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Structural basis of HIV-1 and HIV-2 protease inhibition by a monoclonal antibody
STRUCTURE
HIV-1 protease inhibitors containing an N-hydroxyamino acid core structure
BIOORGANIC & MEDICINAL CHEMISTRY
Synthesis and biological evaluation of prodrug-type anti-HIV agents: Esterconjugates of carboxylic acid-containing dipeptide HIV protease inhibitorsand a reverse transcriptase inhibitor
BIOORGANIC & MEDICINAL CHEMISTRY
Does a diol cyclic urea inhibitor of HIV-1 protease bind tighter than its corresponding alcohol form? A study by free energy perturbation and continuum electrostatics calculations
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
FILO (Field Interaction Ligand Optimization): A simplex strategy for searching the optimal ligand interaction field in drug design
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
1.9 angstrom X-ray study shows closed flap conformation in crystals of tethered HIV-1PR
PROTEINS-STRUCTURE FUNCTION AND GENETICS
Human alpha-1-glycoprotein and its interactions with drugs
DRUG METABOLISM REVIEWS
Saquinavir and ritonavir pharmacokinetics following combined ritonavir andsaquinavir (soft gelatin capsules) administration
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
Effect of alpha(1)-acid glycoprotein on the intracellular accumulation of the HIV protease inhibitors saquinavir, ritonavir and indinavir in vitro
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
Pharmacokinetics and resistance mutations affect virologic response to ritonavir/saquinavir-containing regimens
THERAPEUTIC DRUG MONITORING
Saquinavir soft gelatin capsule - A comparative safety review
DRUG SAFETY
P450 interaction with HIV protease inhibitors: Relationship between metabolic stability, inhibitory potency, and p450 binding spectra
DRUG METABOLISM AND DISPOSITION
Chapter 24. Pharmacokinetics and design of aspartyl protease inhibitors
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 36
Syntheses of FDA approved HIV protease inhihitors
SYNTHESIS-STUTTGART
The interaction of saquinavir (soft gelatin capsule) with ketoconazole, erythromycin and rifampicin: comparison of the effect in healthy volunteers and in HIV-infected patients
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
Mechanism of indinavir-induced hyperbilirubinemia
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
P-glycoprotein limits oral availability, brain, and fetal penetration of saquinavir even with high doses of ritonavir
MOLECULAR PHARMACOLOGY
Design and synthesis of potent C-2-symmetric diol-based HIV-1 protease inhibitors: Effects of fluoro substitution
JOURNAL OF MEDICINAL CHEMISTRY
Inhibition of human endogenous retrovirus-K10 protease in cell-free and cell-based assays
JOURNAL OF BIOLOGICAL CHEMISTRY
Parameterization of the approximate valence bond (AVB) method to describe potential energy surface in the reaction catalyzed by HIV-1 protease
INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY
Real time NMR monitoring of local unfolding of HIV-1 protease tethered dimer driven by autolysis
FEBS LETTERS
Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement
CLINICAL PHARMACOLOGY & THERAPEUTICS
Parallel simulated tempering dynamics of ligand-protein binding with ensembles of protein conformations
CHEMICAL PHYSICS LETTERS
Inhibitory effects on HIV-1 protease of tri-p-coumaroylspermidine from Artemisia caruifolia and related amides
CHEMICAL & PHARMACEUTICAL BULLETIN
Follow the protons: A low-barrier hydrogen bond unifies the mechanisms of the aspartic proteases
ACCOUNTS OF CHEMICAL RESEARCH
Dose-finding study of once-daily indinavir/ritonavir plus zidovudine and lamivudine in HIV-infected patients
JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES
Determination of twelve antiretroviral agents in human plasma sample usingreversed-phase high-performance liquid chromatography
JOURNAL OF CHROMATOGRAPHY B
Systematic mutational analysis of the active-site threonine of HIV-1 proteinase: Rethinking the "fireman's grip" hypothesis
PROTEIN SCIENCE
Phosphinic acid compounds in biochemistry, biology and medicine
CURRENT MEDICINAL CHEMISTRY
Homology model directed alignment selection for comparative molecular field analysis: Application to photosystem II inhibitors
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins
BIOLOGICAL & PHARMACEUTICAL BULLETIN
An alternate binding site for the P1-P3 group of a class of potent HIV-1 protease inhibitors as a result of concerted structural change in the 80s loop of the protease
ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY
