligand X-ray studies. J Med Chem (2013) 0.84
Design of gem-difluoro-bis-tetrahydrofuran as P2 ligand for HIV-1 protease inhibitors to improve brain penetration: synthesis, X-ray studies, and biological evaluation. ChemMedChem (2014) 0.83
Caspase-3 binds diverse P4 residues in peptides as revealed by crystallography and structural modeling. Apoptosis (2009) 0.82
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Reaction intermediates discovered in crystal structures of enzymes. Adv Protein Chem Struct Biol (2012) 0.80
Substituent effects on P2-cyclopentyltetrahydrofuranyl urethanes: design, synthesis, and X-ray studies of potent HIV-1 protease inhibitors. Bioorg Med Chem Lett (2012) 0.80
A case of structure determination using pseudosymmetry. Acta Crystallogr D Biol Crystallogr (2009) 0.79
Design, synthesis, biological evaluation and X-ray structural studies of HIV-1 protease inhibitors containing substituted fused-tetrahydropyranyl tetrahydrofuran as P2-ligands. Org Biomol Chem (2015) 0.75