Results 21 to 30 of about 321,270 (256)

Development of novel ultra-sensitive IL-11 target engagement assays to support mechanistic PK/PD modeling for an anti-IL-11 antibody therapeutic

open access: yesmAbs, 2022
An in-house antibody generation campaign identified a diverse, high affinity set of anti-interleukin-11 (IL-11) monoclonal antibodies (mAbs) to enable successful development of novel, custom ultra-sensitive target engagement assays for detection of “free”
Maria Myzithras   +12 more
doaj   +1 more source

Acute retigabine‐induced effects on myelinated motor axons in amyotrophic lateral sclerosis

open access: yesPharmacology Research & Perspectives, 2022
Altered motor neuron excitability in patients with amyotrophic lateral sclerosis (ALS) has been suggested to be an early pathophysiological mechanism associated with motor neuron death.
Boudewijn T. H. M. Sleutjes   +6 more
doaj   +1 more source

Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry

open access: yesMolecules, 2021
Chemical biology and drug discovery are two scientific activities that pursue different goals but complement each other. The former is an interventional science that aims at understanding living systems through the modulation of its molecular components ...
Benoit Deprez   +8 more
doaj   +1 more source

Current Advances in CETSA

open access: yesFrontiers in Molecular Biosciences, 2022
Knowing that the drug candidate binds to its intended target is a vital part of drug discovery. Thus, several labeled and label-free methods have been developed to study target engagement.
Tuomas Aleksi Tolvanen   +1 more
doaj   +1 more source

Chemo‐proteomics in antimalarial target identification and engagement

open access: yesMedicinal Research Reviews, 2023
AbstractHumans have lived in tenuous battle with malaria over millennia. Today, while much of the world is free of the disease, areas of South America, Asia, and Africa still wage this war with substantial impacts on their social and economic development. The threat of widespread resistance to all currently available antimalarial therapies continues to
Brodie L. Bailey   +3 more
openaire   +2 more sources

Characterization of concurrent target suppression by JNJ-61178104, a bispecific antibody against human tumor necrosis factor and interleukin-17A

open access: yesmAbs, 2020
Tumor necrosis factor (TNF) and interleukin (IL)-17A are pleiotropic cytokines implicated in the pathogenesis of several autoimmune diseases including rheumatoid arthritis (RA) and psoriatic arthritis (PsA).
Songmao Zheng   +10 more
doaj   +1 more source

Inhibition of 11β-HSD1 Ameliorates Cognition and Molecular Detrimental Changes after Chronic Mild Stress in SAMP8 Mice

open access: yesPharmaceuticals, 2021
Impaired glucocorticoid (GC) signaling is a significant factor in aging, stress, and neurodegenerative diseases such as Alzheimer’s disease. Therefore, the study of GC-mediated stress responses to chronic moderately stressful situations, which occur in ...
Dolors Puigoriol-Illamola   +8 more
doaj   +1 more source

Cycloguanil and Analogues Potently Target DHFR in Cancer Cells to Elicit Anti-Cancer Activity

open access: yesMetabolites, 2023
Dihydrofolate reductase (DHFR) is an established anti-cancer drug target whose inhibition disrupts folate metabolism and STAT3-dependent gene expression. Cycloguanil was proposed as a DHFR inhibitor in the 1950s and is the active metabolite of clinically
Jennifer I. Brown   +15 more
doaj   +1 more source

Thermal proteome profiling in bacteria: probing protein state in vivo

open access: yesMolecular Systems Biology, 2018
Increasing antibiotic resistance urges for new technologies for studying microbes and antimicrobial mechanism of action. We adapted thermal proteome profiling (TPP) to probe the thermostability of Escherichia coli proteins in vivo. E.
André Mateus   +7 more
doaj   +1 more source

17β-Estradiol Delivered in Eye Drops: Evidence of Impact on Protein Networks and Associated Biological Processes in the Rat Retina through Quantitative Proteomics

open access: yesPharmaceutics, 2020
To facilitate the development of broad-spectrum retina neuroprotectants that can be delivered through topical dosage forms, this proteomics study focused on analyzing target engagements through the identification of functional protein networks impacted ...
Laszlo Prokai   +3 more
doaj   +1 more source

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