Rob Leurs

This paper identifies abemaciclib, an FDA-approved CDK4/6 inhibitor, as a potent agonist of ACKR3, an atypical chemokine receptor, revealing its ability to modulate chemokine availability and receptor activity.

This study shows ACKR3 is released on extracellular vesicles under both basal and ligand-induced conditions, sequestering chemokines and opioid peptides and modulating their signaling.

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.

This paper characterizes [3H]AZ12464237 as a high-affinity radioligand for the P2Y12 receptor, showing selectivity and utility in in vitro studies.

This paper designs and characterizes the first photoswitchable small-molecule agonist for ACKR3, showing its selectivity and light-controlled activation properties.

This study identifies GPR182/ACKR5 as a scavenger receptor for CXCL17, GPR15L, and endogenous peptides, revealing distinct binding modes and expanding its ligand repertoire beyond classical chemokines.

This study pharmacologically characterizes seven human H3R isoforms, finding differences in agonist and inverse agonist binding affinities, with implications for drug discovery.

This paper develops genetically encoded sensors to measure histamine release in vitro and in vivo, showing high sensitivity and specificity for extracellular histamine detection.