Results 61 to 70 of about 1,238 (123)

Proximity labeling reveals non-catalytic interactions between DPP9 and ubiquitin signaling complexes

Cellular and Molecular Life Sciences
Dipeptidyl peptidase 9 (DPP9) is an amino-peptidase with roles in immunity, DNA-repair, cell signaling, memory and neonatal survival; its dysregulation is linked to cancer and immune-related disorders.
Valentina Elena Wirtgen, Layla Saied, Samuel Zolg, Marta Campos Alonso, Bettina Mayer, Laura Donzelli, Ulrich Maurer, H. T. Marc Timmers, Klaus-Peter Knobeloch, Oded Kleifeld, Ruth Geiss-Friedlander   +10 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

Comparative evaluation of cell-based assay technologies for scoring drug-induced condensation of SARS-CoV-2 nucleocapsid protein

SLAS Discovery
Protein-nucleic acid phase separation has been implicated in many diseases such as viral infections, neurodegeneration, and cancer. There is great interest in identifying condensate modulators (CMODs), which are small molecules that alter the dynamics ...
Rui Tong Quek, Cyna R. Shirazinejad, Christina L. Young, Kierra S. Hardy, Samuel Lim, Phillip J. Elms, David T. McSwiggen, Timothy J. Mitchison, Pamela A. Silver   +8 more
doaj   +1 more source

TrypPROTACs Unlocking New Therapeutic Strategies for Chagas Disease

Pharmaceuticals
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), continues to pose significant public health challenges due to the toxicity, poor tolerability, and limited efficacy of current treatments.
Ana Luísa Rodriguez Gini, Pamela Souza Tada da Cunha, Emílio Emílio João, Chung Man Chin, Jean Leandro dos Santos, Esteban Carlos Serra, Cauê Benito Scarim   +6 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

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

NanoBRET Tracer Development for Class I Bromodomain Target Engagement in Live Cells. [PDF]

Bioconjug Chem
Sneddon MS, Tsou CJ, Fu X, Shelat AA, Pomerantz WCK.   +4 more
europepmc   +1 more source

Inflammasome adaptor protein ASC is a mechanistic checkpoint in IL-1β maturation. [PDF]

Proc Natl Acad Sci U S A
Saha G, Anchi P, Wang R, Biondo A, Meyer S, Kondragunta V, Luchsinger LL, Syed I, Sharif H, Wu H, Giri Magupalli V.   +10 more
europepmc   +1 more source