Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3
AM Zarca, I Adlere, CP Viciano, M Arimont-Segura… - … pharmacology, 2024 - ASPET
… studies, whereupon CXCR3, CXCR4, and ACKR3 small-molecule ligands were competed
for binding against the radiolabeled agonist. Interestingly, the chemokine ligands CXCL11 …
for binding against the radiolabeled agonist. Interestingly, the chemokine ligands CXCL11 …
Pharmacological characterization of allosteric modulators: A case for chemokine receptors
LS den Hollander, AP IJzerman… - Medicinal Research …, 2024 - Wiley Online Library
… ligands and their pharmacological characterization for modulation of chemokine receptors.
Ligands … Thus, the noncompetitive nature of these small molecule antagonists at CXCR3 and …
Ligands … Thus, the noncompetitive nature of these small molecule antagonists at CXCR3 and …
Effects of Small Molecule Ligands on ACKR3 Receptors
… SIGNIFICANCE STATEMENT We are interested in the signaling produced by the G protein
coupled receptor atypical chemokine receptor 3 (ACKR3), which signals atypically. In this …
coupled receptor atypical chemokine receptor 3 (ACKR3), which signals atypically. In this …
Design, synthesis and pharmacological characterization of the first photoswitchable small-molecule agonist for the Atypical Chemokine Receptor 3
S Berenger, JM Adamska, F Deflorian, C de Graaf… - bioRxiv, 2024 - biorxiv.org
… Photochemical and pharmacological characterisation of ligands 3a-l were performed in …
Ability of inhibition of agonist-induced β-arrestin2 recruitment to indicated chemokine receptors …
Ability of inhibition of agonist-induced β-arrestin2 recruitment to indicated chemokine receptors …
The discovery of small-molecule modulators for the ACKR3 receptor
R Riemens - 2023 - research.vu.nl
… bind to chemokines. The development of drugs acting on chemokine receptors has been
challenging.At present, two small-molecule drugs targeting chemokine receptors have been …
challenging.At present, two small-molecule drugs targeting chemokine receptors have been …
Clinical significance of chemokine receptor antagonists
M Miao, E De Clercq, G Li - Expert Opinion on Drug Metabolism & …, 2020 - Taylor & Francis
… For instance, CCR1, CCR2, CCR5, and CXCR3 are all involved in the … of small-molecule
binding to chemokine receptors offers a promising strategy for virtual screening and drug …
binding to chemokine receptors offers a promising strategy for virtual screening and drug …
Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases
EA Meyer, P Äänismaa, S Froidevaux… - Journal of Medicinal …, 2022 - ACS Publications
… However, despite significant investments by the pharmaceutical industries, only one small-molecule
antagonist (AMG 487) reached the clinical phase. (4,5) Unfortunately, its …
antagonist (AMG 487) reached the clinical phase. (4,5) Unfortunately, its …
Examining the mechanism of action of small-molecule negative allosteric modulators of the human chemokine receptor CXCR2
D Nesheva - 2022 - eprints.nottingham.ac.uk
… For example, chemokine agonists for CCR3 and CXCR3 act … to fine tune their pharmacological
properties at the receptor, and … to provide detailed pharmacological characterisation of …
properties at the receptor, and … to provide detailed pharmacological characterisation of …
Stimulation of the atypical chemokine receptor 3 (ACKR3) by a small-molecule agonist attenuates fibrosis in a preclinical liver but not lung injury model
T Van Loy, S De Jonghe, K Castermans… - Cellular and Molecular …, 2022 - Springer
… chemokine receptor 4 (CXCR4), for which it is the sole ligand, while CXCL11 is also interacting
with chemokine receptor CXCR3… potent and drug-like small molecule agonist was shown …
with chemokine receptor CXCR3… potent and drug-like small molecule agonist was shown …
Structural insights into the activation and inhibition of CXC chemokine receptor 3
H Jiao, B Pang, A Liu, Q Chen, Q Pan… - Nature Structural & …, 2024 - nature.com
… The structures of CXCR3 coupled with small molecule agonists PS372424 and VUF11222 …
of small molecule agonists with chemokines targeting typical chemokine receptors. These two …
of small molecule agonists with chemokines targeting typical chemokine receptors. These two …