Design, synthesis, and pharmacological evaluation of benzimidazolo-thiazoles as potent CXCR3 antagonists with therapeutic potential in autoimmune diseases …

E Caroff, EA Meyer, P Äänismaa… - Journal of Medicinal …, 2022 - ACS Publications
The chemokine receptor CXCR3 allows the selective recruitment of innate and adaptive
inflammatory immune cells into inflamed tissue. CXCR3 ligands are secreted after exposure …

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
The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor
(GPCR) involved in various pathologies, in particular autoimmune diseases. It is activated by …

Discovery of Clinical Candidate ACT-777991, a potent CXCR3 antagonist for antigen-driven and inflammatory pathologies

EA Meyer, P Aanismaa, EA Ertel, E Huhn… - Journal of Medicinal …, 2023 - ACS Publications
The CXCR3 chemokine receptor is a G protein-coupled receptor mainly expressed on
immune cells from the lymphoid lineage, including activated T cells. Binding of its inducible …

Discovery of 3, 4-diaminocyclobut-3-ene-1, 2-dione-based CXCR2 receptor antagonists for the treatment of inflammatory disorders

MP Dwyer, P Biju - Current Topics in Medicinal Chemistry, 2010 - ingentaconnect.com
The CXC chemokine receptor 2 (CXCR2) has attracted a considerable amount of attention
as a target for therapeutic intervention due the key role this receptor plays in a number of …

Exploring the CXCR3 chemokine receptor with small-molecule antagonists and agonists

M Wijtmans, D Scholten, W Mooij, MJ Smit… - … : Chemokines and Their …, 2015 - Springer
CXCR3 is a CXC chemokine receptor that, together with its three major ligands, CXCL9
(MIG), CXCL10 (IP-10), and CXCL11 (I-TAC), is involved in inflammatory responses …

Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist

CE Heise, A Pahuja, SC Hudson, MS Mistry… - … of Pharmacology and …, 2005 - ASPET
The CXC chemokine receptor 3 (CXCR3) is predominantly expressed on T helper type 1
(Th1) cells that are involved in inflammatory diseases. The three CXCR3 ligands CXCL9 …

Towards small‐molecule CXCR3 ligands with clinical potential

M Wijtmans, D Verzijl, R Leurs… - ChemMedChem …, 2008 - Wiley Online Library
The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play
an important role in several diseases, most of which are related to inflammation. This review …

Small molecule CXCR3 antagonists

SP Andrews, RJ Cox - Journal of Medicinal Chemistry, 2016 - ACS Publications
Chemokines and their receptors are known to play important roles in disease. More than 40
chemokine ligands and 20 chemokine receptors have been identified, but, to date, only two …

Designing small molecule CXCR3 antagonists

JE Pease - Expert Opinion on Drug Discovery, 2017 - Taylor & Francis
Introduction: By virtue of its specificity for chemokines induced in Th1-associated
pathologies, CXCR3 has attracted considerable attention as a target for therapeutic …

CXCR4 as a novel target in immunology: moving away from typical antagonists

B Caspar, P Cocchiara, A Melet… - Future Drug …, 2022 - Future Science
CXCR4 has been a target of interest in drug discovery for numerous years. However, so far,
most if not all studies focused on finding antagonists of CXCR4 function. Recent studies …