ArticleJournal of medicinal chemistry2007
Novel N7- and N1-substituted cGMP derivatives are potent activators of cyclic nucleotide-gated channels.
Article in Journal of medicinal chemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 11 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
11 citing papers in PubMed, 17 citations in OpenAlex.
- Structural Domains Associated with Permeation, Gating, and Selectivity of Aquaporin Ion Channels Found Across Phyla.Advances in experimental medicine and biology · 2026Review
- Similar Binding Modes of cGMP Analogues Limit Selectivity in Modulating Retinal CNG Channels via the Cyclic Nucleotide-Binding Domain.ACS chemical neuroscience · 2024Article
- Fluorophore-Labeled Cyclic Nucleotides as Potent Agonists of Cyclic Nucleotide-Regulated Ion Channels.Chembiochem : a European journal of chemical biology · 2020Article
- Novel Fluorescent Cyclic Nucleotide Derivatives to Study CNG and HCN Channel Function.Biophysical journal · 2019Article
- Hydrophobic alkyl chains substituted to the 8-position of cyclic nucleotides enhance activation of CNG and HCN channels by an intricate enthalpy - entropy compensation.Scientific reports · 2018Article
- Article
- Development of new 1,3-diazaphenoxazine derivatives (thioG-grasp) to covalently capture 8-thioguanosine.Molecules (Basel, Switzerland) · 2015Article
- Halogen substituents on the aromatic moiety of the tetracaine scaffold improve potency of cyclic nucleotide-gated channel block.Bioorganic & medicinal chemistry letters · 2011Article
- Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.Journal of medicinal chemistry · 2011Article
- Epac signaling is required for hippocampus-dependent memory retrieval.Proceedings of the National Academy of Sciences of the United States of America · 2008Article
- Block of cyclic nucleotide-gated channels by tetracaine derivatives: role of apolar interactions at two distinct locations.Bioorganic & medicinal chemistry letters · 2008Article
Corrections and comments
- Erratum issued
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Cyclic nucleotide-gated (CNG) channels, key players in olfactory and visual signal transduction, generate electrical responses to odorant- and light-induced changes in cyclic nucleotide concentration. Previous work suggests that substitutions are tolerated solely at the C8 position on the purine ring of cGMP. Our studies with C8, 2'-OH, and 2-NH2-modified cGMP derivatives support this assertion. To gain further insight into determinants important for CNG channel binding and activation, we targeted previously unexplored positions. Modifications at N7 of 8-SH-cGMP (6) are well tolerated by olfactory and retinal rod CNG channels. Toleration of a very large substituent, a 3400 molecular weight PEG, at either N7 or C8 argues for broad accommodation at these positions in the binding site. Modification at N1 of cGMP reduces the apparent affinity for the channel; however, when combined with 8-parachlorophenylthio derivatization, the resulting cGMP analogue is more potent than cGMP itself. These studies establish the N7 and N1 positions of cGMP as targets for modification in the design of novel CNG channel agonists.
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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.