ArticleMolecular pharmacology2010
Binding of inositol 1,4,5-trisphosphate (IP3) and adenophostin A to the N-terminal region of the IP3 receptor: thermodynamic analysis using fluorescence polarization with a novel IP3 receptor ligand.
Article in Molecular pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 37 citations in OpenAlex.
- An Experimental Framework for Developing Point-of-Need Biosensors: Connecting Bio-Layer Interferometry and Electrochemical Impedance Spectroscopy.Biosensors · 2022Pooled it
- Substrate promiscuity of inositol 1,4,5-trisphosphate kinase driven by structurally-modified ligands and active site plasticity.Nature communications · 2024Article
- An X-Domain Phosphoinositide Phospholipase C (PI-PLC-like) ofPathogens (Basel, Switzerland) · 2023Article
- Combining IPCurrent research in microbial sciences · 2023Article
- Biophysical characterization of the DNA binding motif of human phospholipid scramblase 1.European biophysics journal : EBJ · 2022Article
- Quantal CaCell reports · 2021Article
- Ten-eleven translocation 1 mediated-DNA hydroxymethylation is required for myelination and remyelination in the mouse brain.Nature communications · 2021Article
- Rapid stimulation of cellular Pi uptake by the inositol pyrophosphate InsPChemical science · 2020Article
- Exploration of inositol 1,4,5-trisphosphate (IPScientific reports · 2019Article
- Hindered cytoplasmic diffusion of inositol trisphosphate restricts its cellular range of action.Science signaling · 2016Article
- IP3 receptors: Take four IP3 to open.Science signaling · 2016Article
- The "Other" Inositols and Their Phosphates: Synthesis, Biology, and Medicine (with Recent Advances in myo-Inositol Chemistry).Angewandte Chemie (International ed. in English) · 2016Review
- Cellular internalisation of an inositol phosphate visualised by using fluorescent InsP5.Chembiochem : a European journal of chemical biology · 2014Article
- Article
- 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
- Analysis of protein-ligand interactions by fluorescence polarization.Nature protocols · 2011Article
- Mitochondrial reactive oxygen species are activated by mGluR5 through IP3 and activate ERK and PKA to increase excitability of amygdala neurons and pain behavior.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2011Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Inositol 1,4,5-trisphosphate (IP(3)) receptors (IP(3)R) are intracellular Ca(2+) channels. Their opening is initiated by binding of IP(3) to the IP(3)-binding core (IBC; residues 224-604 of IP(3)R1) and transmitted to the pore via the suppressor domain (SD; residues 1-223). The major conformational changes leading to IP(3)R activation occur within the N terminus (NT; residues 1-604). We therefore developed a high-throughput fluorescence polarization (FP) assay using a newly synthesized analog of IP(3), fluorescein isothiocyanate (FITC)-IP(3), to examine the thermodynamics of IP(3) and adenophostin A binding to the NT and IBC. Using both single-channel recording and the FP assay, we demonstrate that FITC-IP(3) is a high-affinity partial agonist of the IP(3)R. Conventional [(3)H]IP(3) and FP assays provide similar estimates of the K(D) for both IP(3) and adenophostin A in cytosol-like medium at 4 degrees C. They further establish that the isolated IBC retains the ability of full-length IP(3)R to bind adenophostin A with approximately 10-fold greater affinity than IP(3). By examining the reversible effects of temperature on ligand binding, we established that favorable entropy changes (T Delta S) account for the greater affinities of both ligands for the IBC relative to the NT and for the greater affinity of adenophostin A relative to IP(3). The two agonists differ more substantially in the relative contribution of Delta H and T Delta S to binding to the IBC relative to the NT. This suggests that different initial binding events drive the IP(3)R on convergent pathways toward a similar open state.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.