McCorvy, John D.; Butler, Kyle V.; Kelly, Brendan; Rechsteiner, Katie; Karpiak, Joel; Betz, Robin M.; Kormos, Bethany L.; Shoichet, Brian K.; Dror, Ron O.; Jin, Jian; Roth, Bryan L. published the article 《Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs》. Keywords: indole aripiprazole preparation beta arrestin ligand GPCR dopamine receptor.They researched the compound: 1-Boc-4-Bromoindole( cas:676448-17-2 ).Reference of 1-Boc-4-Bromoindole. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:676448-17-2) here.
Development of biased ligands targeting G protein-coupled receptors (GPCRs) is a promising approach for current drug discovery. Although structure-based drug design of biased agonists remains challenging even with an abundance of GPCR crystal structures, the authors present an approach for translating GPCR structural data into β-arrestin-biased ligands for aminergic GPCRs. The authors identified specific amino acid-ligand contacts at transmembrane helix 5 (TM5) and extracellular loop 2 (EL2) responsible for Gi/o and β-arrestin signaling, resp., and targeted those residues to develop biased ligands. For these ligands, the authors found that bias is conserved at other aminergic GPCRs that retain similar residues at TM5 and EL2. The authors’ approach provides a template for generating arrestin-biased ligands by modifying predicted ligand interactions that block TM5 interactions and promote EL2 interactions. This strategy may facilitate the structure-guided design of arrestin-biased ligands at other GPCRs, including polypharmacol. biased ligands.
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Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI