Results 51 to 60 of about 1,238 (123)

Development of novel small molecule EPHB3 inhibitors to treat neurodegenerative disease by targeting astrocyte‐mediated disease mechanisms

Alzheimer's &Dementia, Volume 21, Issue S5, December 2025.
Abstract Background Brain glial cells have emerged as key pathogenic drivers of Alzheimer’s disease (AD). We previously identified EPHB3 as a novel target that mediates cellular interactions between astrocytes and microglia in vivo to produce neuroinflammation and have now developed small molecule EPHB3 inhibitors with drug‐like properties.
Evan P Lebois, Chinnappa D Kodira, Robert D Hubbard, Darby R Schmidt   +3 more
wiley   +1 more source

tracerDB: a crowdsourced fluorescent tracer database for target engagement analysis

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   +1 more source

Agonist efficacy at the β2AR is driven by the faster association rate of the Gs protein

Frontiers in Pharmacology
IntroductionThe β2-adrenoceptor (β2AR) is a class A G protein-coupled receptor (GPCR). It is therapeutically relevant in asthma and chronic obstructive pulmonary disease (COPD), where β2AR agonists relieve bronchoconstriction.
Clare R. Harwood, Clare R. Harwood, David A. Sykes, David A. Sykes, David A. Sykes, Theo Redfern-Nichols, Owen Underwood, Colin Nicholson, Colin Nicholson, Armin N. Khoshgrudi, Armin N. Khoshgrudi, Eline J. Koers, Eline J. Koers, Graham Ladds, Graham Ladds, Stephen J. Briddon, Stephen J. Briddon, Dmitry B. Veprintsev, Dmitry B. Veprintsev, Dmitry B. Veprintsev   +19 more
doaj   +1 more source

High‐Throughput Synthesis and Screening of a Cyanimide Library Identifies Selective Inhibitors of ISG15‐Specific Protease mUSP18

Angewandte Chemie, Volume 137, Issue 49, December 1, 2025.
Deubiquitinases (DUBs) and Ub‐like proteases are attractive but challenging drug targets. We developed a high‐throughput synthesis method and prepared a 7536‐member cyanimide DUB‐targeted compound library in 1536‐well plates, using Echo acoustic dispensing. Screening yielded a selective, 35 nM inhibitor of mUSP18, the main ISG15 protease.
Raymond Kooij, Vito Pol, Jin Gan, Bjorn R. van Doodewaerd, Aysegul Sapmaz, Marta Campos Alonso, Günter Fritz, Klaus‐Peter Knobeloch, Paul P. Geurink   +8 more
wiley   +1 more source

Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators

Frontiers in Pharmacology
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten, Katrijn Boon, Max Van Hoof, Wim Dehaen, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Steven De Jonghe, Tom Van Loy   +8 more
doaj   +1 more source

AI and network biology for rational polypharmacology in signaling drug design: a review

npj Precision Oncology
The complexity of disease-causing signaling networks is indicative of the failure of single-target therapeutics to work, particularly because of feedback, redundancy and activation of compensatory responses.
Xuehao Li, Zhaoqi Wu, Te Fang, Jun Li, Danyang Li, Ximeng Zhang, Ling Liu, Liming Wang   +7 more
doaj   +1 more source

Publication Only

HemaSphere, Volume 10, Issue S1, June 2026.
wiley   +1 more source

ISEV2026 Abstract Book

Journal of Extracellular Vesicles, Volume 15, Issue S1, June 2026.
wiley   +1 more source

Systematic Assessment of Human CCR7 Signalling Using NanoBRET Biosensors Points towards the Importance of the Cellular Context

Biosensors
The human CC chemokine receptor 7 (CCR7) is activated by two natural ligands, CC chemokine ligand 19 (CCL19) and 21 (CCL21). The CCL19-CCL21-CCR7 axis has been extensively studied in vitro, but there is still debate over whether CCL21 is an overall ...
Nathan Vanalken, Katrijn Boon, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Tom Van Loy   +5 more
doaj   +1 more source

Crystallographic fragment screening reveals ligand hotspots in TRIM21 PRY-SPRY domain

Communications Chemistry
Tripartite motif-containing protein 21 (TRIM21), and particularly its PRY-SPRY protein interaction domain, plays a critical role in the immune response by recognizing intracellular antibodies targeting them for degradation.
Yeojin Kim, Aleksandar Lučić, Christopher Lenz, Frederic Farges, Martin P. Schwalm, Krishna Saxena, Thomas Hanke, Peter G. Marples, Jasmin C. Aschenbrenner, Daren Fearon, Frank von Delft, Andreas Krämer, Stefan Knapp   +12 more
doaj   +1 more source