In this work we report a design, synthesis, and detailed functional characterization of unique
strongly biased allosteric agonists of CXCR3 that contain tetrahydroisoquinoline …

Over the last decade, functional selectivity (or ligand bias) has evolved from being a peculiar
phenomenon to being recognized as an essential feature of synthetic ligands that target G …

Our recent explorations of allosteric modulators with improved properties resulted in the
identification of two biased negative allosteric modulators, BD103 (N-1-{[3-(4-ethoxyphenyl) …

We have shown previously that different chemical classes of small-molecule antagonists of
the human chemokine CXCR2 receptor interact with distinct binding sites of the receptor …

The chemokine receptor CXCR3 is a G protein‐coupled receptor that conveys extracellular
signals into cells by changing its conformation upon ligand binding. We previously …

Chemokine receptor CXCR3 has attracted much attention, as it is thought to be associated
with a wide range of immune-related diseases. As such, several small molecules with …

The chemokine CXCL12 and its shared seven-transmembrane receptors CXCR4 and
CXCR7 regulate diseases including cancer, atherosclerosis, autoimmunity, and HIV …

The CXCR4 receptor binds with meaningful affinities only CXCL12 and synthetic
antagonists/inverse agonists. We recently described high affinity synthetic agonists for this …

Herein, we report the structure-based development of fluorescent ligands targeting the
intracellular allosteric binding site (IABS) of CXC chemokine receptor 2 (CXCR2), a G …

The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic
obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; …