A synthetic diphosphoinositol phosphate analogue of inositol trisphosphate.

ABSTRACT: Diphosphoinositol phosphates (PP-InsPs) are inositol phosphates (InsPs) that contain PP (diphosphate) groups. Converting a phosphate group in an InsP into a diphosphate has been reported to enhance affinity for some binding proteins. We synthesised 1-PP-Ins(4,5)P₂, the first diphosphate analogue of the intracellular signalling molecule InsP₃, and examined its effects on InsP₃ receptors, which are intracellular Ca²⁺ channels. 1-PP-Ins(4,5)P₂ was indistinguishable from InsP₃ in its ability to bind to and activate type 1 InsP₃ receptors, indicating that the diphosphate modification of InsP₃ affected neither affinity nor efficacy. Nevertheless, 1-PP-Ins(4,5)P₂ is the most potent 1-phosphate modif

SUBMITTER: Riley AM 

PROVIDER: S-EPMC6071853 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature