ArticleThe Biochemical journal2001
Selective recognition of inositol phosphates by subtypes of the inositol trisphosphate receptor.
Article in The Biochemical journal, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed.
- From IP3RPEP6 Inhibition of IPCellular and molecular life sciences : CMLS · 2025Review
- Neuronal microRNAs safeguard ER CaCellular and molecular life sciences : CMLS · 2022Article
- KRAP tethers IPNature communications · 2021Article
- The discovery and development of IP3 receptor modulators: an update.Expert opinion on drug discovery · 2021Article
- Biological Regulatory Network (BRN) Analysis and Molecular Docking Simulations to Probe the Modulation of IPGenes · 2020Article
- d-Journal of medicinal chemistry · 2020Article
- Review
- A synthetic cyclitol-nucleoside conjugate polyphosphate is a highly potent second messenger mimic.Chemical science · 2019Article
- IPCellular and molecular life sciences : CMLS · 2017Review
- The "Other" Inositols and Their Phosphates: Synthesis, Biology, and Medicine (with Recent Advances in myo-Inositol Chemistry).Angewandte Chemie (International ed. in English) · 2016Review
- The type 2 inositol 1,4,5-trisphosphate receptor, emerging functions for an intriguing Ca²⁺-release channel.Biochimica et biophysica acta · 2015Review
- Influence of sex on genetic regulation of "drinking in the dark" alcohol consumption.Mammalian genome : official journal of the International Mammalian Genome Society · 2015Article
- Interactions of antagonists with subtypes of inositol 1,4,5-trisphosphate (IP3) receptor.British journal of pharmacology · 2014Article
- Stimulation of inositol 1,4,5-trisphosphate (IP3) receptor subtypes by adenophostin A and its analogues.PloS one · 2013Article
- Stimulation of inositol 1,4,5-trisphosphate (IP3) receptor subtypes by analogues of IP3.PloS one · 2013Article
- Contribution of phosphates and adenine to the potency of adenophostins at the IP₃ receptor: synthesis of all possible bisphosphates of adenophostin A.Journal of medicinal chemistry · 2012Article
- Inositol 1,4,5-trisphosphate receptor subtype-specific regulation of calcium oscillations.Neurochemical research · 2011Review
- Selective determinants of inositol 1,4,5-trisphosphate and adenophostin A interactions with type 1 inositol 1,4,5-trisphosphate receptors.British journal of pharmacology · 2010Article
- Three-dimensional structure of recombinant type 1 inositol 1,4,5-trisphosphate receptor.The Biochemical journal · 2010Article
- Regulation of inositol 1,4,5-trisphosphate receptors by cAMP independent of cAMP-dependent protein kinase.The Journal of biological chemistry · 2010Article
Corrections and comments
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Synthetic analogues of inositol trisphosphate (IP(3)), all of which included structures equivalent to the 4,5-bisphosphate of (1,4,5)IP(3), were used to probe the recognition properties of rat full-length type 1, 2 and 3 IP(3) receptors expressed in insect Spodoptera frugiperda 9 cells. Using equilibrium competition binding with [(3)H](1,4,5)IP(3) in Ca(2+)-free cytosol-like medium, the relative affinities of the receptor subtypes for (1,4,5)IP(3) were type 3 (K(d)=11+/-2 nM)>type 2 (K(d)=17+/-2 nM)>type 1 (K(d)=24+/-4 nM). (1,4,5)IP(3) binding was reversibly stimulated by increased pH, but the subtypes differed in their sensitivity to pH (type 1>type 2>type 3). For all three subtypes, the equatorial 6-hydroxy group of (1,4,5)IP(3) was essential for high-affinity binding, the equatorial 3-hydroxy group significantly improved affinity, and the axial 2-hydroxy group was insignificant; a 1-phosphate (or in its absence, a 2-phosphate) improved binding affinity. The subtypes differed in the extents to which they tolerated inversion of the 3-hydroxy group of (1,4,5)IP(3) (type 1>type 2>type 3), and this probably accounts for the selectivity of (1,4,6)IP(3) for type 1 receptors. They also differed in their tolerance of inversion, removal or substitution (by phosphate) of the 2-hydroxy group (types 2 and 3>type 1), hence the selectivity of (1,2,4,5)IP(4) for type 2 and 3 receptors. Removal of the 3-hydroxy group or its replacement by fluorine or CH(2)OH was best tolerated by type 3 receptors, and accounts for the selectivity of 3-deoxy(1,4,5)IP(3) for type 3 receptors. Our results provide the first systematic analysis of the recognition properties of IP(3) receptor subtypes and have identified the 2- and 3-positions of (1,4,5)IP(3) as key determinants of subtype selectivity.
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