Results 1 to 10 of about 4,123,279 (296)

Optimization of TMS target engagement: current state and future perspectives [PDF]

Frontiers in Neuroscience
Neuromodulation 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, Pantelis Lioumis, Pantelis Lioumis, Timo Roine, Timo Roine, Ida Granö, Dogu Baran Aydogan, Dogu Baran Aydogan, Elena Ukharova, Victor H. Souza, Dubravko Kičić, Risto J. Ilmoniemi, Nikos Makris, Nikos Makris, Nikos Makris, Nikos Makris   +15 more
doaj   +4 more sources

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells

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, Jeffery L. Smith, Michael T. Beck, Jennifer M. Wilkinson, Ani Michaud, James D. Vasta, Matthew B. Robers, Timothy M. Willson   +7 more
doaj   +3 more sources

Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM [PDF]

Nature Communications
Cellular 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, Kumar Sanjiv, Oliver Mortusewicz, Si Min Zhang, Seher Alam, Maria J. Pires, Hannah Stigsdotter, Azita Rasti, Marie-France Langelier, Daniel Rehling, Adam Throup, Oryn Purewal-Sidhu, Matthieu Desroses, Jacob Onireti, Prasad Wakchaure, Ingrid Almlöf, Johan Boström, Luka Bevc, Giorgia Benzi, Pål Stenmark, John M. Pascal, Thomas Helleday, Brent D. G. Page, Mikael Altun   +23 more
doaj   +2 more sources

Modeling Pharmacokinetics and Pharmacodynamics of Therapeutic Antibodies: Progress, Challenges, and Future Directions

Pharmaceutics, 2021
With more than 90 approved drugs by 2020, therapeutic antibodies have played a central role in shifting the treatment landscape of many diseases, including autoimmune disorders and cancers. While showing many therapeutic advantages such as long half-life
Yu Tang, Yanguang Cao
doaj   +1 more source

Minimal Physiologically-Based Pharmacokinetic (mPBPK) Metamodeling of Target Engagement in Skin Informs Anti-IL17A Drug Development in Psoriasis

Frontiers in Pharmacology, 2022
The pharmacologic effect(s) of biotherapeutics directed against soluble targets are driven by the magnitude and duration of free target suppression at the tissue site(s) of action. Interleukin (IL)-17A is an inflammatory cytokine that plays a key role in
Vivaswath S. Ayyar, Jong Bong Lee, Weirong Wang, Meghan Pryor, Yanli Zhuang, Thomas Wilde, An Vermeulen, An Vermeulen   +7 more
doaj   +1 more source

Nonclinical safety evaluation, pharmacokinetics, and target engagement of Lu AF82422, a monoclonal IgG1 antibody against alpha-synuclein in development for treatment of synucleinopathies

mAbs, 2021
Alpha-synuclein is a 15 kDa protein associated with neurodegenerative diseases such as Parkinson disease and multiple-system atrophy where pathological forms of alpha-synuclein aggregate and become neurotoxic.
Lone Fjord-Larsen, Annemette Thougaard, Karen Malene Wegener, Joan Christiansen, Frank Larsen, Lise Maj Schrøder-Hansen, Marianne Kaarde, Dorte Kornerup Ditlevsen   +7 more
doaj   +1 more source

Assessing target engagement using proteome-wide solvent shift assays

eLife, 2021
Recent advances in mass spectrometry (MS) have enabled quantitative proteomics to become a powerful tool in the field of drug discovery, especially when applied toward proteome-wide target engagement studies.
Jonathan G Van Vranken, Jiaming Li, Dylan C Mitchell, José Navarrete-Perea, Steven P Gygi   +4 more
doaj   +1 more source

Specificity and Durability of Changes in Auditory Processing Efficiency After Targeted Cognitive Training in Individuals With Recent-Onset Psychosis

Frontiers in Psychiatry, 2020
BackgroundWe previously demonstrated that the high heterogeneity of response to computerized Auditory Training (AT) in psychosis can be ascribed to individual differences in sensory processing efficiency and neural plasticity.
Bruno Biagianti, Bruno Biagianti, Melissa Fisher, Rachel Loewy, Benjamin Brandrett, Catalina Ordorica, Kristin LaCross, Brandon Schermitzler, Michelle McDonald, Ian Ramsay, Sophia Vinogradov   +10 more
doaj   +1 more source

Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth

eLife, 2022
Drugs that target human thymidylate synthase (hTS), a dimeric enzyme, are widely used in anticancer therapy. However, treatment with classical substrate-site-directed TS inhibitors induces over-expression of this protein and development of drug ...
Luca Costantino, Stefania Ferrari, Matteo Santucci, Outi MH Salo-Ahen, Emanuele Carosati, Silvia Franchini, Angela Lauriola, Cecilia Pozzi, Matteo Trande, Gaia Gozzi, Puneet Saxena, Giuseppe Cannazza, Lorena Losi, Daniela Cardinale, Alberto Venturelli, Antonio Quotadamo, Pasquale Linciano, Lorenzo Tagliazucchi, Maria Gaetana Moschella, Remo Guerrini, Salvatore Pacifico, Rosaria Luciani, Filippo Genovese, Stefan Henrich, Silvia Alboni, Nuno Santarem, Anabela da Silva Cordeiro, Elisa Giovannetti, Godefridus J Peters, Paolo Pinton, Alessandro Rimessi, Gabriele Cruciani, Robert M Stroud, Rebecca C Wade, Stefano Mangani, Gaetano Marverti, Domenico D'Arca, Glauco Ponterini, Maria Paola Costi   +38 more
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Development of novel ultra-sensitive IL-11 target engagement assays to support mechanistic PK/PD modeling for an anti-IL-11 antibody therapeutic

mAbs, 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, Siqi Lin, Legairre Radden, Cynthia Hess Kenny, Zheng Cai, Angus MacDonald, Ralph Binetti, Michael Marlow, Paul Fracasso, Glenn Gibson, Christina Bartlett, Julie Hawkins, Steven Hansel   +12 more
doaj   +1 more source