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Structural basis of second-generation HIV integrase inhibitor action and viral resistance

Science (American Association for the Advancement of Science), 2020-02, Vol.367 (6479), p.806-810

2020

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In Vitro Antiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor

Antimicrobial Agents and Chemotherapy, 2011-02, Vol.55 (2), p.813-821

2011

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Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8189-8206

2016

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Efficacies of Cabotegravir and Bictegravir against drug-resistant HIV-1 integrase mutants

Retrovirology, 2018-05, Vol.15 (1), p.37-37, Article 37

2018

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Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572)

Molecular pharmacology, 2011-10, Vol.80 (4), p.565-572

2011

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Advances in the development of HIV integrase strand transfer inhibitors

European journal of medicinal chemistry, 2021-12, Vol.225, p.113787-113787, Article 113787

2021

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Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs

Viruses, 2021-01, Vol.13 (2), p.205

2021

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Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance

Proceedings of the National Academy of Sciences - PNAS, 2010-11, Vol.107 (46), p.20057-20062

2010

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New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action

The Journal of biological chemistry, 2012-06, Vol.287 (25), p.21189-21203

2012

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Inhibiting the HIV Integration Process: Past, Present, and the Future

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.539-566

Di Santo, Roberto

2014

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Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV‑1 Integrase and Reverse Transcriptase Ribonuclease H Domain

Journal of medicinal chemistry, 2015-02, Vol.58 (4), p.1915-1928

2015

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Identification by Phage Display Selection of a Short Peptide Able To Inhibit Only the Strand Transfer Reaction Catalyzed by Human Immunodeficiency Virus Type 1 Integrase

Biochemistry (Easton), 2004-10, Vol.43 (41), p.13097-13105

2004

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Dolutegravir (S/GSK1349572) Exhibits Significantly Slower Dissociation than Raltegravir and Elvitegravir from Wild-Type and Integrase Inhibitor-Resistant HIV-1 Integrase-DNA Complexes

Antimicrobial Agents and Chemotherapy, 2011-10, Vol.55 (10), p.4552-4559

2011

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7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

Angewandte Chemie (International ed.), 2018-06, Vol.57 (24), p.7181-7185

International ed. in English, 2018

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Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization

Antimicrobial Agents and Chemotherapy, 2012-08, Vol.56 (8), p.4365-4374

2012

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Structural basis for strand-transfer inhibitor binding to HIV intasomes

Science (American Association for the Advancement of Science), 2020-02, Vol.367 (6479), p.810-814

2020

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Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors

Journal of medicinal chemistry, 2017-09, Vol.60 (17), p.7315-7332

2017

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Close‐up: HIV/SIV intasome structures shed new light on integrase inhibitor binding and viral escape mechanisms

The FEBS journal, 2021-01, Vol.288 (2), p.427-433

2021

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Chromenone derivatives as a versatile scaffold with dual mode of inhibition of HIV-1 reverse transcriptase-associated Ribonuclease H function and integrase activity

European journal of medicinal chemistry, 2019-11, Vol.182, p.111617, Article 111617

2019

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Design, synthesis and biological evaluation of imidazole and oxazole fragments as HIV-1 integrase-LEDGF/p75 disruptors and inhibitors of microbial pathogens

Bioorganic & medicinal chemistry, 2020-01, Vol.28 (1), p.115210, Article 115210

2020

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Computational design of small molecular modulators of protein–protein interactions with a novel thermodynamic cycle: Allosteric inhibitors of HIV‐1 integrase

Protein science, 2021-02, Vol.30 (2), p.438-447

2021

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Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors

Bioorganic & medicinal chemistry letters, 2020-02, Vol.30 (3), p.126784, Article 126784

2020

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Allosteric HIV Integrase Inhibitors Promote Formation of Inactive Branched Polymers via Homomeric Carboxy-Terminal Domain Interactions

Structure (London), 2021-03, Vol.29 (3), p.213-225.e5

2021

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Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity

Bioorganic & medicinal chemistry letters, 2023-06, Vol.89, p.129303-129303, Article 129303

2023

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A supramolecular assembly mediates lentiviral DNA integration

Science (American Association for the Advancement of Science), 2017-01, Vol.355 (6320), p.93-95

2017

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Structural basis of second-generation HIV integrase inhibitor action and viral resistance

In Vitro Antiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor

Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia

Efficacies of Cabotegravir and Bictegravir against drug-resistant HIV-1 integrase mutants

Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572)

Advances in the development of HIV integrase strand transfer inhibitors

Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs

Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance

New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action

Inhibiting the HIV Integration Process: Past, Present, and the Future

Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV‑1 Integrase and Reverse Transcriptase Ribonuclease H Domain

Identification by Phage Display Selection of a Short Peptide Able To Inhibit Only the Strand Transfer Reaction Catalyzed by Human Immunodeficiency Virus Type 1 Integrase

Dolutegravir (S/GSK1349572) Exhibits Significantly Slower Dissociation than Raltegravir and Elvitegravir from Wild-Type and Integrase Inhibitor-Resistant HIV-1 Integrase-DNA Complexes

7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization

Structural basis for strand-transfer inhibitor binding to HIV intasomes

Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors

Close‐up: HIV/SIV intasome structures shed new light on integrase inhibitor binding and viral escape mechanisms

Chromenone derivatives as a versatile scaffold with dual mode of inhibition of HIV-1 reverse transcriptase-associated Ribonuclease H function and integrase activity

Design, synthesis and biological evaluation of imidazole and oxazole fragments as HIV-1 integrase-LEDGF/p75 disruptors and inhibitors of microbial pathogens

Computational design of small molecular modulators of protein–protein interactions with a novel thermodynamic cycle: Allosteric inhibitors of HIV‐1 integrase

Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors

Allosteric HIV Integrase Inhibitors Promote Formation of Inactive Branched Polymers via Homomeric Carboxy-Terminal Domain Interactions

Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity

A supramolecular assembly mediates lentiviral DNA integration

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