Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor

Autor: Daan van der Es, Adriaan P. IJzerman, Jelle Offringa, Xue Yang, Laura H. Heitman, Eelke B. Lenselink, Jacobus P. D. van Veldhoven, Boaz J. Kuiper

Publikováno v: Journal of Medicinal Chemistry, 62(7), 3539-3552
Journal of Medicinal Chemistry

The development of covalent ligands for G protein-coupled receptors (GPCRs) is not a trivial process. Here, we report a streamlined workflow thereto from synthesis to validation, exemplified by the discovery of a covalent antagonist for the human ade

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bf14842a65be649f77157c82babf912
http://hdl.handle.net/1887/80320

Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A(3) Receptor Antagonists

Autor: Eelke B. Lenselink, Jacobus P. D. van Veldhoven, Tirsa T. van Duijl, Laura H. Heitman, Adriaan P. IJzerman, Boaz J. Kuiper, Ellen Paasman, Lizi Xia, Wessel A.C. Burger

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 60(17), 7555-7568
Journal of Medicinal Chemistry, 60(17), 7555-7568. AMER CHEMICAL SOC

We expanded on a series of pyrido[2,1-f]purine-2,4-dione derivatives as human adenosine A3 receptor (hA3R) antagonists to determine their kinetic profiles and affinities. Many compounds showed high affinities and a diverse range of kinetic profiles.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06ecab5d892365671aa9093720b68b2e
https://hdl.handle.net/1887/135658