darunavir has been researched along with saquinavir in 51 studies
| Studies (darunavir) | Trials (darunavir) | Recent Studies (post-2010) (darunavir) | Studies (saquinavir) | Trials (saquinavir) | Recent Studies (post-2010) (saquinavir) |
|---|---|---|---|---|---|
| 1,148 | 224 | 780 | 1,454 | 256 | 219 |
| Protein | Taxonomy | darunavir (IC50) | saquinavir (IC50) |
|---|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | 1.9 | |
| Bile salt export pump | Homo sapiens (human) | 3.9 | |
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 (BRU ISOLATE) | 0.016 | |
| Gag-Pol polyprotein | Human immunodeficiency virus type 2 (ISOLATE ROD) | 0.0084 | |
| Gag polyprotein | HIV-1 M:B_MN | 0.0131 | |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | 4.05 | |
| Cytochrome P450 3A4 | Homo sapiens (human) | 1.5 | |
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | 0.0066 | |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | 4.273 | |
| Substance-K receptor | Homo sapiens (human) | 6.214 | |
| Thromboxane-A synthase | Homo sapiens (human) | 2.182 | |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | 4.273 | |
| Mu-type opioid receptor | Homo sapiens (human) | 9.625 | |
| Kappa-type opioid receptor | Homo sapiens (human) | 6.951 | |
| Exoribonuclease H | Human immunodeficiency virus 2 | 0.0005 | |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | 1.9 | |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | 1.9 | |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | 1.9 | |
| Genome polyprotein | Human rhinovirus sp. | 0.0005 | |
| Solute carrier family 22 member 1 | Rattus norvegicus (Norway rat) | 8.26 | |
| Protease | Human immunodeficiency virus 1 | 0.0217 | |
| Protease | Human immunodeficiency virus 1 | 0.0004 |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 20 (39.22) | 29.6817 |
| 2010's | 26 (50.98) | 24.3611 |
| 2020's | 5 (9.80) | 2.80 |
| Authors | Studies |
|---|---|
| Azijn, H; de Bethune, MP; de Kock, HA; De Meyer, S; King, NM; Maes, LJ; Pauwels, R; Peeters, A; Pille, GM; Prabu-Jeyabalan, M; Schiffer, CA; Surleraux, DL; Vendeville, S; Verschueren, WG; Wigerinck, PB | 1 |
| Cho, H; Ghosh, AK; Hussain, KA; Kay, S; Koh, Y; Leshchenko, S; Mitsuya, H; Swanson, LM; Walters, DE | 1 |
| Andrews, CW; Brieger, M; Furfine, ES; Hale, MR; Hanlon, MH; Hazen, RJ; Kaldor, I; McLean, EW; Miller, JF; Reynolds, D; Sammond, DM; Sherrill, RG; Spaltenstein, A; Tung, R; Turner, EM; Xu, RX | 1 |
| Das, D; Gatanaga, H; Ghosh, AK; Grum-Tokars, V; Hussain, AK; Koh, Y; Kovalevsky, AY; Leshchenko, S; Li, J; Maeda, K; Mitsuya, H; Sridhar, PR; Walters, DE; Weber, IT; Wedekind, JE | 1 |
| Amano, M; Boross, PI; Das, D; Ghosh, AK; Koh, Y; Leschenko, S; Li, J; Mitsuya, H; Wang, YF; Weber, IT | 1 |
| Bernstein, B; Dekhtyar, T; Gao, F; Hanna, GJ; Kempf, D; Koev, G; Lu, L; Lu, X; Masse, S; Mo, H; Molla, A | 1 |
