Results 81 to 90 of about 488 (104)

Small Molecule Modulation of NOS1AP for Molecularly Targeted Glioblastoma Therapy

Life
NOS1AP (CAPON) is a signaling adaptor implicated in glioblastoma (GBM) proliferation, but its chemical tractability remains largely unexplored. Here, affinity selection–mass spectrometry screening of 10,000 drug-like compounds identified NGM1, a small ...
Ashraf N. Abdo, Sungwoo Cho, Moustafa Gabr   +2 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

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

Development of NanoBRET‐Binding Assays for FKBP‐Ligand Profiling in Living Cells

FK506‐binding proteins (FKBPs) are promising targets for a variety of disorders and infectious diseases. High FKBP occupancy is thought to be necessary for ligands to effectively compete with the endogenous intracellular functions of FKBPs.
Walz, Michael, Kolos, Jürgen M., Kuehn, Angela, Gutfreund, Niklas, Hausch, Felix, Geiger, Thomas M., Gnatzy, Monika T.   +6 more
core   +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

Dataset for "NanoBRET-based detection of ligand-receptor interactions at the neuropeptide FF receptor 1"

The neuropeptide FF receptor 1 (NPFFR1) belongs to the RF-amide G protein-coupled receptor family. Even though it is a promising therapeutic target for the treatment of chronic pain, this receptor still has not been used as a drug target.
Lentschat, Hannah, Beck-Sickinger, Annette G.   +1 more
core   +1 more source

Elucidating the molecular pharmacology of VEGFR-1 using NanoBRET

Vascular Endothelial Growth Factor Receptors 1 and 2 (VEGFR-1 and VEGFR-2) are tyrosine kinase receptors that regulate angiogenesis through VEGF binding. Although VEGF-A strongly drives pro-angiogenic responses through VEGFR-2, initial binding studies in

core   +1 more source

A Live-Cell NanoBRET Assay to Monitor RNA–Protein Interactions and Their Inhibition by Small Molecules

ACS Central Science
Jingsong Shan, Amirhossein Taghavi, Elizabeth A. Caine, Ryuichi Sekioka, Veronika Rajchin, James M. Burke, J. Monty Watkins, Jessica L. Childs-Disney, Matthew D. Disney   +8 more
doaj   +1 more source

NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET [PDF]

Cell Reports Methods, 2023
The therapeutic potential of ligands targeting disease-associated membrane proteins is predicted by ligand-receptor binding constants, which can be determined using NanoLuciferase (NanoLuc)-based bioluminescence resonance energy transfer (NanoBRET ...
Raimond Heukers
exaly   +2 more sources