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- W2594829311 abstract "The adenosine A1 receptor (A1-AR) is a G-protein-coupled receptor that plays a vital role in cardiac, renal, and neuronal processes but remains poorly targeted by current drugs. We determined a 3.2 Å crystal structure of the A1-AR bound to the selective covalent antagonist, DU172, and identified striking differences to the previously solved adenosine A2A receptor (A2A-AR) structure. Mutational and computational analysis of A1-AR revealed a distinct conformation of the second extracellular loop and a wider extracellular cavity with a secondary binding pocket that can accommodate orthosteric and allosteric ligands. We propose that conformational differences in these regions, rather than amino-acid divergence, underlie drug selectivity between these adenosine receptor subtypes. Our findings provide a molecular basis for AR subtype selectivity with implications for understanding the mechanisms governing allosteric modulation of these receptors, allowing the design of more selective agents for the treatment of ischemia-reperfusion injury, renal pathologies, and neuropathic pain." @default.
- W2594829311 created "2017-03-16" @default.
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- W2594829311 date "2017-02-01" @default.
- W2594829311 modified "2023-10-14" @default.
- W2594829311 title "Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity" @default.
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- W2594829311 doi "https://doi.org/10.1016/j.cell.2017.01.042" @default.
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