| Babusis, D; Bhoopathy, S; Hidalgo, IJ; Phan, TK; Ray, AS; Rhodes, GR; Robinson, KL; Strab, R; Tong, L | 1 |
| DeGoey, DA; Dekhtyar, T; Flosi, WJ; Grampovnik, DJ; Kempf, DJ; Klein, LL; Lu, L; Masse, S; Molla, A; Ng, TI | 1 |
| Bénard, A; Brun-Vézinet, F; Campa, P; Chêne, G; Collin, G; Damond, F; Desbois, D; Descamps, D; Matheron, S; Peytavin, G; Roquebert, B | 1 |
| Brynda, J; Cígler, P; Fanfrlík, J; Grantz Sasková, K; Grüner, B; Konvalinka, J; Kozísek, M; Král, V; Lepsík, M; Plesek, J; Pokorná, J; Rezácová, P; Václavíková, J | 1 |
| Baldridge, A; Gemma, S; Ghosh, AK; Koh, Y; Kovalevsky, AY; Mitsuya, H; Wang, YF; Weber, IT | 1 |
| Ghosh, AK; Kovalevsky, AY; Weber, IT | 1 |
| Amano, M; Das, D; Ghosh, AK; Koh, Y; Leschenko, S; Mitsuya, H; Nakata, H; Nakayama, M; Ogata-Aoki, H | 1 |
| Ghosh, AK | 1 |
| Amano, M; Anderson, DD; Baldridge, A; Chumanevich, AA; Ghosh, AK; Hong, L; Koh, Y; Kovalevsky, AY; Kulkarni, S; Mitsuya, H; Tang, J; Tojo, Y; Wang, YF; Weber, IT | 1 |
| Axelsson, L; Ekegren, JK; Hallberg, A; Kihlström, J; Larhed, M; Mahalingam, AK; Samuelsson, B; Unge, T; Wallberg, H; Wannberg, J | 1 |
| Andrews, KT; Butterworth, AS; Eickel, N; Gardiner, DL; MacDonald, T; McCarthy, JS; Peatey, CL; Skinner-Adams, TS; Trenholme, KR | 1 |
| Amano, M; Anderson, DD; Aoki, M; Das, D; Ghosh, AK; Koh, Y; Kulkarni, S; Mitsuya, H; Tojo, Y | 1 |
| Kempf, DJ; Norton, M; Parkin, NT; Pilot-Matias, T; Stawiski, E; Trinh, R; Young, TP | 1 |
| Cane, PA; Kolli, M; Myers, RE; Parry, CM; Pillay, D; Schiffer, C | 1 |
| Amano, M; Baldridge, A; Chapsal, BD; Ghosh, AK; Koh, Y; Mitsuya, H; Steffey, MP; Walters, DE | 1 |
| Agniswamy, J; Amano, M; Chapsal, BD; Ghosh, AK; Mitsuya, H; Parham, GL; Steffey, M; Wang, YF; Weber, IT | 1 |
| Hamburger, M; Hamy, F; Klimkait, T; Louvel, S; Mojarrab, M; Potterat, O; Sanglier, JJ; Vidal, V | 1 |
| Agniswamy, J; Ghosh, AK; Louis, JM; Rao, KV; Sayer, JM; Shen, CH; Wang, YF; Weber, IT; Xu, CX | 1 |
| Agniswamy, J; Amano, M; Ghosh, AK; Martyr, CD; Mitsuya, H; Nyalapatla, PR; Osswald, HL; Parham, GL; Wang, YF; Weber, IT | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Agniswamy, J; Aoki, M; Bulut, H; Das, D; Ghosh, AK; Hayashi, H; Martyr, CD; Mitsuya, H; Nyalapatla, PR; Osswald, HL; Rao, KV; Wang, YF; Weber, IT | 1 |
| Agniswamy, J; Amano, M; Aoki, M; Brindisi, M; Ghosh, AK; Kovela, S; Mitsuya, H; Osswald, HL; R Nyalapatla, P; Rao, KV; Wang, YF; Weber, IT | 1 |
| Agniswamy, J; Ghosh, AK; Hattori, SI; Jadhav, RD; Kovela, S; Mitsuya, H; Osswald, H; Simpson, H; Wang, YF; Weber, IT | 1 |
| Agniswamy, J; Ghosh, AK; Hattori, SI; Hayashi, H; Ho, RY; Mitsuya, H; Simpson, HM; Wang, YF; Weber, IT; Williams, JN | 1 |
| Agniswamy, J; Amano, M; Aoki, M; Ghosh, AK; Kovela, S; Mitsuya, H; Osswald, HL; Wang, YF; Weber, IT | 1 |
| Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M | 1 |