Competing drug-drug interactions among multidrug antiretroviral regimens used in the treatment of HIV-infected subjects: ACTG 884
AIDS
New antiretroviral drugs in development
AIDS
The influence of natural products upon drug discovery
NATURAL PRODUCT REPORTS
Binding free energy simulations of the HIV-1 protease and hydroxyethylene isostere inhibitors
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
Structural and biochemical studies of retroviral proteases
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEIN STRUCTURE AND MOLECULAR ENZYMOLOGY
Novel variable selection quantitative structure-property relationship approach based on the k-nearest-neighbor principle
JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES
Pharmacokinetic interaction between amprenavir and clarithromycin in healthy male volunteers
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Pharmacokinetic interactions between HIV-1 protease inhibitors in rats: Study on combinations of two kinds of HIV-1 protease inhibitors
JOURNAL OF PHARMACY AND PHARMACOLOGY
Free energy calculations on dimer stability of the HIV protease using molecular dynamics and a continuum solvent model
JOURNAL OF MOLECULAR BIOLOGY
Chemometric classification of HIV-1 protease inhibitors
INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY
Amprenavir - A review of its clinical potential in patients with HIV infection
DRUGS
Ab initio studies on the catalytic mechanism of aspartic proteinases: Nucleophilic versus general acid/general base mechanism
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
High-performance liquid chromatographic method for the simultaneous determination of HIV-1 protease inhibitors indinavir, saquinavir and ritonavir inplasma of patients during highly active antiretroviral therapy
JOURNAL OF CHROMATOGRAPHY B
Determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine using high-performance liquid chromatography with fluorescence detection
JOURNAL OF CHROMATOGRAPHY B
Autoprocessing of HIV-1 protease is tightly coupled to protein folding
NATURE STRUCTURAL BIOLOGY
Nelfinavir mesylate: A protease inhibitor
ANNALS OF PHARMACOTHERAPY
Flap opening and dimer-interface flexibility in the free and inhibitor-bound HIV protease, and their implications for function
STRUCTURE WITH FOLDING & DESIGN
Drug resistance mutations can affect dimer stability of HIV-1 protease at neutral pH
PROTEIN SCIENCE
Thermodynamic linkage between the binding of protons and inhibitors to HIV-1 protease
PROTEIN SCIENCE
Anti-HIV effect of saquinavir combined with ritonavir is limited by previous long-term therapy with protease inhibitors
AIDS RESEARCH AND HUMAN RETROVIRUSES
Extensive impairment of triazolam and alprazolam clearance by short-term low-dose ritonavir: The clinical dilemma of concurrent inhibition and induction
JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY
The steady-state plasma pharmacokinetics of indinavir alone and in combination with a low dose of ritonavir in twice daily dosing regimens in HIV-1-infected individuals
AIDS
Role of pharmacokinetics in the discovery and development of indinavir
ADVANCED DRUG DELIVERY REVIEWS
P-glycoprotein, secretory transport, and other barriers to the oral delivery of anti-HIV drugs
ADVANCED DRUG DELIVERY REVIEWS
A phase I trial of the pharmacokinetics, toxicity, and activity of KNI-272, an inhibitor of HIV-1 protease, in patients with AIDS or symptomatic HIV infection
ANTIVIRAL RESEARCH
Pharmacokinetic interactions between HIV-protease inhibitors in rats
BIOPHARMACEUTICS & DRUG DISPOSITION
Mechanism of action of aspartyl proteases. VII. Noncovalent complexes of HIV-1 aspartic protease with substrate and substrate-like inhibitor
BIOORGANICHESKAYA KHIMIYA
FDA evaluations using in vitro metabolism to predict and interpret in vivometabolic drug-drug interactions: Impact on labeling
JOURNAL OF CLINICAL PHARMACOLOGY
Assessment of the quality and quantity of drug-drug interaction studies inrecent NDA submissions: Study design and data analysis issues
JOURNAL OF CLINICAL PHARMACOLOGY
Potent inhibition of the cytochrome P-450 3A-mediated human liver microsomal metabolism of a novel HIV protease inhibitor by ritonavir: A positive drug-drug interaction
DRUG METABOLISM AND DISPOSITION
In vitro metabolism of the HIV-1 protease inhibitor ABT-378: Species comparison and metabolite identification
DRUG METABOLISM AND DISPOSITION
A convergent, stereocontrolled synthesis of C-2-symmetrical and pseudosymmetrical sulfur-tethered bis(amino alcohols)
TETRAHEDRON LETTERS
