Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2
Natalia V. Ortiz Zacarı́as, Kirti Kandhwal Chahal, Tereza Šimková, Cas van der Horst, Yi Zheng, Asuka Inoue, Emy Theunissen, Lloyd Mallee, Daan van der Es, Julien Louvel, Adriaan P. IJzerman, Tracy M. Handel, Irina Kufareva, Laura H. Heitman
Abstract
represents the first covalent ligand reported for CCR2. Due to its unique properties, it may represent a promising tool for ongoing and future studies of CCR2 pharmacology.
Topics & Concepts
ChemistryCovalent bondLigand (biochemistry)G protein-coupled receptorIn silicoAntagonistIn vivoCysteineSmall moleculeCCR2Chemokine receptorPharmacologyReceptorBiochemistryCombinatorial chemistryChemokineBiologyEnzymeBiotechnologyGeneOrganic chemistryChemokine receptors and signalingChemical Synthesis and AnalysisClick Chemistry and Applications