Guanophostin A: Synthesis and evaluation of a high affinity agonist of the D-myo-inositol 1,4,5-trisphosphate receptor
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 i...
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Veröffentlicht in: | Chemical communications (Cambridge, England) England), 2006-01 (19), p.2015-2017 |
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container_end_page | 2017 |
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container_issue | 19 |
container_start_page | 2015 |
container_title | Chemical communications (Cambridge, England) |
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creator | Sureshan, Kana M Trusselle, Melanie Tovey, Stephen C Taylor, Colin W Potter, Barry V L |
description | 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. |
doi_str_mv | 10.1039/b517911d |
format | Article |
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source | MEDLINE; Royal Society Of Chemistry Journals; Royal Society of Chemistry Journals Archive (1841-2007); Alma/SFX Local Collection |
subjects | Animals Calcium - metabolism Calcium Channel Agonists - chemistry Calcium Channel Agonists - pharmacology Guanine - analogs & derivatives Guanosine - analogs & derivatives Guanosine - chemical synthesis Guanosine - chemistry Guanosine - pharmacology Hydrogen Bonding Inositol 1,4,5-Trisphosphate Receptors - agonists Inositol 1,4,5-Trisphosphate Receptors - metabolism Mice Models, Molecular Protein Binding Structure-Activity Relationship |
title | Guanophostin A: Synthesis and evaluation of a high affinity agonist of the D-myo-inositol 1,4,5-trisphosphate receptor |
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