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Novel allosteric ligands of the angiotensin receptor AT1R as autoantibody blockers

Proc Natl Acad Sci U S A. 2021-08; 
Khuraijam Dhanachandra Singh, Zaira P Jara, Terri Harford, Prasenjit Prasad Saha, Triveni R Pardhi, Russell Desnoyer, Sadashiva S Karnik
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Mutant Libraries Complementary DNA encoding the wild-type and mutant (166A, 183A, 187A) HA-AT1R cloned into a pcDNA3.1 expression vector (GenScript). Get A Quote

摘要

While orthosteric ligands of the angiotensin II (AngII) type 1 receptor (AT1R) are available for clinical and research applications, allosteric ligands are not known for this important G protein-coupled receptor (GPCR). Allosteric ligands are useful tools to modulate receptor pharmacology and subtype selectivity. Here, we report AT1R allosteric ligands for a potential application to block autoimmune antibodies. The epitope of autoantibodies for AT1R is outside the orthosteric pocket in the extracellular loop 2. A molecular dynamics simulation study of AT1R structure reveals the presence of a druggable allosteric pocket encompassing the autoantibody epitope. Small molecule binders were then identified for this p... More

关键词

AT1R, GPCRs, allosteric ligand, angiotensin, autoantibody