Results 11 to 20 of about 4,123,279 (296)
Identification of direct target engagement biomarkers for kinase-targeted therapeutics. [PDF]
PLoS ONE, 2011 Pharmacodynamic (PD) biomarkers are an increasingly valuable tool for decision-making and prioritization of lead compounds during preclinical and clinical studies as they link drug-target inhibition in cells with biological activity.
Cloud P Paweletz +12 more
doaj +4 more sources
Target Engagement Assays in Early Drug Discovery. [PDF]
J Med ChemIn target-based drug discovery, quantification of target engagement is required to build structure-activity relationships and develop a potent clinical candidate. Target engagement data also provides evidence of a drug's mechanism of action (MoA) which although is not required for approval, can increase the chance of a successful clinical outcome ...
St John-Campbell S, Bhalay G.
europepmc +4 more sources
Targeting, Deployment, and Loss-Tolerance in Lanchester Engagements [PDF]
Operations Research, 2021 Incorporating Imperfect Targeting, Deployment Restrictions, and Morale into Combat Models
Michael P. Atkinson +2 more
openaire +4 more sources
Freiwilliges Engagement in Deutschland [PDF]
, 2022 Das Open Access Buch bietet eine aktuelle Bestandsaufnahme zum freiwilligen Engagement in Deutschland. Die Ergebnisse basieren auf dem Deutschen Freiwilligensurvey, der zum fünften Mal im Jahr 2019 durchgeführt wurde und vom Bundesministerium für Familie,
core +1 more source
Importance of Quantifying Drug-Target Engagement in Cells [PDF]
ACS Medicinal Chemistry Letters, 2020 Measuring and quantifying the binding of a drug to a protein target inside living cells and thereby correlating biochemical or biophysical activity with target engagement in cells or tissue represents a key step in target validation and drug development.
Jakub Stefaniak, Kilian V. M. Huber
openaire +2 more sources
Determining target engagement in living systems [PDF]
Nature Chemical Biology, 2013 Chemical probes are critical tools for elucidating the biological functions of proteins and can lead to new medicines for treating disease. The pharmacological validation of protein function requires verification that chemical probes engage their intended targets in vivo. Here we discuss technologies, both established and emergent, for measuring target
Gabriel M, Simon +2 more
openaire +2 more sources
Small-Molecule Target Engagement in Cells [PDF]
Cell Chemical Biology, 2016 Monitoring how, when, and where small molecules engage their targets inside living cells is a critical step in chemical biology and pharmacological research, because it enables compound efficacy and confirmation of mode of action to be assessed. In this mini-review we summarize the currently available methodologies to detect and prove direct target ...
Schürmann, M. +3 more
openaire +3 more sources
Golgi Recruitment Assay for Visualizing Small-Molecule Ligand–target Engagement in Cells [PDF]
, 2020 The development of methods that allow detection of ligand–target engagement in cells is an important challenge in chemical biology and drug discovery. Here, we present a Golgi recruitment (G-REC) assay in which the ligand binding to the target protein ...
Masahiro, Ikuta +5 more
core +2 more sources
Acute retigabine‐induced effects on myelinated motor axons in amyotrophic lateral sclerosis
Pharmacology 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
Molecules, 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