Guanophostin A: Synthesis and evaluation of a high affinity agonist of the d-myo-inositol 1,4,5-trisphosphate receptor

Sureshan, Kana M. ; Trusselle, Melanie ; Tovey, Stephen C. ; Taylor, Colin W. ; Potter, Barry V. L. (2006) Guanophostin A: Synthesis and evaluation of a high affinity agonist of the d-myo-inositol 1,4,5-trisphosphate receptor Chemical Communications (19). p. 2015. ISSN 1359-7345

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Official URL: http://doi.org/10.1039/B517911D

Related URL: http://dx.doi.org/10.1039/B517911D

Abstract

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-π stacking with Arg504 and hydrogen bonding with Glu505 and interaction of the ribosyl 2′-phosphate group with the helix-dipole of α6.

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