Results 1 to 10 of about 321,171 (157)
Optimization of TMS target engagement: current state and future perspectives [PDF]
Frontiers in NeuroscienceNeuromodulation is based on the principle that brain stimulation produces plastic changes in cerebral circuitry. Given the intersubject structural and functional variability, neuromodulation has a personalized effect in the brain.
Pantelis Lioumis +15 more
doaj +4 more sources
Molecules, 2023 PLK1 is a protein kinase that regulates mitosis and is both an important oncology drug target and a potential antitarget of drugs for the DNA damage response pathway or anti-infective host kinases.
Xuan Yang +7 more
doaj +3 more sources
Target Engagement in Lead Generation
Bioorganic and Medicinal Chemistry Letters, 2015 The pharmaceutical industry is currently facing multiple challenges, in particular the low number of new drug approvals in spite of the high level of R&D investment. In order to improve target selection and assess properly the clinical hypothesis, it is important to start building an integrated drug discovery approach during Lead Generation.
Timothy B Durham, Maria-Jesus Blanco
exaly +3 more sources
The Opportunities and Use of Imaging to Measure Target Engagement [PDF]
SLAS Discovery, 2020 Lack of efficacy and poor safety outcomes are deemed to be the greatest causes of clinical failure of novel therapeutics. The use of biomarkers that give accurate information on target engagement, providing confidence that pharmacological activity in the target organ is being achieved, is key in optimizing clinical success.
Juliana Maynard
exaly +3 more sources
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 +3 more sources
Size-Dependent Target Engagement of Covalent Probes. [PDF]
J Med ChemLabeling proteins with covalent ligands is finding increasing use in proteomics applications, including identifying nucleophilic residues amenable for labeling and in the development of targeted covalent inhibitors (TCIs). Labeling efficiency is measured by the covalent occupancy of the target or by biochemical activity.
Petri L +7 more
europepmc +3 more sources
Development of SYK NanoBRET cellular target engagement assays for gain–of–function variants [PDF]
Frontiers in Chemical BiologySpleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase that is activated by phosphorylation events downstream of FcR, B-cell and T-cell receptors, integrins, and C-type lectin receptors. When the tandem Src homology 2 (SH2) domains of SYK bind to
Jacob L. Capener +15 more
doaj +2 more sources
Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM [PDF]
Nature CommunicationsCellular target engagement technologies enable quantification of intracellular drug binding; however, simultaneous assessment of drug-associated phenotypes has proven challenging. Here, we present cellular target engagement by accumulation of mutant as a
Nicholas C. K. Valerie +23 more
doaj +2 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