darunavir has been researched along with amprenavir in 61 studies
| Studies (darunavir) | Trials (darunavir) | Recent Studies (post-2010) (darunavir) | Studies (amprenavir) | Trials (amprenavir) | Recent Studies (post-2010) (amprenavir) |
|---|---|---|---|---|---|
| 1,148 | 224 | 780 | 555 | 91 | 94 |
| Protein | Taxonomy | darunavir (IC50) | amprenavir (IC50) |
|---|---|---|---|
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 (BRU ISOLATE) | 0.027 | |
| Gag-Pol polyprotein | Human immunodeficiency virus type 2 (ISOLATE ROD) | 0.0026 | |
| Gag polyprotein | HIV-1 M:B_MN | 0.013 | |
| Cytochrome P450 3A4 | Homo sapiens (human) | 1 | |
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | 0.0558 | |
| Thromboxane-A synthase | Homo sapiens (human) | 6.727 | |
| Protease | Human immunodeficiency virus 1 | 0.1553 |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (1.64) | 18.2507 |
| 2000's | 27 (44.26) | 29.6817 |
| 2010's | 32 (52.46) | 24.3611 |
| 2020's | 1 (1.64) | 2.80 |
| Authors | Studies |
|---|---|
| Buthod, J; Cho, H; Cho, W; Ghosh, AK; Holland, L; Hussain, KA; Kincaid, JF; Koo, Y; Krishnan, K; Rudall, C; Walters, DE | 1 |
| Azijn, H; de Bethune, MP; de Kock, HA; De Meyer, S; Jonckers, TH; King, NM; Pauwels, R; Peeters, A; Pille, GM; Prabu-Jeyabalan, M; Schiffer, CA; Surleraux, DL; Tahri, A; Verschueren, WG; Wigerinck, PB | 1 |
| 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 |
| Boone, L; Craig, C; Ferris, R; Furfine, E; Griffin, P; Hale, M; Hanlon, M; Harvey, R; Hazen, R; Kaldor, I; Miller, J; Ray, J; Samano, V; Spaltenstein, A; St Clair, M; Tung, R; Yates, P | 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 |
| Anderson, DD; Baldridge, A; Ghosh, AK; Koh, Y; Leshchenko-Yashchuk, S; Miller, HB; Mitsuya, H; Noetzel, M; Tie, Y; Wang, YF; Weber, IT | 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 |
| Amano, M; Baldridge, A; Gemma, S; Ghosh, AK; Ide, K; Koh, Y; Mitsuya, H; Simoni, E; Tojo, Y; Walters, DE | 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 |
| Boross, PI; Chiu, TY; Ghosh, AK; Harrison, RW; Louis, JM; Tie, Y; Tozser, J; Wang, YF; Weber, IT | 1 |
| Ali, A; Cao, H; Huggins, DJ; Nalam, MN; Parai, MK; Rana, TM; Schiffer, CA; Tidor, B | 1 |
| Bandaranayake, RM; Haliloğlu, T; King, NM; Nalam, MN; Nalivaika, EA; Özen, A; Prabu-Jeyabalan, M; Schiffer, CA; Yilmaz, NK | 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 |
| Ali, A; Altman, MD; Cao, H; Nalam, MN; Rana, TM; Schiffer, CA; Shen, Y; Tidor, B | 1 |
| Agniswamy, J; Amano, M; Ghosh, AK; Mitsuya, H; Osswald, HL; Wang, YF; Weber, IT; Yu, X | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Agniswamy, J; Aoki, M; Ghosh, AK; Glauninger, K; Hayashi, H; Mitsuya, H; Osswald, HL; 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 |
| Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M | 1 |
| Bilcer, G; Boross, P; Devasamudram, T; Gaddis, L; Ghosh, AK; Harrison, RW; Kincaid, JF; Koh, Y; Maeda, K; Mitsuya, H; Nakata, H; Ogata, H; Tie, Y; Volarath, P; Wang, YF; Weber, IT | 1 |
| de Béthune, MP; King, NM; Nalivaika, EA; Prabu-Jeyabalan, M; Schiffer, CA; Wigerinck, P | 1 |
| Berthé, H; de Truchis, P; Delaugerre, C; Galperine, T; Long, K; Mathez, D; Peytavin, G | 1 |
| Adams, E; Hoogmartens, J; Van Schepdael, A; Yekkala, R | 1 |
| de Béthune, MP; De Meyer, S; Picchio, G | 1 |
| Bruzzone, B; Cenderello, G; Dentone, C; Di Biagio, A; Ferrea, G; Icardi, G; Mularoni, A; Rosso, R; Viscoli, C | 1 |
| Ali, A; Altman, MD; Anjum, SG; Cao, H; Chellappan, S; Fernandes, MX; Gilson, MK; Kairys, V; Nalam, MN; Rana, TM; Reddy, GS; Schiffer, CA; Tidor, B | 1 |
| Louis, JM; Sayer, JM | 1 |
| Hidalgo Tenorio, C; Pasquau Liaño, J | 1 |
