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The functional significance of the 2- and 3-hydroxyl groups of 1 D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] was probed by using Ins(1,4,5)P3 analogues variously modified at positions 2 and 3 or elsewhere. The intrinsic activities of these compounds were compared to that of Ins(1,4,5)P3, using the calcium-mobilising receptor of the 1321N1 human astrocytoma cell line. The ligand-binding affinities were also determined using membrane preparations from rat cerebellum and bovine adrenal cortex. The results show that HO-2 and HO-3 of Ins(1,4,5)P3 have a relatively insignificant role in receptor binding and calcium release. However, the possibility of a regulatory role for the 3-position of Ins(1,4,5)P3 in these processes is proposed.

Type

Journal

Carbohydr Res

Publication Date

09/10/1992

Volume

234

Pages

237 - 246

Keywords

Adrenal Cortex, Animals, Astrocytoma, Calcium, Calcium Channels, Cattle, Cell Membrane Permeability, Cerebellum, Humans, Hydroxylation, Inositol 1,4,5-Trisphosphate, Inositol 1,4,5-Trisphosphate Receptors, Molecular Structure, Rats, Receptors, Cell Surface, Receptors, Cytoplasmic and Nuclear, Tumor Cells, Cultured