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Guanophostin A, the guanosine counterpart of the inositol 1,4,5-trisphosphate receptor agonist adenophostin A, has been synthesized and is the first synthetic adenophostin A-like analogue to be equipotent to its parent in stimulating intracellular Ca2+ release; its nucleotide moiety is proposed to interact with the receptor binding core by guanine base cation-pi stacking with Arg504 and hydrogen bonding with Glu505 and interaction of the ribosyl 2'-phosphate group with the helix-dipole of alpha6.

Original publication

DOI

10.1039/b517911d

Type

Journal article

Journal

Chem Commun (Camb)

Publication Date

21/05/2006

Pages

2015 - 2017

Keywords

Animals, Calcium, Calcium Channel Agonists, Guanine, Guanosine, Hydrogen Bonding, Inositol 1,4,5-Trisphosphate Receptors, Mice, Models, Molecular, Protein Binding, Structure-Activity Relationship