Results 51 to 60 of about 7,154 (184)
Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley +1 more source
Aim of the study: Our hypothesis is that nirmatrelvir can penetrate the blood‒brain barrier and reach effective concentrations in the brain. Furthermore, herbal formulations can help maintain nirmatrelvir levels in the body, suggesting potential ...
Wan-Hsin Lee +8 more
doaj +1 more source
Abstract Ritonavir (RTV) is a potent CYP3A inhibitor that is widely used as a pharmacokinetic (PK) enhancer to increase exposure to select protease inhibitors. However, as a strong and complex perpetrator of CYP3A interactions, RTV can also enhance the exposure of other co‐administered CYP3A substrates, potentially causing toxicity.
Lien Thi Ngo +5 more
wiley +1 more source
Effects of nirmatrelvir on yeast expressing Mpro from SARS-CoV-1 and Bat-CoV-HKU9.
Growth of yeast expressing Mpro from the indicated coronavirus is plotted in the presence or absence of nirmatrelvir. Mpro from both viruses remain responsive to nirmatrelvir as indicated by improved growth (nearly matching the empty vector (EV) control)
Ryan T. Morgan (16642962) +14 more
core +1 more source
Large‐scale cohorts and multimodal biomedical data have enabled powerful predictive models for clinical risk stratification, but prediction alone cannot guide effective interventions. This review introduces causal artificial intelligence as a design‐first framework that integrates target trial emulation, causal discovery, and robust effect estimation ...
Linlin Cao +5 more
wiley +1 more source
In response to the COVID-19 pandemic, nirmatrelvir/ritonavir was approved as the first per os treatment to prevent severe disease progression. This study explores patients’ self-management of nirmatrelvir/r and its impact on their long-term medications ...
Beatriz Santos MS +4 more
doaj +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Background The effectiveness of nirmatrelvir–ritonavir has mainly been shown in non-hospitalized patients with mild-to-moderate coronavirus disease 2019 (COVID-19).
Xiaobo Han +24 more
doaj +1 more source
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Aims The repurposed use of favipiravir in COVID‐19 has been reported to have limited clinical efficacy, yet it has been widely used in some countries. Favipiravir causes mutagenesis in RNA viruses, and it is currently unknown whether it may have a measurable effect on the virus in humans.
Akosua A. Agyeman +9 more
wiley +1 more source

