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 …
Small molecule CXCR3 antagonists
SP Andrews, RJ Cox - Journal of Medicinal Chemistry, 2016 - ACS Publications
… chemokine ligands and 20 chemokine receptors have been identified, but, to date, only two
small molecule chemokine receptor … The chemokine receptor CXCR3 was identified in 1996, …
small molecule chemokine receptor … The chemokine receptor CXCR3 was identified in 1996, …
Designing small molecule CXCR3 antagonists
JE Pease - Expert Opinion on Drug Discovery, 2017 - Taylor & Francis
… of leukocyte migration by interfering with chemokine receptor signaling is an attractive … both
academia and the pharmaceutical industry. The chemokine receptor CXCR3 is expressed by …
academia and the pharmaceutical industry. The chemokine receptor CXCR3 is expressed by …
Discovery and characterization of biased allosteric agonists of the chemokine receptor CXCR3
L Milanos, R Brox, T Frank, G Poklukar… - Journal of Medicinal …, 2016 - ACS Publications
… (16) Besides this, the development of small-molecule agonists of CXCR3 was largely … We
combined this approach with detailed pharmacological characterization of novel compounds …
combined this approach with detailed pharmacological characterization of novel compounds …
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 …
Molecular pharmacology of chemokine receptors
RH de Wit, SM de Munnik, R Leurs, HF Vischer… - Methods in …, 2016 - Elsevier
… Small molecule and antibody-based antagonists have been … Displacement binding allows
pharmacological characterization of … -dependent manner in CXCR3-expressing HEK293 cells. …
pharmacological characterization of … -dependent manner in CXCR3-expressing HEK293 cells. …
Structure–activity relationships and biological characterization of a novel, potent, and serum stable CXC chemokine receptor type 4 (CXCR4) antagonist
S Di Maro, FS Di Leva, AM Trotta… - Journal of Medicinal …, 2017 - ACS Publications
… CXCR3 chemokine receptors and remains unaltered up to 2 h in human serum. Moreover,
NMR and advanced molecular modeling studies allowed us to define the structural reasons …
NMR and advanced molecular modeling studies allowed us to define the structural reasons …