Unveiling α1-AR secrets: breakthrough structures and targeted drug design NatureComms drugdesign drug target medicine
By Neha MathurAug 14 2023Reviewed by Lily Ramsey, LLM In a recent study published in Nature Communications, researchers explored the structural basis of agonist specificity of α1A-adrenergic receptors .
Researchers have not yet discovered selective pharmacological agonists for α1-ARs; hence, their therapeutic potential remains largely unexplored. About the study The present study used cryo-electron microscopy to decipher the molecular structures of α1A-AR/Gq complexes with epinephrine at 2.6 angstroms and A61603 at 3.0 Å.
The team created three point mutants, α1A-AR, α1A-AR, and α1A-AR, by mutating three residues involved in hydrophobic interactions with A61603, namely V1855.40, A1895.44, and M2926.55 to the corresponding residues in α1B-AR.
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