Results 71 to 80 of about 1,298 (145)

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

Quantification of Wnt3a, Wnt5a and Wnt16 Binding to Multiple Frizzleds Under Physiological Conditions Using NanoBit/BRET

Cells
Upon engagement of one of the nineteen secreted Wnt signaling proteins with one of the ten Frizzled transmembrane Wnt receptors (FZD1–10), a wide variety of cellular Wnt signaling responses can be elicited, the selectivity of which depends on the ...
Janine Wesslowski, Sadia Safi, Michelle Rottmann, Melanie Rothley, Gary Davidson   +4 more
doaj   +1 more source

New heterocyclic A1/A3 adenosine receptor ligands through molecular simplification strategies

European Journal of Medicinal Chemistry Reports
In this paper we report the synthesis of new A1/A3 adenosine receptor antagonists designed as simplification products of the A1 antagonists with pyrazolo[1′,5′:1,6]pyrimido [4,5-d]pyridazin-4(3H)-one scaffold previously developed by us.
Letizia Crocetti, Abigail Pearce, Venkat S. Vege, Qi Xu, Jing Xu, Hannes Buthmann, Maria Paola Giovannoni, Gabriella Guerrini, Francesca Catarzi, Silvia Selleri, Xianglin Huang, Aneesh Chandran, Graham Ladds, Agostino Cilibrizzi   +13 more
doaj   +1 more source

Scaffold-hopping for molecular glues targeting the 14-3-3/ERα complex

Nature Communications
Molecular glues, small molecules that bind cooperatively at a protein-protein interface, have emerged as powerful modalities for the modulation of protein-protein interactions (PPIs) and “undruggable” targets.
Markella Konstantinidou, Marios Zingiridis, Marloes A. M. Pennings, Michael Fragkiadakis, Johanna M. Virta, Jezrael L. Revalde, Emira J. Visser, Christian Ottmann, Luc Brunsveld, Constantinos G. Neochoritis, Michelle R. Arkin   +10 more
doaj   +1 more source

BromoCatch: a self-labelling tag platform for protein modification and live cell imaging

Nature Communications
Visualizing and manipulating proteins in live cells is crucial for studying complex biological processes. Self-labelling protein (SLP) tags such as HaloTag and SNAP-tag are widely used for protein labelling, and new systems are needed to expand ...
Maria Rodriguez-Rios, Conner Craigon, Mark A. Nakasone, Gajanan Sathe, Adam G. Bond, Mark Dorward, Anthony K. Edmonds, Mark C. Norley, Robert E. Arnold, Paul M. Wood, Stephen J. Reynolds, Joel O. Cresser-Brown, Graham P. Marsh, Hannah J. Maple, Alessio Ciulli   +14 more
doaj   +1 more source

Systematic assessment of chemokine ligand bias at the human chemokine receptor CXCR2 indicates G protein bias over β-arrestin recruitment and receptor internalization

Cell Communication and Signaling
Background The human CXC chemokine receptor 2 (CXCR2) is a G protein-coupled receptor (GPCR) interacting with multiple chemokines (i.e., CXC chemokine ligands CXCL1-3 and CXCL5-8). It is involved in inflammatory diseases as well as cancer.
Katrijn Boon, Nathan Vanalken, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Tom Van Loy   +5 more
doaj   +1 more source

Quantifying VEGF binding at VEGFR2 and Neuropilin-1 using NanoBRET

Proceedings for Annual Meeting of The Japanese Pharmacological Society, 2018
Peach, Chloe, Kilpatrick, Laura, Friedman-Ohana, Rachel, Robers, Matt, Woolard, Jeanette, Hill, Steve   +5 more
openaire   +2 more sources

NanoBRET Saturation Analysis with a Novel HaloTag Ligand Reveals Butyrophilin Heteromeric Interactions Controlling γ9δ2 T Cell Activation. [PDF]

ACS Chem Biol
Pawge G, Bashir S, Parikh R, Hsiao CC, Wiemer AJ.   +4 more
europepmc   +1 more source

Cellular Target Engagement and Dissociation Kinetics of Class I-Selective Histone Deacetylase (HDAC) Inhibitors. [PDF]

Int J Mol Sci
Honin I, Novakova Z, Feller F, Schneider S, Schäker-Hübner L, Barinka C, K Hansen F.   +6 more
europepmc   +1 more source