| Agniswamy, J; Amano, M; Aoki, M; Baldridge, A; Ghosh, AK; Miguel, SG; Mitsuya, H; Rao, KV; Wang, YF; Weber, IT; Xu, CX | 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 |
| Bandaranayake, RM; King, NM; Mittal, S; Nalam, MN; Nalivaika, EA; Prabu-Jeyabalan, M; Schiffer, CA; Yilmaz, NK | 1 |
| Amano, M; Aoki, M; Campbell, JR; Das, D; Ghosh, AK; Mitsuya, H; Rao, KV; Salcedo-Gómez, PM; Tojo, Y; Xu, CX | 1 |
| Leonis, G; Papadopoulos, MG; Steinbrecher, T | 1 |
| Chen, J; Liang, Z; Wang, W; Yi, C; Zhang, Q; Zhang, S | 1 |
| Amano, M; Das, D; Ghosh, AK; Mitsuya, H; Nyalapatla, PR; Parham, GL; Salcedo-Gómez, PM; Tojo, Y | 1 |
| Shao, Q; Shi, J; Wang, J; Yu, Y; Zhu, W | 1 |
| Raines, RT; Windsor, IW | 1 |
| Alibés, A; Gil, V; Guallar, V; Hosseini, A; Noguera-Julian, M; Orozco, M; Paredes, R; Soliva, R | 1 |
| Amano, M; Bulut, H; Das, D; Delino, NS; Ghosh, AK; Mitsuya, H; Salcedo-Gómez, PM; Sheri, VR; Yedidi, RS; Zhao, R | 1 |
| Camproux, AC; Cano Contreras, ME; Descamps, D; Flatters, D; Regad, L; Triki, D; Visseaux, B | 1 |
| Chen, J; Peng, C; Wang, J; Zhu, W | 1 |
5 review(s) available for darunavir and amprenavir
| 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 |
Response to "key amprenavir resistance mutations counteract dramatic efficacy of darunavir in highly experienced patients".
Topics: Carbamates; Darunavir; Drug Resistance, Viral; Furans; HIV; HIV Infections; HIV Protease Inhibitors; Humans; Sulfonamides; Treatment Outcome | 2008 |
[Chemical characteristics, mechanism of action and antiviral activity of darunavir].
Topics: Administration, Oral; Carbamates; Clinical Trials as Topic; Cytochrome P-450 CYP3A; Darunavir; Drug Interactions; Drug Resistance, Viral; Drug Therapy, Combination; Female; Furans; HIV; HIV Infections; HIV Protease Inhibitors; Humans; Male; Molecular Structure; Ritonavir; Sulfonamides | 2008 |
1 trial(s) available for darunavir and amprenavir
| Article | Year |
|---|---|
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 |
55 other study(ies) available for darunavir and amprenavir
| Article | Year |
|---|---|
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Topics: Cell Line; Drug Design; HIV Protease Inhibitors; Humans; Ligands; Models, Chemical; Saquinavir; Sulfonamides | 1998 |
Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.
Topics: Administration, Oral; Animals; Biological Availability; Cell Line; Crystallography, X-Ray; Darunavir; Dogs; Drug Resistance, Multiple, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; In Vitro Techniques; Microsomes, Liver; Models, Molecular; Molecular Conformation; Mutation; Rats; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Thermodynamics | 2005 |
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 |
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Topics: Algorithms; Anti-Retroviral Agents; Benzodioxoles; Blood Proteins; Carbamates; Cell Line; Drug Resistance, Viral; HeLa Cells; HIV Protease Inhibitors; HIV-1; Humans; Orosomucoid; Phenotype; Serum; Serum Albumin; Tyrosine | 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 of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
Topics: Binding Sites; Crystallography, X-Ray; Drug Design; HIV Protease Inhibitors; Ligands; Oxazolidinones; Protein Binding; Pyrrolidinones; Structure-Activity Relationship | 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 |
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
Topics: Animals; Cricetinae; Crystallography, X-Ray; Drug Evaluation, Preclinical; Furans; HIV Protease; HIV Protease Inhibitors; Humans; Ligands; Phenylbutyrates; Protein Binding; Stereoisomerism | 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 |
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 |
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.
