Homobivalent Dopamine D2 Receptor Ligands Modulate the Dynamic Equilibrium of D2 Monomers and Homo- and Heterodimers.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical biology"
DOI: 10.1021/acschembio.0c00895
Abstract: Dopamine D2 receptors (D2Rs) are major targets in the treatment of psychiatric and neurodegenerative diseases. As with many other G protein-coupled receptors (GPCRs), D2Rs interact within the cellular membrane, leading to a transient receptor homo-… read more here.
Keywords: dynamic equilibrium; dopamine; equilibrium monomers; bivalent ligands ... See more keywords
Exploring the signaling space of a GPCR using bivalent ligands with a rigid oligoproline backbone.
Sign Up to like & getrecommendations! Published in 2021 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2108776118
Abstract: G protein-coupled receptors (GPCRs) are one of the most important drug-target classes in pharmaceutical industry. Their diversity in signaling, which can be modulated with drugs, permits the design of more effective and better-tolerated therapeutics. In… read more here.
Keywords: space; exploring signaling; rigid oligoproline; distance ... See more keywords