Interactions of HIV protease inhibitors with ATP-dependent drug export proteins
MOLECULAR PHARMACOLOGY
Simultaneous investigation of indinavir nonlinear pharmacokinetics and bioavailability in healthy volunteers using stable isotope labeling technique:Study design and model-independent data analysis
JOURNAL OF PHARMACEUTICAL SCIENCES
Diversity analysis of 14 156 molecules tested by the National Cancer Institute for anti-HIV activity using the quantitative structure-activity relational expert system MCASE
JOURNAL OF MEDICINAL CHEMISTRY
Inhibitors of the C-2-symmetric HIV-1 protease: Nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2 ' side chains
JOURNAL OF MEDICINAL CHEMISTRY
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors
JOURNAL OF MEDICINAL CHEMISTRY
A distinct member of the aspartic proteinase gene family from the human malaria parasite Plasmodium falciparum
FEBS LETTERS
Structural and kinetic analysis of drug resistant mutants of HIV-1 protease
EUROPEAN JOURNAL OF BIOCHEMISTRY
Safety and efficacy of ritonavir and saquinavir in combination with zidovudine and lamivudine
CLINICAL PHARMACOLOGY & THERAPEUTICS
Comparative quantitative structure-activity relationship studies on anti-HIV drugs
CHEMICAL REVIEWS
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease
BIOCHEMISTRY
HIV protease inhibitor ritonavir: A more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833
BIOCHEMICAL PHARMACOLOGY
Caged HIV-1 protease: Dimerization is independent of the ionization state of the active site aspartates
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
DESIGN AND SELECTION OF DMP-850 AND DMP-851 - THE NEXT-GENERATION OF CYCLIC UREA HIV PROTEASE INHIBITORS
Chemistry & biology
THE SYNTHESIS OF SYMMETRICAL AND UNSYMMETRICAL P1 P1' CYCLIC UREAS ASHIV PROTEASE INHIBITORS/
Bioorganic & medicinal chemistry letters
THE SYNTHESIS AND EVALUATION OF CYCLIC UREAS AS HIV PROTEASE INHIBITORS - MODIFICATIONS OF THE P1 P1' RESIDUES/
Bioorganic & medicinal chemistry letters
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P-3 ligands
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Tricyclic ureas: A new class of HIV-1 protease inhibitors
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Restricting the flexibility of crosslinked, interfacial peptide inhibitorsof HIV-1 protease
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
INHIBITING THE DIMERIZATION OF HIV-1 PROTEASE
Synlett
RECEPTOR-BASED PREDICTION OF BINDING AFFINITIES
Perspectives in drug discovery and design
A-PRIORI PREDICTION OF LIGAND AFFINITY BY ENERGY MINIMIZATION
Perspectives in drug discovery and design
3D QSAR - CURRENT STATE, SCOPE, AND LIMITATIONS
Perspectives in drug discovery and design
RECENT PROGRESS IN COMFA METHODOLOGY AND RELATED TECHNIQUES
Perspectives in drug discovery and design
INHIBITION AND INDUCTION OF CYTOCHROME-P450 AND THE CLINICAL IMPLICATIONS
Clinical pharmacokinetics
THE DURATION OF VIRAL SUPPRESSION DURING PROTEASE INHIBITOR THERAPY FOR HIV-1 INFECTION IS PREDICTED BY PLASMA HIV-1 RNA AT THE NADIR
AIDS
RECENT DEVELOPMENTS IN HIV PROTEASE INHIBITOR THERAPY
Antiviral research
FOCAL MYCOBACTERIAL LYMPHADENITIS FOLLOWING INITIATION OF PROTEASE-INHIBITOR THERAPY IN PATIENTS WITH ADVANCED HIV-1 DISEASE
Lancet
PHARMACOKINETIC INTERACTION BETWEEN RITONAVIR AND INDINAVIR IN HEALTHY-VOLUNTEERS
Antimicrobial agents and chemotherapy
PHARMACOKINETIC ASPECTS OF PALINAVIR, AN HIV PROTEASE INHIBITOR, IN SPRAGUE-DAWLEY RATS
Journal of pharmaceutical sciences
ROLE OF P-GLYCOPROTEIN AND CYTOCHROME-P450 3A IN LIMITING ORAL ABSORPTION OF PEPTIDES AND PEPTIDOMIMETICS
Journal of pharmaceutical sciences
INHIBITION OF DESIPRAMINE HYDROXYLATION (CYTOCHROME P450-2D6) IN-VITRO BY QUINIDINE AND BY VIRAL PROTEASE INHIBITORS - RELATION TO DRUG-INTERACTIONS IN-VIVO
Journal of pharmaceutical sciences
DISCOVERY OF RITONAVIR, A POTENT INHIBITOR OF HIV PROTEASE WITH HIGH ORAL BIOAVAILABILITY AND CLINICAL EFFICACY
Journal of medicinal chemistry
TIPRANAVIR (PNU-140690) - A POTENT, ORALLY BIOAVAILABLE NONPEPTIDIC HIV PROTEASE INHIBITOR OF THE 5,6-DIHYDRO-4-HYDROXY-2-PYRONE SULFONAMIDE CLASS
Journal of medicinal chemistry
NONSYMMETRIC P2 P2' CYCLIC UREA HIV PROTEASE INHIBITORS - STRUCTURE-ACTIVITY RELATIONSHIP, BIOAVAILABILITY, AND RESISTANCE PROFILE OF MONOINDAZOLE-SUBSTITUTED P2 ANALOGS/
Journal of medicinal chemistry
CYCLIC HIV PROTEASE INHIBITORS - DESIGN AND SYNTHESIS OF ORALLY BIOAVAILABLE, PYRAZOLE P2 P2' CYCLIC UREAS WITH IMPROVED POTENCY/
Journal of medicinal chemistry
MOLECULAR RECOGNITION OF CYCLIC UREA HIV-1 PROTEASE INHIBITORS
The Journal of biological chemistry