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Nicotinamide 8-Br-hypoxanthine dinucleotide (8-Br-NHD+) was cyclised at the N-1 position by ADP-ribosyl cyclase from Aplysia californica to give cyclic 8-Br-inosine diphosphoribose, a novel membrane-permeant analogue of cyclic-ADP ribose and agonist in human T cells. Adenine-substituted analogues of adenophostin A with potent Ca2+ releasing activity were synthesized; docking studies using the binding core of the Ins(1,4,5)P3 receptor identified specific residues that could be of importance in determining the hyperagonist nature of adenophostin activity.

Type

Journal article

Journal

Nucleic Acids Res Suppl

Publication Date

2003

Pages

1 - 2

Keywords

Adenosine, Animals, Aplysia, Calcium, Calcium Channels, Cyclic ADP-Ribose, Humans, Inositol 1,4,5-Trisphosphate Receptors, Nucleic Acid Conformation, Receptors, Cytoplasmic and Nuclear, Signal Transduction