Page last updated: 2024-08-07 13:50:07
Protease
[no definition available]
Synonyms
Research
Bioassay Publications (85)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (1.18) | 18.2507 |
| 2000's | 27 (31.76) | 29.6817 |
| 2010's | 53 (62.35) | 24.3611 |
| 2020's | 4 (4.71) | 2.80 |
Compounds (41)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nelfinavir | Human immunodeficiency virus 1 | Kd | 0.0147 | 3 | 3 |
| lopinavir | Human immunodeficiency virus 1 | EC50 | 1.1600 | 1 | 1 |
| lopinavir | Human immunodeficiency virus 1 | Kd | 0.0006 | 2 | 2 |
| atazanavir | Human immunodeficiency virus 1 | EC50 | 0.0007 | 1 | 1 |
| darunavir | Human immunodeficiency virus 1 | EC50 | 0.0624 | 2 | 2 |
| darunavir | Human immunodeficiency virus 1 | Kd | 0.0000 | 1 | 1 |
| ritonavir | Human immunodeficiency virus 1 | EC50 | 0.1500 | 1 | 1 |
| saquinavir | Human immunodeficiency virus 1 | Kd | 0.0018 | 3 | 3 |
| je 2147 | Human immunodeficiency virus 1 | EC50 | 2.7300 | 1 | 1 |
| indinavir sulfate | Human immunodeficiency virus 1 | Kd | 0.0027 | 3 | 3 |
| streptomyces pepsin inhibitor | Human immunodeficiency virus 1 | Kd | 3.0390 | 3 | 3 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nelfinavir | Human immunodeficiency virus 1 | Km | 15.0000 | 1 | 1 |
| amprenavir | Human immunodeficiency virus 1 | IC90 | 0.0400 | 1 | 1 |
| amprenavir | Human immunodeficiency virus 1 | K | 0.0004 | 1 | 1 |
| darunavir | Human immunodeficiency virus 1 | K | 0.0000 | 1 | 1 |
| pl 100 | Human immunodeficiency virus 1 | Activity | 0.0200 | 1 | 1 |
Oleanolic Acid Derivatives as Potential Inhibitors of HIV-1 Protease.Journal of natural products, , 10-25, Volume: 82, Issue:10, 2019
Semi-synthesis of acylated triterpenes from olive-oil industry wastes for the development of anticancer and anti-HIV agents.European journal of medicinal chemistry, , Mar-03, Volume: 74, 2014
Novel 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: the benzothiophene ring as an effective moiety.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: implications for the charge state of the protein ionogenic groups.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Synthesis of new thienyl ring containing HIV-1 protease inhibitors: promising preliminary pharmacological evaluation against recombinant HIV-1 proteases.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
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.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:9, 2007
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Rational approaches to improving selectivity in drug design.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease.European journal of medicinal chemistry, , Volume: 53, 2012
Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.ACS medicinal chemistry letters, , Jul-14, Volume: 7, Issue:7, 2016
Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease.European journal of medicinal chemistry, , Volume: 53, 2012
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
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.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.The Journal of biological chemistry, , Sep-28, Volume: 282, Issue:39, 2007
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
HIV-1 Protease Inhibitors Incorporating Stereochemically Defined P2' Ligands To Optimize Hydrogen Bonding in the Substrate Envelope.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Overview of Recent Strategic Advances in Medicinal Chemistry.Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
Design, synthesis and biological evaluation of novel HIV-1 protease inhibitors with pentacyclic triterpenoids as P2-ligands.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 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.Journal of medicinal chemistry, , 11-08, Volume: 61, Issue:21, 2018
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.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Design and synthesis of potent HIV-1 protease inhibitors with (S)-tetrahydrofuran-tertiary amine-acetamide as P2-ligand: Structure-activity studies and biological evaluation.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Design of HIV-1 Protease Inhibitors with Amino-bis-tetrahydrofuran Derivatives as P2-Ligands to Enhance Backbone-Binding Interactions: Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Substituted Bis-THF Protease Inhibitors with Improved Potency against Highly Resistant Mature HIV-1 Protease PR20.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Structure-based design, synthesis, X-ray studies, and biological evaluation of novel HIV-1 protease inhibitors containing isophthalamide-derived P2-ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 25, Issue:21, 2015
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Dual inhibitors for aspartic proteases HIV-1 PR and renin: advancements in AIDS-hypertension-diabetes linkage via molecular dynamics, inhibition assays, and binding free energy calculations.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.ACS medicinal chemistry letters, , Jun-09, Volume: 2, Issue:6, 2011
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
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.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
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.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:9, 2007
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.The Journal of biological chemistry, , Sep-28, Volume: 282, Issue:39, 2007
Design and synthesis of selenazole-substituted ritonavir analogs.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 28, Issue:14, 2018
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Rational approaches to improving selectivity in drug design.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: implications for the charge state of the protein ionogenic groups.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Synthesis of new thienyl ring containing HIV-1 protease inhibitors: promising preliminary pharmacological evaluation against recombinant HIV-1 proteases.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
3D-QSAR CoMFA/CoMSIA models based on theoretical active conformers of HOE/BAY-793 analogs derived from HIV-1 protease inhibitor complexes.European journal of medicinal chemistry, , Volume: 44, Issue:11, 2009
Design, synthesis, evaluation, and crystallographic-based structural studies of HIV-1 protease inhibitors with reduced response to the V82A mutation.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.The Journal of biological chemistry, , Sep-28, Volume: 282, Issue:39, 2007
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 20, Issue:14, 2010
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Applications of Fluorine in Medicinal Chemistry.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Structural basis for HTLV-1 protease inhibition by the HIV-1 protease inhibitor indinavir.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Design and synthesis of highly potent HIV-1 protease inhibitors with novel isosorbide-derived P2 ligands.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 24, Issue:11, 2014
Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: implications for the charge state of the protein ionogenic groups.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Design and synthesis of sulfoximine based inhibitors for HIV-1 protease.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 17, Issue:19, 2007
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
An allosteric modulator of HIV-1 protease shows equipotent inhibition of wild-type and drug-resistant proteases.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Modular construction of quaternary hemiaminal-based inhibitor candidates and their in cellulo assessment with HIV-1 protease.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Synthesis of dammarane-type triterpene derivatives and their ability to inhibit HIV and HCV proteases.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
On the inhibition of HIV-1 protease by hydrazino-ureas displaying the N-->C=O interaction.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program.Journal of natural products, , Volume: 64, Issue:2, 2001
Oleanolic Acid Derivatives as Potential Inhibitors of HIV-1 Protease.Journal of natural products, , 10-25, Volume: 82, Issue:10, 2019
Rational approaches to improving selectivity in drug design.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: implications for the charge state of the protein ionogenic groups.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Is quantum mechanics necessary for predicting binding free energy?Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
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.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:9, 2007
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.The Journal of biological chemistry, , Sep-28, Volume: 282, Issue:39, 2007
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Highly potent HIV-1 protease inhibitors with novel tricyclic P2 ligands: design, synthesis, and protein-ligand X-ray studies.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013