1350765-47-7Relevant academic research and scientific papers
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2
Ortiz Zacarías, Natalia V.,Chahal, Kirti K.,?imková, 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.
, p. 2608 - 2621 (2021/03/09)
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 recept
CCR2 receptor antagonists: Optimization of biaryl sulfonamides to increase activity in whole blood
Wang, Gren Z.,Haile, Pamela A.,Daniel, Tom,Belot, Benjamin,Viet, Andrew Q.,Goodman, Krista B.,Sha, Deyou,Dowdell, Sarah E.,Varga, Norbert,Hong, Xuan,Chakravorty, Subhas,Webb, Christine,Cornejo, Carla,Olzinski, Alan,Bernard, Roberta,Evans, Christopher,Emmons, Amanda,Briand, Jacques,Chung, Chun-Wa,Quek, Ruben,Lee, Dennis,Gough, Peter J.,Sehon, Clark A.
, p. 7291 - 7294 (2012/02/04)
A series of biarylsulfonamides was identified as hCCR2 receptor antagonist but suffered from high plasma protein binding resulting in a >100 fold shift in activity in a functional GTPγS assay run in tandem in the presence and absence of human serum albumin. Introduction of an aryl amide with ethylenediamine linker led to compounds with reduced shifts and improved activity in whole blood.
