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 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.
Sureshan
Kana M
KM
Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, UK BA2 7AY.
Trusselle
Melanie
M
Tovey
Stephen C
SC
Taylor
Colin W
CW
Potter
Barry V L
BV
D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002120:Calcium Channel Agonists / Q000737:chemistry / Q000494:pharmacology*; D006147:Guanine / Q000031:analogs & derivatives*; D006151:Guanosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006860:Hydrogen Bonding; D053496:Inositol 1,4,5-Trisphosphate Receptors / Q000819:agonists* / Q000378:metabolism; D051379:Mice; D008958:Models, Molecular; D011485:Protein Binding; D013329:Structure-Activity Relationship
D002120:Calcium Channel Agonists; D053496:Inositol 1,4,5-Trisphosphate Receptors; C519369:guanophostin A; D006151:Guanosine; D006147:Guanine; D002118:Calcium