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Article

Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.

Journal of medicinal chemistry - 11 Mar 2021

Ortiz Zacarías Natalia V, Chahal Kirti K, Šimková Tereza, van der Horst Cas, Zheng Yi, Inoue Asuka, Theunissen Emy, Mallee Lloyd, van der Es Daan, Louvel Julien, IJzerman Adriaan P, Handel Tracy M, Kufareva Irina, Heitman Laura H

Abstract excerpt

Covalently acting inhibitors constitute a large and growing fraction of approved small-molecule therapeutics as well as useful tools for a variety of in vitro and in vivo applications. Here, we aimed to develop a covalent antagonist of CC chemokine receptor 2 (CCR2), a class A GPCR that has been pursued as a therapeutic target in inflammation and immuno-oncology. Based on a known intracellularly binding CCR2...

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Identifiers

PMID: 33600174
DOI: 10.1021/acs.jmedchem.0c01137
PMCID: PMC7958898

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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