Results 11 to 20 of about 321,270 (256)

tracerDB: a crowdsourced fluorescent tracer database for target engagement analysis [PDF]

Nature Communications
Investigating ligand-protein complexes is essential in the areas of chemical biology and drug discovery. However, detailed information on key reagents such as fluorescent tracers and associated data for the development of widely used bioluminescence ...
Johannes Dopfer, James D. Vasta, Susanne Müller, Stefan Knapp, Matthew B. Robers, Martin P. Schwalm   +5 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

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

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
doaj   +1 more source

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., Janning, P., Ziegler, S., Waldmann, H.   +3 more
openaire   +3 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, Micah J, Niphakis, Benjamin F, Cravatt   +2 more
openaire   +2 more sources