Ross C. Larue
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View article: Nucleoside Reverse Transcriptase Inhibitor (NRTI)-Induced Neuropathy and Mitochondrial Toxicity: Limitations of the Poly-γ Hypothesis and the Potential Roles of Autophagy and Drug Transport
Nucleoside Reverse Transcriptase Inhibitor (NRTI)-Induced Neuropathy and Mitochondrial Toxicity: Limitations of the Poly-γ Hypothesis and the Potential Roles of Autophagy and Drug Transport Open
Nucleoside reverse transcriptase inhibitors (NRTIs) are the backbone of highly active antiretroviral therapy (HAART)—the current standard of care for treating human immunodeficiency virus (HIV) infection. Despite their efficacy, NRTIs caus…
View article: BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications
BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications Open
The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. They are epigenetic readers o…
View article: Human immunodeficiency virus integration complexes are active following ordered addition of wild type integrase, viral DNA, and LEDGF/p75
Human immunodeficiency virus integration complexes are active following ordered addition of wild type integrase, viral DNA, and LEDGF/p75 Open
Human immunodeficiency virus (HIV-1) requires integration of the viral genome into the host DNA for replication. Efficient HIV-1 integration employs a host co-factor LEDGF/p75 to stabilize the HIV-1 integration complex and tether that comp…
View article: Identification and Optimization of a Novel HIV-1 Integrase Inhibitor
Identification and Optimization of a Novel HIV-1 Integrase Inhibitor Open
Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS). HIV-1, like all retroviruses, stably integrates its vDNA copy into host chromatin, a process allowing for permanent infection. This…
View article: Conformation of HIV-1 Envelope Governs Rhesus CD4 Usage and Simian-Human Immunodeficiency Virus Replication
Conformation of HIV-1 Envelope Governs Rhesus CD4 Usage and Simian-Human Immunodeficiency Virus Replication Open
Rhesus macaques are a critical animal model for preclinical testing of HIV-1 vaccine and prevention approaches. However, HIV-1 does not replicate in rhesus macaques, and thus, chimeric simian-human immunodeficiency viruses (SHIVs), which e…
View article: Prototype Foamy Virus Integrase Displays Unique Biochemical Activities among Retroviral Integrases
Prototype Foamy Virus Integrase Displays Unique Biochemical Activities among Retroviral Integrases Open
Integrases of different retroviruses assemble as functional complexes with varying multimers of the protein. Retroviral integrases require a divalent metal cation to perform one-step transesterification catalysis. Tetrameric prototype foam…
View article: Among retroviral integrases prototype foamy virus integrase displays unique biochemical activities
Among retroviral integrases prototype foamy virus integrase displays unique biochemical activities Open
Integrase enzymes of different retroviruses assemble as functional complexes with varying multimers of the protein. Retroviral integrases require a divalent metal cation to perform one-step transesterification catalysis. Tetrameric prototy…
View article: The intrinsic kinase activity of BRD4 spans its BD2-B-BID domains
The intrinsic kinase activity of BRD4 spans its BD2-B-BID domains Open
Bromodomain protein 4 (BRD4) is a transcriptional and epigenetic regulator that is a therapeutic target in many cancers and inflammatory diseases. BRD4 plays important roles in transcription as an active kinase, which phosphorylates the ca…
View article: Development of Murine Leukemia Virus Integrase-Derived Peptides That Bind Brd4 Extra-Terminal Domain as Candidates for Suppression of Acute Myeloid Leukemia
Development of Murine Leukemia Virus Integrase-Derived Peptides That Bind Brd4 Extra-Terminal Domain as Candidates for Suppression of Acute Myeloid Leukemia Open
The bromodomain and extra-terminal (BET) domain family of proteins, which include its prototypical member Brd4, is implicated in a variety of cancers and viral infections due to their interaction with cellular and viral proteins. BET prote…
View article: Conformation of HIV-1 Envelope governs rhesus CD4 usage and simian-human immunodeficiency virus replication
Conformation of HIV-1 Envelope governs rhesus CD4 usage and simian-human immunodeficiency virus replication Open
Infection of rhesus macaques with simian-human immunodeficiency viruses (SHIVs) is the preferred model system for vaccine development because SHIVs encode HIV-1 envelope glycoproteins (Env) – a key target of HIV-1 neutralizing antibodies. …
View article: Strategies for Targeting Retroviral Integration for Safer Gene Therapy: Advances and Challenges
Strategies for Targeting Retroviral Integration for Safer Gene Therapy: Advances and Challenges Open
Retroviruses are obligate intracellular parasites that must integrate a copy of the viral genome into the host DNA. The integration reaction is performed by the viral enzyme integrase in complex with the two ends of the viral cDNA genome a…
View article: Rationally Designed ACE2-Derived Peptides Inhibit SARS-CoV-2
Rationally Designed ACE2-Derived Peptides Inhibit SARS-CoV-2 Open
Severe acute respiratory syndrome coronavirus (SARS-CoV)-2 is a novel and highly pathogenic coronavirus and is the causative agent of the coronavirus disease 2019 (COVID-19). The high morbidity and mortality associated with COVID-19 and th…
View article: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors
HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors Open
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are a promising new class of antiretroviral agents that disrupt proper viral maturation by inducing hyper-multimerization of IN. Here we show that lead pyridine-based ALLINI KF116 exhibi…
View article: Author response: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors
Author response: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors Open
Article Figures and data Abstract eLife digest Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract Allosteric HIV-1 integrase (I…
View article: Author response: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors
Author response: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors Open
Article Figures and data Abstract eLife digest Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract Allosteric HIV-1 integrase (I…
View article: HIV-1 Integrase Catalytic Core Domain Complexed with Allosteric Inhibitor (2S)-[1-(1-benzyl-1H-pyrazol-4-yl)-3-(3,4-dihydro-2H-1-benzopyran-6-yl)isoquinolin-4-yl](tert-butoxy)acetic acid
HIV-1 Integrase Catalytic Core Domain Complexed with Allosteric Inhibitor (2S)-[1-(1-benzyl-1H-pyrazol-4-yl)-3-(3,4-dihydro-2H-1-benzopyran-6-yl)isoquinolin-4-yl](tert-butoxy)acetic acid Open
Allosteric HIV-1 integrase inhibitors (ALLINIs) are a new class of potential antiretroviral therapies with a unique mechanism of action and drug resistance profile. To further extend this class of inhibitors via a scaffold hopping approach…
View article: Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol polyprotein proteolytic processing
Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol polyprotein proteolytic processing Open
The pyridine-based multimerization selective HIV-1 integrase (IN) inhibitors (MINIs) are a distinct subclass of allosteric IN inhibitors. MINIs potently inhibit HIV-1 replication during virion maturation by inducing hyper- or aberrant IN m…
View article: The FACT Complex Promotes Avian Leukosis Virus DNA Integration
The FACT Complex Promotes Avian Leukosis Virus DNA Integration Open
All retroviruses need to integrate a DNA copy of their genome into the host chromatin. Cellular proteins regulating and targeting lentiviral and gammaretroviral integration in infected cells have been discovered, but the factors that media…
View article: The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency
The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency Open
Allosteric HIV-1 integrase inhibitors (ALLINIs) have recently emerged as a promising class of antiretroviral agents and are currently in clinical trials. In infected cells, ALLINIs potently inhibit viral replication by impairing virus part…
View article: Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction
Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction Open
Significance Bromodomain and extraterminal domain (BET) proteins recruit a variety of cellular factors to epigenetic marks on chromatin to modulate essential cellular processes, including DNA repair and transcription. To facilitate their r…