ArticleJournal of biomolecular screening2008
Development of a fission yeast-based high-throughput screen to identify chemical regulators of cAMP phosphodiesterases.
Article in Journal of biomolecular screening, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed, 37 citations in OpenAlex.
- A fission yeast-based platform for nematode PDE inhibitor discovery.Cellular signalling · 2026Article
- Integrated analysis of single-cell RNA sequencing, transcriptomics, and thermal proteome profiling identifies PLCG1 as the therapeutic target of isopimpinellin in treating rheumatoid arthritis.Cellular & molecular biology letters · 2026Article
- A multiplexed, three-dimensional pooling and next-generation sequencing strategy for creating barcoded mutant arrays: construction of a Schizosaccharomyces pombe transposon insertion library.Nucleic acids research · 2022Article
- cAMP export by the fission yeastmicroPublication biology · 2021Article
- Use of a Fission Yeast Platform to Identify and Characterize Small Molecule PDE Inhibitors.Frontiers in pharmacology · 2021Review
- Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages.PLoS neglected tropical diseases · 2020Article
- A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.Cellular signalling · 2019Article
- Development of A Fission Yeast Cell-Based Platform for High Throughput Screening of HIV-1 Protease Inhibitors.Current HIV research · 2019Article
- Identification and characterization of a potent and biologically-active PDE4/7 inhibitor via fission yeast-based assays.Cellular signalling · 2017Article
- Panspecies small-molecule disruptors of heterochromatin-mediated transcriptional gene silencing.Molecular and cellular biology · 2015Article
- Anti-cancer drug discovery: update and comparisons in yeast, Drosophila, and zebrafish.Current molecular pharmacology · 2014Article
- Article
- Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay.European journal of pharmacology · 2011Article
- Use of a Schizosaccharomyces pombe PKA-repressible reporter to study cGMP metabolising phosphodiesterases.Cellular signalling · 2011Article
- A fission yeast-based platform for phosphodiesterase inhibitor HTSs and analyses of phosphodiesterase activity.Handbook of experimental pharmacology · 2011Review
- New classes of PDE7 inhibitors identified by a fission yeast-based HTS.Journal of biomolecular screening · 2010Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Cyclic nucleotide phosphodiesterases (PDEs) comprise a superfamily of enzymes that serve as drug targets in many human diseases. There is a continuing need to identify high-specificity inhibitors that affect individual PDE families or even subtypes within a single family. The authors describe a fission yeast-based high-throughput screen to detect inhibitors of heterologously expressed adenosine 3',5'-cyclic monophosphate (cAMP) PDEs. The utility of this system is demonstrated by the construction and characterization of strains that express mammalian PDE2A, PDE4A, PDE4B, and PDE8A and respond appropriately to known PDE2A and PDE4 inhibitors. High-throughput screens of 2 bioactive compound libraries for PDE inhibitors using strains expressing PDE2A, PDE4A, PDE4B, and the yeast PDE Cgs2 identified known PDE inhibitors and members of compound classes associated with PDE inhibition. The authors verified that the furanocoumarin imperatorin is a PDE4 inhibitor based on its ability to produce a PDE4-specific elevation of cAMP levels. This platform can be used to identify PDE activators, as well as genes encoding PDE regulators, which could serve as targets for future drug screens.
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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.