Eugene L. Stewart
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View article: Fostemsavir resistance in clinical context: a narrative review
Fostemsavir resistance in clinical context: a narrative review Open
Fostemsavir, a prodrug of the first-in-class gp120-directed attachment inhibitor temsavir, is indicated in combination with other antiretrovirals for the treatment of multidrug-resistant HIV-1 in adults who are heavily treatment-experience…
View article: Characterization of clinical envelopes with lack of sensitivity to the HIV-1 inhibitors temsavir and ibalizumab
Characterization of clinical envelopes with lack of sensitivity to the HIV-1 inhibitors temsavir and ibalizumab Open
Previous data suggest a lack of cross-resistance between the gp120-directed attachment inhibitor temsavir (active moiety of fostemsavir) and the CD4-directed post-attachment inhibitor ibalizumab. Recently, analysis of HIV-1 envelopes with …
View article: Correction for Underwood et al., “Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study”
Correction for Underwood et al., “Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study” Open
Volume 66, no. 1, e0164321, 2022, https://doi.org/10.1128/AAC.01643-21. Page 12, “Data availability” paragraph, line 2: The reported GenBank accession numbers (MZ568467 to MZ568625) are incorrect. The GenBank accession numbers should be MZ…
View article: Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance
Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance Open
The androgen receptor (AR) is required for male sex development and contributes to prostate cancer cell survival. In contrast to other nuclear receptors that bind the LXXLL motifs of coactivators, the AR ligand binding domain is preferenti…
View article: Emergence of Resistance in HIV-1 Integrase with Dolutegravir Treatment in a Pediatric Population from the IMPAACT P1093 Study
Emergence of Resistance in HIV-1 Integrase with Dolutegravir Treatment in a Pediatric Population from the IMPAACT P1093 Study Open
P1093 is a multicenter, open-label, phase I/II study of pharmacokinetics, safety, and tolerability of dolutegravir plus an optimized background regimen in pediatric participants aged 4 weeks to <18 years with HIV-1. Most participants were …
View article: A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors Open
View article: Susceptibility of global HIV-1 clinical isolates to fostemsavir using the PhenoSense® Entry assay
Susceptibility of global HIV-1 clinical isolates to fostemsavir using the PhenoSense® Entry assay Open
Background Fostemsavir is a prodrug of a first-in-class HIV-1 attachment inhibitor, temsavir, that binds to gp120 and blocks attachment to the host-cell CD4 receptor, preventing entry and infection of the target cell. Previous studies usin…
View article: Complementary NAD+ replacement strategies fail to functionally protect dystrophin-deficient muscle
Complementary NAD+ replacement strategies fail to functionally protect dystrophin-deficient muscle Open
View article: The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure Open
View article: Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle
Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle Open
Background Duchenne muscular dystrophy (DMD) is a progressive muscle wasting disorder stemming from a loss of functional dystrophin. Current therapeutic options for DMD are limited, as small molecule modalities remain largely unable to dec…
View article: Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle
Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle Open
Background Duchenne muscular dystrophy (DMD) is a progressive muscle wasting disorder stemming from a loss of functional dystrophin. Current therapeutic options for DMD are limited, as small molecule modalities remain largely unable to les…
View article: Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle
Complementary NAD+ Replacement Strategies Fail to Functionally Protect Dystrophin-Deficient Muscle Open
Background Duchenne muscular dystrophy (DMD) is a progressive muscle wasting disorder stemming from a loss of functional dystrophin. Current therapeutic options for DMD are limited, as small molecule modalities remain largely unable to les…
View article: Additional file 1 of Complementary NAD+ replacement strategies fail to functionally protect dystrophin-deficient muscle
Additional file 1 of Complementary NAD+ replacement strategies fail to functionally protect dystrophin-deficient muscle Open
Additional file 1. Frederick et al Supplemental Table 1.
View article: The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors Open
View article: 2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships
2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships Open
View article: QTL mapping reveals complex genetic architecture of quantitative virulence in the wheat pathogen<i>Zymoseptoria tritici</i>
QTL mapping reveals complex genetic architecture of quantitative virulence in the wheat pathogen<i>Zymoseptoria tritici</i> Open
Summary We conducted a comprehensive analysis of virulence in the fungal wheat pathogen Zymoseptoria tritici using QTL mapping. High throughput phenotyping based on automated image analysis allowed measurement of pathogen virulence on a sc…
View article: QTL mapping of temperature sensitivity reveals candidate genes for thermal adaptation and growth morphology in the plant pathogenic fungus Zymoseptoria tritici
QTL mapping of temperature sensitivity reveals candidate genes for thermal adaptation and growth morphology in the plant pathogenic fungus Zymoseptoria tritici Open
View article: Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38 Open
Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline ring resulted in the identific…
View article: Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors Open
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD…