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Inhibitors of HIV‑1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir

Journal of medicinal chemistry, 2018-01, Vol.61 (1), p.62-80

2018

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EDP-938, a novel nucleoprotein inhibitor of respiratory syncytial virus, demonstrates potent antiviral activities in vitro and in a non-human primate model

PLoS pathogens, 2021-03, Vol.17 (3), p.e1009428-e1009428

2021

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Prevalence of gp160 polymorphisms known to be related to decreased susceptibility to temsavir in different subtypes of HIV-1 in the Los Alamos National Laboratory HIV Sequence Database

Journal of antimicrobial chemotherapy, 2021-11, Vol.76 (11), p.2958-2964

2021

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Activity of the HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068, against CD4-Independent Viruses and HIV-1 Envelopes Resistant to Other Entry Inhibitors

Antimicrobial Agents and Chemotherapy, 2013-09, Vol.57 (9), p.4172-4180

2013

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Resistance profile of the HIV-1 maturation inhibitor GSK3532795 in vitro and in a clinical study

PloS one, 2019-10, Vol.14 (10), p.e0224076-e0224076

2019

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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, 2019-04, Vol.62 (7), p.3553-3574

2019

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Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV‑1 Integrase Inhibitors

Journal of medicinal chemistry, 2020-03, Vol.63 (5), p.2620-2637

2020

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Homology models of the HIV-1 attachment inhibitor BMS-626529 bound to gp120 suggest a unique mechanism of action

Proteins, structure, function, and bioinformatics, 2015-02, Vol.83 (2), p.331-350

2015

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In Vitro Antiviral Characteristics of HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068

Antimicrobial Agents and Chemotherapy, 2012-07, Vol.56 (7), p.3498-3507

2012

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Prevalence and clinical significance of HIV drug resistance mutations by ultra-deep sequencing in antiretroviral-naïve subjects in the CASTLE study

PloS one, 2010-06, Vol.5 (6), p.e10952-e10952

2010

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(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration

European journal of medicinal chemistry, 2020-12, Vol.207, p.112749, Article 112749

2020

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Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (22), p.127531-127531, Article 127531

2020

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The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor

Bioorganic & medicinal chemistry letters, 2018-07, Vol.28 (12), p.2124-2130

2018

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Mechanistic Studies and Modeling Reveal the Origin of Differential Inhibition of Gag Polymorphic Viruses by HIV-1 Maturation Inhibitors

PLoS pathogens, 2016-11, Vol.12 (11), p.e1005990-e1005990

2016

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Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

Bioorganic & medicinal chemistry letters, 2015-02, Vol.25 (3), p.717-720

2015

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Antiviral Activity, Pharmacokinetics, and Safety of BMS-488043, a Novel Oral Small-Molecule HIV-1 Attachment Inhibitor, in HIV-1-Infected Subjects

Antimicrobial Agents and Chemotherapy, 2011-02, Vol.55 (2), p.722-728

2011

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In Vitro Cross-Resistance Profile of Nucleoside Reverse Transcriptase Inhibitor (NRTI) BMS-986001 against Known NRTI Resistance Mutations

Antimicrobial Agents and Chemotherapy, 2013-11, Vol.57 (11), p.5500-5508

2013

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Influenza Nucleoprotein: Promising Target for Antiviral Chemotherapy

Antiviral Chemistry and Chemotherapy, 2013-06, Vol.23 (3), p.77-91

2013

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In Vivo Patterns of Resistance to the HIV Attachment Inhibitor BMS-488043

Antimicrobial Agents and Chemotherapy, 2011-02, Vol.55 (2), p.729-737

2011

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The Terminal (Catalytic) Adenosine of the HIV LTR Controls the Kinetics of Binding and Dissociation of HIV Integrase Strand Transfer Inhibitors

Biochemistry (Easton), 2008-12, Vol.47 (51), p.13481-13488

2008

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Biochemical Analysis of HIV-1 Integrase Variants Resistant to Strand Transfer Inhibitors

The Journal of biological chemistry, 2008-08, Vol.283 (35), p.23599-23609

2008

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Targeting a Binding Pocket within the Trimer-of-Hairpins: Small-Molecule Inhibition of Viral Fusion

Proceedings of the National Academy of Sciences - PNAS, 2004-10, Vol.101 (42), p.15046-15051

2004

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Orally Active Fusion Inhibitor of Respiratory Syncytial Virus

Antimicrobial Agents and Chemotherapy, 2004-02, Vol.48 (2), p.413-422

2004

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Changes to the HIV Long Terminal Repeat and to HIV Integrase Differentially Impact HIV Integrase Assembly, Activity, and the Binding of Strand Transfer Inhibitors

The Journal of biological chemistry, 2007-10, Vol.282 (43), p.31186-31196

2007

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Oral Efficacy of a Respiratory Syncytial Virus Inhibitor in Rodent Models of Infection

Antimicrobial Agents and Chemotherapy, 2004-07, Vol.48 (7), p.2448-2454

2004

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Inhibitors of HIV‑1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir

EDP-938, a novel nucleoprotein inhibitor of respiratory syncytial virus, demonstrates potent antiviral activities in vitro and in a non-human primate model

Prevalence of gp160 polymorphisms known to be related to decreased susceptibility to temsavir in different subtypes of HIV-1 in the Los Alamos National Laboratory HIV Sequence Database

Activity of the HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068, against CD4-Independent Viruses and HIV-1 Envelopes Resistant to Other Entry Inhibitors

Resistance profile of the HIV-1 maturation inhibitor GSK3532795 in vitro and in a clinical study

Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV‑1 Protease Inhibitor Atazanavir

Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV‑1 Integrase Inhibitors

Homology models of the HIV-1 attachment inhibitor BMS-626529 bound to gp120 suggest a unique mechanism of action

In Vitro Antiviral Characteristics of HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068

Prevalence and clinical significance of HIV drug resistance mutations by ultra-deep sequencing in antiretroviral-naïve subjects in the CASTLE study

(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration

Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase

The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor

Mechanistic Studies and Modeling Reveal the Origin of Differential Inhibition of Gag Polymorphic Viruses by HIV-1 Maturation Inhibitors

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

Antiviral Activity, Pharmacokinetics, and Safety of BMS-488043, a Novel Oral Small-Molecule HIV-1 Attachment Inhibitor, in HIV-1-Infected Subjects

In Vitro Cross-Resistance Profile of Nucleoside Reverse Transcriptase Inhibitor (NRTI) BMS-986001 against Known NRTI Resistance Mutations

Influenza Nucleoprotein: Promising Target for Antiviral Chemotherapy

In Vivo Patterns of Resistance to the HIV Attachment Inhibitor BMS-488043

The Terminal (Catalytic) Adenosine of the HIV LTR Controls the Kinetics of Binding and Dissociation of HIV Integrase Strand Transfer Inhibitors

Biochemical Analysis of HIV-1 Integrase Variants Resistant to Strand Transfer Inhibitors

Targeting a Binding Pocket within the Trimer-of-Hairpins: Small-Molecule Inhibition of Viral Fusion

Orally Active Fusion Inhibitor of Respiratory Syncytial Virus

Changes to the HIV Long Terminal Repeat and to HIV Integrase Differentially Impact HIV Integrase Assembly, Activity, and the Binding of Strand Transfer Inhibitors

Oral Efficacy of a Respiratory Syncytial Virus Inhibitor in Rodent Models of Infection

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