Inhibition of constitutive activity of the atypical chemokine receptor ACKR3 by the small-molecule inverse agonist VUF16840
Reggie Bosma, Desislava N. Nesheva, Merel Rijnsburger, Rick Riemens, Justyna M. Adamska, Max Meyrath, Simon Mobach, Maurice C. M. L. Buzink, Suzanne van der Pol, Iwan J. P. de Esch, Martyna Szpakowska, Maikel Wijtmans, Andy Chevigné, Henry F. Vischer, Rob Leurs
This study characterizes VUF16840 as a selective inverse agonist of ACKR3 that inhibits constitutive and chemokine-induced signaling by stabilizing the inactive conformation of the receptor.
Molecular Pharmacology · Oct 26, 2025Peer-reviewedPharmacology & Toxicology