| Adams, E; Hoogmartens, J; Van Schepdael, A; Yekkala, R | 1 |
| De Pauw, M; Hoetelmans, RM; Lefebvre, E; Mariën, K; Sekar, VJ; Vangeneugden, T | 1 |
| Bacha, UM; Brower, ET; Freire, E; Kawasaki, Y | 1 |
| Ghosh, AK; Harrison, RW; Kovalevsky, AY; Liu, F; Tie, Y; Weber, IT | 1 |
| Louis, JM; Sayer, JM | 1 |
| Berginc, K; Kristl, A; Trontelj, J | 1 |
| Fessel, WJ; Hellinger, J; Kaufman, D; Rhee, SY; Ruane, P; Shafer, RW; Shirvani, V; Taylor, J; Towner, W; Troia, P; Zolopa, A | 1 |
| Haefeli, WE; Herzog, M; König, SK; Theile, D; Weiss, J; Zembruski, N | 1 |
| Berginc, K; Kristl, A; Milisav, I | 1 |
| Berginc, K; Kristl, A; Trdan, T; Trontelj, J | 1 |
| de Béthune, MP; De Meyer, S; Dierynck, I; Lathouwers, E; Picchio, G; Spinosa-Guzman, S; Van De Casteele, T; Vanden Abeele, C | 1 |
| Nsanzabana, C; Rosenthal, PJ | 1 |
| Boross, PI; Chiu, TY; Ghosh, AK; Harrison, RW; Louis, JM; Tie, Y; Tozser, J; Wang, YF; Weber, IT | 1 |
| Daniels, SI; Davidoff, KS; Davis, DA; Naiman, NE; Soule, EE; Yarchoan, R | 1 |
| Leonis, G; Papadopoulos, MG; Steinbrecher, T | 1 |
| Amano, M; Das, D; Ghosh, AK; Mitsuya, H; Mizuno, A; Salcedo Gómez, PM; Yashchuk, S | 1 |
| Festa, L; Geiger, JD; Grinspan, JB; Jordan-Sciutto, KL; K Jensen, B; Roth, LM | 1 |
| Talluri, S | 1 |
| Hirano, Y; Komatsu, TS; Koyama, YM; Morimoto, G; Ohno, Y; Okimoto, N; Taiji, M | 1 |
3 review(s) available for darunavir and saquinavir
| Article | Year |
|---|---|
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.
Topics: Alzheimer Disease; Amyloid Precursor Protein Secretases; Animals; Antiviral Agents; Aspartic Acid Endopeptidases; Biological Products; Darunavir; Drug Design; Drug Discovery; Drug Resistance, Viral; Enzyme Inhibitors; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Molecular Mimicry; Molecular Structure; Peptides; Structure-Activity Relationship; Sulfonamides | 2009 |
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
Quality control of protease inhibitors.
Topics: Anti-HIV Agents; Atazanavir Sulfate; Carbamates; Chromatography, Liquid; Darunavir; Drug Contamination; Furans; HIV Protease Inhibitors; Indinavir; Lopinavir; Nelfinavir; Oligopeptides; Organophosphates; Pyridines; Pyrimidinones; Pyrones; Quality Control; Ritonavir; Saquinavir; Sulfonamides | 2008 |
2 trial(s) available for darunavir and saquinavir
| Article | Year |
|---|---|
Pharmacokinetic interaction between darunavir and saquinavir in HIV-negative volunteers.
Topics: Adolescent; Adult; Anti-HIV Agents; Area Under Curve; Cross-Over Studies; Darunavir; Dose-Response Relationship, Drug; Drug Interactions; Drug Monitoring; Drug Therapy, Combination; HIV Seronegativity; Humans; Middle Aged; Ritonavir; Saquinavir; Sulfonamides | 2007 |
In vitro susceptibility and virological outcome to darunavir and lopinavir are independent of HIV type-1 subtype in treatment-naive patients.
Topics: Adamantane; Adult; Analysis of Variance; Atazanavir Sulfate; Carbamates; Darunavir; Drug Resistance, Viral; Furans; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Indinavir; Lopinavir; Microbial Sensitivity Tests; Molecular Typing; Nelfinavir; Neuraminidase; Oligopeptides; Pyridines; Pyrimidinones; Pyrones; Saquinavir; Sulfonamides; Viral Load | 2010 |
46 other study(ies) available for darunavir and saquinavir
| Article | Year |
|---|---|
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
Topics: Animals; Benzoxazoles; Binding Sites; Calorimetry; Cell Line; Crystallography, X-Ray; Dogs; Drug Resistance, Multiple, Viral; Drug Stability; HIV Protease Inhibitors; HIV-1; Humans; In Vitro Techniques; Microsomes, Liver; Models, Molecular; Rats; Rats, Wistar; Sulfonamides; Thermodynamics; Thiazoles | 2005 |
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.
Topics: Cell Line; Crystallography, X-Ray; Drug Design; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Lactams; Lactams, Macrocyclic; Models, Molecular; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Sulfonamides | 2005 |
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Topics: HIV Protease Inhibitors; Molecular Structure; Sulfonamides | 2006 |
Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance.
Topics: Bridged Bicyclo Compounds, Heterocyclic; Cell Line; Crystallography, X-Ray; Darunavir; Drug Design; Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Models, Molecular; Molecular Structure; Protein Conformation; Protein Structure, Tertiary; Stereoisomerism; Structure-Activity Relationship; Sulfonamides | 2006 |
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
Topics: Amino Acid Sequence; Drug Design; Drug Resistance, Multiple, Viral; Furans; HIV Infections; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Microbial Sensitivity Tests; Models, Molecular; Molecular Sequence Data; Sulfonamides; Urethane; Virus Replication | 2007 |
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
Topics: Amino Acid Sequence; Anti-HIV Agents; Cell Line; Cytopathogenic Effect, Viral; Drug Resistance, Viral; HIV Core Protein p24; HIV Protease Inhibitors; HIV-2; Humans; Lopinavir; Molecular Sequence Data; Mutagenesis, Site-Directed; Phenotype; Pyrimidinones; RNA-Directed DNA Polymerase; Virus Replication | 2007 |
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
Topics: Adenine; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Cell Line; Chromatography, High Pressure Liquid; Data Interpretation, Statistical; Dose-Response Relationship, Drug; Drug Interactions; Epithelium; HIV Protease Inhibitors; Humans; Hydrolysis; Indicators and Reagents; Intestinal Absorption; Mass Spectrometry; Organophosphonates; Subcellular Fractions; Tenofovir | 2007 |
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
Topics: Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Lopinavir; Microbial Sensitivity Tests; Mutation; Phenotype; Pyrimidinones; Selection, Genetic; Serial Passage | 2008 |
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
Topics: Darunavir; HIV Protease; HIV Protease Inhibitors; HIV-2; Humans; Inhibitory Concentration 50; Lopinavir; Microbial Sensitivity Tests; Phenotype; Pyrimidinones; Saquinavir; Sulfonamides | 2008 |
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Topics: Boron Compounds; Crystallography, X-Ray; Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Metals; Models, Molecular; Molecular Structure; Mutation | 2008 |
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.
Topics: Antiviral Agents; Cell Survival; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Ethers, Cyclic; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Hydrogen Bonding; Ligands; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Polyesters; Stereoisomerism; Structure-Activity Relationship; T-Lymphocytes; Water | 2008 |
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Topics: Binding Sites; Carbamates; Darunavir; Furans; HIV Protease Inhibitors; HIV-1; Kinetics; Models, Molecular; Molecular Structure; Sulfonamides | 2008 |
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
Topics: Amino Acid Sequence; Carbamates; Cyclopentanes; Dose-Response Relationship, Drug; Drug Resistance, Viral; Furans; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Molecular Structure; Sulfonamides | 2009 |
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.
