A5047195598- Neuroscience and Neuropharmacology Research
- Receptor Mechanisms and Signaling
- Pharmacogenetics and Drug Metabolism
- Pharmacological Effects and Toxicity Studies
- Neurotransmitter Receptor Influence on Behavior
- Analytical Chemistry and Chromatography
- Drug Transport and Resistance Mechanisms
- HIV Research and Treatment
- Parkinson's Disease Mechanisms and Treatments
- HIV/AIDS drug development and treatment
- Long-Term Effects of COVID-19
- COVID-19 Clinical Research Studies
- Immune Cell Function and Interaction
- SARS-CoV-2 and COVID-19 Research
- Drug-Induced Hepatotoxicity and Protection
- Computational Drug Discovery Methods
- Analytical Methods in Pharmaceuticals
- Eicosanoids and Hypertension Pharmacology
- Migraine and Headache Studies
- Nausea and vomiting management
- Epilepsy research and treatment
- Veterinary Pharmacology and Anesthesia
- Cancer therapeutics and mechanisms
- Heart Failure Treatment and Management
- Cholesterol and Lipid Metabolism
Centre Hospitalier de l’Université de Montréal
2016-2025
Université de Montréal
2015-2018
Small CD4-mimetic compounds (CD4mc) sensitize HIV-1-infected cells to antibody-dependent cellular cytotoxicity (ADCC) by facilitating antibody recognition of epitopes that are otherwise occluded on the unliganded viral envelope (Env). Combining CD4mc with two families CD4-induced (CD4i) antibodies, which frequently found in plasma individuals, stabilizes Env a conformation is vulnerable ADCC. We employed new-generation SRG-15 humanized mice, supporting natural killer (NK) cell and...
While HIV-1-mediated CD4 downregulation protects infected cells from antibody-dependent cellular cytotoxicity (ADCC), shed gp120 binds to on uninfected bystander CD4+ T cells, sensitizing them ADCC mediated by HIV+ plasma. Soluble gp120-CD4 interaction multiple immune also triggers a cytokine burst. The small molecule temsavir acts as an HIV-1 attachment inhibitor preventing envelope glycoprotein (Env)-CD4 and alters the overall antigenicity of Env affecting its processing glycosylation....
ABSTRACT Anti-HIV-1 antibodies capable of mediating ADCC are elicited by the majority people with HIV-1 and preferentially target “open,” CD4-bound conformation envelope glycoproteins (Env). However, due to “closed” sampled unliganded HIV-1-Envs, these ineffective at eliminating infected cells. BNM-III-170 is a small-molecule CD4-mimetic compound that binds Phe43 cavity gp120 subunit Env, forcing Env “open up,” thus exposing epitopes targeted CD4-induced (CD4i), ADCC-mediating antibodies....
The relevance of endogenous 4β‐hydroxycholesterol (4β‐OHC) plasma concentrations or the 4β‐OHC/total cholesterol concentration ratio (4β‐OHC ratio) as surrogate markers cytochrome P450 3A (CYP3A) activity was evaluated in individuals with ( n = 38) without 35) type 2 diabetes (T2D). Midazolam used a comparator to validate exploratory measures phenotypic CYP3A activity. Metabolic ratios orally administered midazolam nondiabetic and diabetic populations correlated significantly 4β‐OHC r s 0.64...
The human small intestine can be involved in the first-pass metabolism of drugs. Under this condition, members CYP450 superfamily are expected to contribute drug presystemic biotransformation. aim study was quantify protein expression levels 16 major isoforms tissue obtained from nine organ donors seven subsections intestine, i.e., duodenum (one section, N = 7 samples), jejunum (three (proximal, mid and distal), 9 samples) ileum subsections, using liquid chromatography tandem mass...
SARS-CoV-2 infection of host cells starts by binding the Spike glycoprotein (S) to ACE2 receptor. The S-ACE2 interaction is a potential target for therapies against COVID-19 as demonstrated development immunotherapies blocking this interaction. VE607 - commercially available compound composed three stereoisomers was described an inhibitor SARS-CoV-1. Here, we show that broadly inhibits pseudoviral particles bearing from major VOCs (D614G, Alpha, Beta, Gamma, Delta, Omicron BA.1, and BA.2)...
Abstract Triple quadrupole mass spectrometers coupled with high performance liquid chromatography are workhorses in quantitative bioanalyses. They provide substantial benefits including reproducibility, sensitivity and selectivity for trace analysis. Selected reaction monitoring allows targeted assay development but datasets generated contain very limited information. Data mining analysis of nontargeted high‐resolution spectrometry profiles biological samples offer the opportunity to perform...
1. The objective of our study was to develop and validate a cocktail approach allow the simultaneous characterization various CYP450-mediated oxidations by human heart microsomes for nine probe drug substrates, namely, 7-ethoxyresorufin, bupropion, repaglinide, tolbutamide, bufuralol, chlorzoxazone, ebastine, midazolam dodecanoic acid.2. first validation step conducted using recombinant CYP450 isoenzymes comparing activity measured each as function (1) buffer used, (2) selectivity towards...
The organic anion transporting polypeptide 1A2 (OATP1A2), a membrane drug transporter expressed on important organs (such as the brain, kidney, and intestine) may be key element in disposition of drugs. Previous studies demonstrated that it could transport broad spectrum substrates, including endogenous molecules clinically relevant drugs, such several <i>β</i>-blockers 3-hydroxy-3-methylglutaryl–CoA reductase inhibitors. primary objective this study was to investigate OATP1A2 activity using...