Topics: Chemistry Techniques, Synthetic; Crystallography, X-Ray; Drug Design; Drug Resistance, Multiple; Drug Resistance, Viral; HIV Protease; HIV Protease Inhibitors; HIV-1; Models, Molecular; Protein Conformation; Structure-Activity Relationship | 2012 |
Extreme entropy-enthalpy compensation in a drug-resistant variant of HIV-1 protease.
Topics: Catalytic Domain; Crystallography, X-Ray; Drug Resistance, Viral; Entropy; HIV Protease; HIV Protease Inhibitors; HIV-1; Models, Molecular; Mutation; Protein Binding; Thermodynamics | 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 |
Testing the substrate-envelope hypothesis with designed pairs of compounds.
Topics: Computer Simulation; Crystallography, X-Ray; Drug Resistance, Viral; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Models, Molecular; Mutation; Substrate Specificity; Viral Structural Proteins | 2013 |
Structure-based design of potent HIV-1 protease inhibitors with modified P1-biphenyl ligands: synthesis, biological evaluation, and enzyme-inhibitor X-ray structural studies.
Topics: Binding Sites; Biphenyl Compounds; Carbamates; Crystallography, X-Ray; Drug Design; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Models, Molecular; Molecular Dynamics Simulation; Molecular Structure; Protein Conformation; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Urethane | 2015 |
Probing Lipophilic Adamantyl Group as the P1-Ligand for HIV-1 Protease Inhibitors: Design, Synthesis, Protein X-ray Structural Studies, and Biological Evaluation.
Topics: Adamantane; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; HIV Protease; HIV Protease Inhibitors; Hydrophobic and Hydrophilic Interactions; Ligands; Models, Molecular; Molecular Structure; Structure-Activity Relationship | 2016 |
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 |
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 |
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
Topics: Amino Acid Substitution; Antiviral Agents; Carbamates; CD4-Positive T-Lymphocytes; Cell Line; Crystallography, X-Ray; Darunavir; Drug Resistance, Multiple, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Models, Molecular; Sulfonamides; Virus Replication | 2003 |
Structural and thermodynamic basis for the binding of TMC114, a next-generation human immunodeficiency virus type 1 protease inhibitor.
Topics: Binding Sites; Carbamates; Darunavir; Drug Resistance, Multiple, Viral; Furans; HIV Protease Inhibitors; HIV-1; Humans; Hydrogen Bonding; Sulfonamides; Thermodynamics | 2004 |
Key amprenavir resistance mutations counteract dramatic efficacy of darunavir in highly experienced patients.
Topics: Carbamates; CD4 Lymphocyte Count; Darunavir; Drug Resistance, Viral; Drug Therapy, Combination; Furans; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Reverse Transcriptase Inhibitors; Risk Factors; Ritonavir; Sulfonamides; Treatment Failure; Viral Load | 2007 |
Different evidence of key amprenavir resistance mutations on the efficacy of darunavir.
Topics: Carbamates; Darunavir; Drug Resistance, Viral; Drug Therapy, Combination; Furans; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Mutation; Reverse Transcriptase Inhibitors; Ritonavir; Sulfonamides; Treatment Failure; Treatment Outcome | 2008 |
HIV-1 protease inhibitors from inverse design in the substrate envelope exhibit subnanomolar binding to drug-resistant variants.
Topics: Algorithms; Carbamates; Crystallography, X-Ray; Darunavir; Drug Design; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Kinetics; Models, Molecular; Structure-Activity Relationship; 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 |
Probing multidrug-resistance and protein-ligand interactions with oxatricyclic designed ligands in HIV-1 protease inhibitors.
Topics: Carbamates; Crystallography, X-Ray; Darunavir; Dimerization; Drug Design; Drug Resistance, Multiple, Viral; Furans; Heterocyclic Compounds, 3-Ring; HIV Infections; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Ligands; Proteins; Structure-Activity Relationship; 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 |
Structural and thermodynamic basis of amprenavir/darunavir and atazanavir resistance in HIV-1 protease with mutations at residue 50.
Topics: Anti-HIV Agents; Atazanavir Sulfate; Carbamates; Crystallography, X-Ray; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV-1; Humans; Kinetics; Models, Molecular; Mutant Proteins; Mutation, Missense; Oligopeptides; Point Mutation; Protein Binding; Protein Conformation; Pyridines; Sulfonamides; Thermodynamics | 2013 |
GRL-0519, a novel oxatricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor (PI), potently suppresses replication of a wide spectrum of multi-PI-resistant HIV-1 variants in vitro.
Topics: Amino Acid Sequence; Atazanavir Sulfate; Binding Sites; Carbamates; Cell Line, Tumor; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Lopinavir; Molecular Docking Simulation; Molecular Sequence Data; Oligopeptides; Protein Binding; Pyridines; Ritonavir; Structure-Activity Relationship; Sulfonamides; T-Lymphocytes; Virus Replication | 2013 |
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 |
Revealing origin of decrease in potency of darunavir and amprenavir against HIV-2 relative to HIV-1 protease by molecular dynamics simulations.
Topics: Carbamates; Catalytic Domain; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; HIV-2; Hydrogen Bonding; Molecular Dynamics Simulation; Protein Binding; Protein Structure, Secondary; Sulfonamides; Thermodynamics | 2014 |
A novel tricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor, GRL-0739, effectively inhibits the replication of multidrug-resistant HIV-1 variants and has a desirable central nervous system penetration property in vitro.
Topics: Blood-Brain Barrier; Carbamates; Darunavir; Drug Resistance, Multiple, Viral; Drug Resistance, Viral; Furans; HIV Protease Inhibitors; HIV-1; Humans; Sulfonamides; Virus Replication | 2015 |
Effects of drug-resistant mutations on the dynamic properties of HIV-1 protease and inhibition by Amprenavir and Darunavir.
Topics: Binding Sites; Carbamates; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Hydrogen Bonding; Hydrophobic and Hydrophilic Interactions; Molecular Dynamics Simulation; Mutation; Protein Binding; Protein Structure, Tertiary; Sulfonamides; Thermodynamics | 2015 |
Fluorogenic Assay for Inhibitors of HIV-1 Protease with Sub-picomolar Affinity.
Topics: Carbamates; Darunavir; Fluorescence; Fluorescent Dyes; Furans; HIV Infections; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Kinetics; Pyridines; Pyrones; Sulfonamides | 2015 |
Computational Prediction of HIV-1 Resistance to Protease Inhibitors.
Topics: Amino Acid Sequence; Carbamates; Computational Biology; Darunavir; Drug Evaluation, Preclinical; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Models, Molecular; Mutation; Protein Multimerization; Protein Structure, Quaternary; Sulfonamides | 2016 |
A Modified P1 Moiety Enhances In Vitro Antiviral Activity against Various Multidrug-Resistant HIV-1 Variants and In Vitro Central Nervous System Penetration Properties of a Novel Nonpeptidic Protease Inhibitor, GRL-10413.
Topics: Animals; Blood-Brain Barrier; Carbamates; Cell Line; Central Nervous System; Crystallography, X-Ray; Darunavir; Drug Evaluation, Preclinical; Drug Resistance, Multiple, Viral; Ethylamines; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Lopinavir; Microbial Sensitivity Tests; Peptides; Rats; Structure-Activity Relationship; Sulfonamides; Virus Replication | 2016 |
Analysis of the HIV-2 protease's adaptation to various ligands: characterization of backbone asymmetry using a structural alphabet.
Topics: Carbamates; Crystallography, X-Ray; Darunavir; Enzyme Inhibitors; Furans; HIV Protease; Protein Binding; Protein Conformation; Protein Subunits; Sulfonamides | 2018 |
Exploring molecular mechanism of allosteric inhibitor to relieve drug resistance of multiple mutations in HIV-1 protease by enhanced conformational sampling.
Topics: Allosteric Regulation; Binding Sites; Carbamates; Darunavir; Drug Resistance, Viral; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Hydrogen Bonding; Molecular Dynamics Simulation; Mutation; Protein Binding; Protein Conformation; Sulfonamides; Thermodynamics | 2018 |