Topics: Anti-HIV Agents; Cell Line; Crystallography, X-Ray; Drug Design; Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Macrocyclic Compounds; Models, Molecular; Molecular Conformation; Mutation | 2009 |
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.
Topics: Alcohols; Antiviral Agents; Crystallography, X-Ray; HIV Protease; HIV Protease Inhibitors; HIV-1; Inhibitory Concentration 50; Molecular Mimicry; Mutation, Missense | 2010 |
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
Topics: Animals; Antimalarials; Darunavir; Erythrocytes; HIV Protease Inhibitors; Humans; Life Cycle Stages; Parasitic Sensitivity Tests; Plasmodium falciparum; Pyridines; Pyrones; Sulfonamides | 2010 |
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
Topics: Cell Line; Dimerization; Drug Resistance, Multiple, Viral; Furans; Genetic Variation; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Macrocyclic Compounds; Microbial Sensitivity Tests; Models, Molecular; Structure-Activity Relationship; Virus Replication | 2010 |
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
Topics: Antiviral Agents; Carbamates; Darunavir; Furans; HIV Protease; HIV Protease Inhibitors; Humans; Indinavir; Lopinavir; Mutation; Pyrimidinones; Sulfonamides | 2010 |
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
Topics: Cell Line; Drug Resistance, Viral; Enzyme-Linked Immunosorbent Assay; gag Gene Products, Human Immunodeficiency Virus; HIV Antigens; HIV Protease Inhibitors; HIV-1; Humans; Mutagenesis, Site-Directed; Virus Replication | 2011 |
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
Topics: Carbamates; Catalytic Domain; Cell Line; Crystallography, X-Ray; Drug Resistance, Multiple, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Models, Molecular; Protein Binding; Stereoisomerism; Structure-Activity Relationship; Sulfonamides | 2011 |
Design of HIV-1 protease inhibitors with C3-substituted hexahydrocyclopentafuranyl urethanes as P2-ligands: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.
Topics: Amino Acid Substitution; Binding Sites; Biocatalysis; Cell Line; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Models, Chemical; Models, Molecular; Molecular Structure; Mutation; Protein Binding; Protein Structure, Tertiary; Structure-Activity Relationship; Urethane | 2011 |
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
Topics: Anti-HIV Agents; CCR5 Receptor Antagonists; Daphne; Diterpenes; Heterocyclic Compounds, 4 or More Rings; Mediterranean Region; Molecular Structure; Receptors, CXCR4 | 2012 |
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Topics: Binding Sites; Calorimetry, Differential Scanning; Carbamates; Crystallization; Darunavir; Drug Resistance, Multiple; Drug Resistance, Viral; Escherichia coli; Furans; Genes, Synthetic; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Models, Molecular; Mutation; Pyrrolidinones; Structure-Activity Relationship; Sulfonamides | 2013 |
Highly potent HIV-1 protease inhibitors with novel tricyclic P2 ligands: design, synthesis, and protein-ligand X-ray studies.
Topics: Crystallography, X-Ray; HIV Protease; HIV Protease Inhibitors; Ligands; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular | 2013 |
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
Topics: Benzothiazoles; Crystallography, X-Ray; Drug Design; Drug Resistance, Multiple, Viral; Furans; HIV Infections; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Molecular Docking Simulation; Pyrans; Structure-Activity Relationship; Sulfonamides | 2017 |
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
Topics: Catalytic Domain; Crystallography, X-Ray; Drug Design; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Models, Molecular; Molecular Structure; Protein Conformation; Stereoisomerism; Structure-Activity Relationship | 2018 |
Design, synthesis, and X-ray studies of potent HIV-1 protease inhibitors incorporating aminothiochromane and aminotetrahydronaphthalene carboxamide derivatives as the P2 ligands.
