A5075478141- HIV Research and Treatment
- HIV/AIDS drug development and treatment
- Protein Structure and Dynamics
- Advanced NMR Techniques and Applications
- Pharmaceutical Economics and Policy
- Pharmaceutical studies and practices
- NMR spectroscopy and applications
- Enzyme Structure and Function
- Hepatitis B Virus Studies
- Antibiotic Resistance in Bacteria
- Adolescent and Pediatric Healthcare
- Financial Reporting and Valuation Research
- Pneumocystis jirovecii pneumonia detection and treatment
- Hepatitis C virus research
- Carbohydrate Chemistry and Synthesis
- Biotechnology and Related Fields
- Asymmetric Hydrogenation and Catalysis
- HIV/AIDS Research and Interventions
- Vibrio bacteria research studies
- Financial Markets and Investment Strategies
- Bacterial Genetics and Biotechnology
- Antimicrobial Peptides and Activities
- Organophosphorus compounds synthesis
- Chemical Synthesis and Analysis
- Childhood Cancer Survivors' Quality of Life
Medicines Patent Pool
2021-2025
Thermo Fisher Scientific (United States)
2025
University of Wisconsin–Madison
2021
International AIDS Society
2014-2018
Boehringer Ingelheim (Canada)
2010-2016
University of Basel
2010-2014
Institut de Biologie Structurale
2014
Universität Innsbruck
2014
Université Grenoble Alpes
2014
University of Leeds
2014
An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization beginning with 1 established importance C3 C4 substituent antiviral potency against viruses different aa124/aa125 variants IN. The C7 position on serum shifted established. Introduction a quinoline at provided balance metabolic stability. Combination these findings ultimately led discovery 26 (BI 224436), first NCINI advance...
Globally, there is a considerable burden of HCV and HIV infections among people who inject drugs (PWID) transmission both continues. Needle syringe programme (NSP) opioid substitution therapy (OST) coverage remains low, despite evidence demonstrating their prevention benefit. Direct-acting antiviral therapies (DAA) with cure >95% PWID provide an opportunity to reverse rising trends in HCV-related morbidity mortality reduce incidence. However, testing, linkage care, treatment remain low due...
Respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infection (LRTI), hospitalisation, and mortality in infants young children, with the highest burden severe disease low-income middle-income countries (LMICs).1Li Y Wang X Blau DM et al.Global, regional, national estimates acute infections due to children younger than 5 years 2019: systematic analysis.Lancet. 2022; 399: 2047-2064Summary Full Text PDF PubMed Google Scholar The predominant hospitalisation occurs...
Nuclear magnetic resonance (NMR) is a powerful tool for observing the motion of biomolecules at atomic level. One technique, analysis relaxation dispersion phenomenon, highly suited studying kinetics and thermodynamics biological processes. Built on top relax computational environment NMR dynamics new designed to be comprehensive, accurate easy-to-use. The software supports more models, both numeric analytic, than current solutions. An automated protocol, available scripting driving...
The alkylation of phosphine boranes with various electrophiles proceeds good to excellent yields in a biphasic solution the presence tetrabutylammonium bromide as phase-transfer catalyst. [reaction: see text]
Background The immune system exerts a diversifying selection pressure on HIV through cellular, humoral and innate mechanisms. This drives viral evolution throughout infection. A better understanding of the natural virus during infection is warranted, given clinical interest in eliciting sustaining an response to which can help control We undertook evaluate potential novel HIV-induced, monocyte-derived factor visfatin modulate infection, as part populations. Results show that capable...
Engineered cyclic peptides (ECPs) have been in the spotlight as novel drug modalities for challenging therapeutic targets. Oral delivery of engineered benefits from ease administration. However, one main hurdles developing orally effective peptide drugs is their potential metabolic instability due to enzymatic degradation. To that end, vitro experiments with simulated intestinal fluid (SIF) used assess stability gastrointestinal tract. Currently, evaluations and biotransformation assessments...
Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) based on compound 2 has led to the discovery molecules capable inhibiting virus harboring N124 variants HIV (IN) while maintaining minimal contribution enterohepatic recirculation clearance in rat. Structure-activity relationships at C6 position established chemical space where extent rat is minimized. Desymmetrization C4 substituent allowed for potency optimization against having variant integrase. Combination...
The potent nitric oxide dioxygenase (NOD) activity (trHbN–Fe2+–O2 + •NO → trHbN–Fe3+–OH2 NO3–) of Mycobacterium tuberculosis truncated hemoglobin N (trHbN) protects aerobic respiration from inhibition by •NO. high trHbN has been attributed in part to the presence numerous short-lived hydrophobic cavities that allow partition and diffusion gaseous substrates O2 active site. We investigated relation between these dynamics protein using solution NMR spectroscopy molecular (MD). Results both...
Abstract Introduction Despite the coordinated efforts by several stakeholders to speed up access HIV treatment for children, development of optimal paediatric formulations still lags 8 10 years behind that adults, due mainly lack market incentives and technical complexities in manufacturing. The small fragmented also hinders launch uptake new formulations. Moreover, problems affecting similarly affect other disease areas where introduction is even slower. Therefore, accelerating processes...
Abstract Background Pre-elafin/trappin-2 is a human innate defense molecule initially described as potent inhibitor of neutrophil elastase. The full-length protein well the N-terminal "cementoin" and C-terminal "elafin" domains were also shown to possess broad antimicrobial activity, namely against opportunistic pathogen P. aeruginosa . mode action these peptides has, however, yet be fully elucidated. Both pre-elafin/trappin-2 are polycationic, but only structure elafin domain currently...