ArticleNature chemical biology2009
Synthetic partial agonists reveal key steps in IP3 receptor activation.
Article in Nature chemical biology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed.
- Article
- From IP3RPEP6 Inhibition of IPCellular and molecular life sciences : CMLS · 2025Review
- Quantal CaCell reports · 2021Article
- A Comparative Perspective on Functionally-Related, Intracellular Calcium Channels: The Insect Ryanodine and Inositol 1,4,5-Trisphosphate Receptors.Biomolecules · 2021Review
- IP3R Channels in Male Reproduction.International journal of molecular sciences · 2020Review
- Article
- Both d- and l-Glucose Polyphosphates Mimic d-Journal of medicinal chemistry · 2020Article
- Reliable measurement of free CaCell calcium · 2020Article
- d-Journal of medicinal chemistry · 2020Article
- Exploration of inositol 1,4,5-trisphosphate (IPScientific reports · 2019Article
- Cryo-EM reveals ligand induced allostery underlying InsPCell research · 2018Article
- Redox regulation of type-I inositol trisphosphate receptors in intact mammalian cells.The Journal of biological chemistry · 2018Article
- Prostaglandin EMolecular pharmacology · 2017Article
- A novel gain-of-function mutation in the ITPR1 suppressor domain causes spinocerebellar ataxia with altered CaJournal of neurology · 2017Article
- Synthesis of dimeric analogs of adenophostin A that potently evoke CaRSC advances · 2016Article
- Inositol 1,4,5-trisphosphate receptors in the endoplasmic reticulum: A single-channel point of view.Cell calcium · 2015Review
- Triazolophostins: a library of novel and potent agonists of IP3 receptors.Organic & biomolecular chemistry · 2015Article
- Aberrant calcium signaling by transglutaminase-mediated posttranslational modification of inositol 1,4,5-trisphosphate receptors.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Intracellular calcium channels: inositol-1,4,5-trisphosphate receptors.European journal of pharmacology · 2014Review
- Interactions of antagonists with subtypes of inositol 1,4,5-trisphosphate (IP3) receptor.British journal of pharmacology · 2014Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
Inositol 1,4,5-trisphosphate receptors (IP(3)Rs) are ubiquitous intracellular Ca2+ channels. IP(3) binding to the IP(3)-binding core (IBC) near the N terminus initiates conformational changes that lead to opening of a pore. The mechanisms underlying this process are unresolved. We synthesized 2-O-modified IP(3) analogs that are partial agonists of IP(3)R. These are similar to IP(3) in their interactions with the IBC, but they are less effective than IP(3) in rearranging the relationship between the IBC and the N-terminal suppressor domain (SD), and they open the channel at slower rates. IP(3)R with a mutation in the SD occupying a position similar to the 2-O substituent of the partial agonists has a reduced open probability that is similar for full and partial agonists. Bulky or charged substituents from either the ligand or the SD therefore block obligatory coupling of the IBC and the SD. Analysis of DeltaG for ligand binding shows that IP(3) is recognized by the IBC and conformational changes then propagate entirely via the SD to the pore.
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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.