Topics: Antiviral Agents; Chromans; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; HIV; HIV Protease; HIV Protease Inhibitors; Ligands; Models, Molecular; Molecular Structure; Naphthalenes; Structure-Activity Relationship | 2018 |
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
Topics: Catalytic Domain; Chemistry Techniques, Synthetic; Drug Design; HIV Protease; HIV Protease Inhibitors; HIV-1; Ligands; Models, Molecular; Oxazolidinones; Stereoisomerism; Structure-Activity Relationship | 2018 |
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
Topics: Amino Acid Substitution; Catalytic Domain; Cell Line, Tumor; Crystallography, X-Ray; Drug Design; Furans; Heterocyclic Compounds, Bridged-Ring; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Protein Binding; Stereoisomerism | 2020 |
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries | 2023 |
Inhibition of HIV-2 protease by HIV-1 protease inhibitors in clinical use.
Topics: Darunavir; HIV Protease; HIV Protease Inhibitors; Hydrogen Bonding; Kinetics; Lopinavir; Pyridines; Pyrimidinones; Pyrones; Saquinavir; Structure-Activity Relationship; Substrate Specificity; Sulfonamides | 2008 |
Effect of flap mutations on structure of HIV-1 protease and inhibition by saquinavir and darunavir.
Topics: Crystallography, X-Ray; Darunavir; Dimerization; Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; Kinetics; Models, Molecular; Mutation; Protein Structure, Quaternary; Protein Structure, Tertiary; Saquinavir; Sulfonamides | 2008 |
Interactions of different inhibitors with active-site aspartyl residues of HIV-1 protease and possible relevance to pepsin.
Topics: Atazanavir Sulfate; Binding Sites; Binding, Competitive; Calorimetry, Differential Scanning; Carbamates; Crystallography, X-Ray; Darunavir; Furans; HIV Protease; HIV Protease Inhibitors; Humans; Indinavir; Kinetics; Lopinavir; Models, Molecular; Molecular Structure; Mutation; Nelfinavir; Oligopeptides; Pepsin A; Protein Binding; Protein Structure, Tertiary; Pyridines; Pyrimidinones; Pyrones; Ritonavir; Saquinavir; Sulfonamides | 2009 |
The influence of aged garlic extract on the uptake of saquinavir and darunavir into HepG2 cells and rat liver slices.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Darunavir; Duodenum; Garlic; Hep G2 Cells; Herb-Drug Interactions; HIV Protease Inhibitors; Humans; Liver; Male; Membrane Transport Proteins; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Plant Extracts; Rats; Rats, Wistar; Ritonavir; Saquinavir; Sulfonamides | 2010 |
HIV-1 protease mutations and protease inhibitor cross-resistance.
Topics: Atazanavir Sulfate; Carbamates; Darunavir; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Indinavir; Least-Squares Analysis; Lopinavir; Mutation; Nelfinavir; Oligopeptides; Organophosphates; Polymorphism, Genetic; Pyridines; Pyrimidinones; Pyrones; Saquinavir; Sulfonamides | 2010 |
Impact of drug transporters on cellular resistance towards saquinavir and darunavir.
Topics: Anti-Retroviral Agents; Biological Transport; Cell Line; Darunavir; Drug Resistance, Viral; Gene Expression; Gene Expression Profiling; Humans; Membrane Transport Proteins; Multidrug Resistance-Associated Protein 2; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Saquinavir; Sulfonamides | 2010 |
Garlic flavonoids and organosulfur compounds: impact on the hepatic pharmacokinetics of saquinavir and darunavir.
Topics: Animals; Anti-Retroviral Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Darunavir; Flavonoids; Garlic; Hepatocytes; Humans; Liver; Male; Microsomes, Liver; Plant Extracts; Rats; Rats, Wistar; Saquinavir; Sulfonamides | 2010 |
HIV protease inhibitors: garlic supplements and first-pass intestinal metabolism impact on the therapeutic efficacy.
Topics: Animals; Anti-HIV Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Caco-2 Cells; Cytochrome P-450 CYP3A; Darunavir; Dietary Supplements; Drug Interactions; Enterocytes; Garlic; HIV Protease Inhibitors; Humans; Intestinal Absorption; Intestinal Mucosa; Jejunum; Male; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Plant Extracts; Rats; Rats, Wistar; Ritonavir; Saquinavir; Sulfonamides | 2010 |
In vitro activity of antiretroviral drugs against Plasmodium falciparum.
Topics: Alkynes; Animals; Anti-Retroviral Agents; Antimalarials; Benzoxazines; Carbamates; Cyclopropanes; Darunavir; Furans; Lopinavir; Nelfinavir; Nevirapine; Plasmodium falciparum; Pyridines; Pyrones; Ritonavir; Saquinavir; Sulfonamides | 2011 |
Critical differences in HIV-1 and HIV-2 protease specificity for clinical inhibitors.
Topics: Amino Acid Sequence; Binding Sites; Carbamates; Crystallography, X-Ray; Darunavir; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; HIV-2; Kinetics; Saquinavir; Sulfonamides | 2012 |
Activity of human immunodeficiency virus type 1 protease inhibitors against the initial autocleavage in Gag-Pol polyprotein processing.
Topics: Cell Line; Darunavir; Gene Products, gag; Gene Products, pol; HIV Protease Inhibitors; HIV-1; Humans; Saquinavir; Sulfonamides | 2012 |
A contribution to the drug resistance mechanism of darunavir, amprenavir, indinavir, and saquinavir complexes with HIV-1 protease due to flap mutation I50V: a systematic MM-PBSA and thermodynamic integration study.
Topics: Anti-HIV Agents; Carbamates; Cluster Analysis; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Hydrogen Bonding; Indinavir; Molecular Dynamics Simulation; Mutation; Protein Conformation; Saquinavir; Sulfonamides; Thermodynamics | 2013 |
GRL-04810 and GRL-05010, difluoride-containing nonpeptidic HIV-1 protease inhibitors (PIs) that inhibit the replication of multi-PI-resistant HIV-1 in vitro and possess favorable lipophilicity that may allow blood-brain barrier penetration.
Topics: Animals; Astrocytes; Atazanavir Sulfate; Blood-Brain Barrier; Carbamates; Cell Line; Darunavir; Drug Resistance, Multiple, Viral; Endothelial Cells; Fluorides; Haplorhini; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Hydrophobic and Hydrophilic Interactions; Lopinavir; Models, Biological; Molecular Docking Simulation; Oligopeptides; Pericytes; Pyridines; Rats; Saquinavir; Sulfonamides; T-Lymphocytes; Virus Replication | 2013 |
Protease Inhibitors, Saquinavir and Darunavir, Inhibit Oligodendrocyte Maturation: Implications for Lysosomal Stress.
Topics: Animals; Apoptosis; Cell Differentiation; Cells, Cultured; Darunavir; Depression, Chemical; Dose-Response Relationship, Drug; Endosomes; HIV Protease Inhibitors; Hydrogen-Ion Concentration; Lysosomes; Myelin Proteins; Oligodendroglia; Oxidative Stress; Phthalimides; Quinolines; Rats; Rats, Sprague-Dawley; Saquinavir; Transient Receptor Potential Channels | 2021 |
Molecular Docking and Virtual Screening Based Prediction of Drugs for COVID-19.
Topics: Antiviral Agents; Benzazepines; COVID-19; COVID-19 Drug Treatment; Cyclopropanes; Darunavir; Drug Evaluation, Preclinical; Drug Repositioning; High-Throughput Screening Assays; Humans; Indoles; Isoindoles; Lactams, Macrocyclic; Molecular Docking Simulation; Proline; Saquinavir; SARS-CoV-2; Sulfonamides | 2021 |
Drug binding dynamics of the dimeric SARS-CoV-2 main protease, determined by molecular dynamics simulation.
Topics: Betacoronavirus; Binding Sites; Biophysical Phenomena; Catalytic Domain; Computational Biology; Coronavirus 3C Proteases; Coronavirus Infections; COVID-19; Cysteine Endopeptidases; Darunavir; Drug Repositioning; HIV Protease Inhibitors; Humans; Indinavir; Lopinavir; Molecular Dynamics Simulation; Nelfinavir; Pandemics; Pneumonia, Viral; Ritonavir; Saquinavir; SARS-CoV-2; Viral Nonstructural Proteins | 2020 |