ArticleJournal of biomolecular screening2010
New classes of PDE7 inhibitors identified by a fission yeast-based HTS.
Article in Journal of biomolecular screening, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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The trial behind it
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Who cites it
14 citing papers in PubMed.
- A fission yeast-based platform for nematode PDE inhibitor discovery.Cellular signalling · 2026Article
- Yeast as a Model for Human Disease.International journal of molecular sciences · 2026Review
- Recent Advances in Medicinal Chemistry of Phosphodiesterase 7 Inhibitors and their Potential Therapeutic Applications.Recent advances in inflammation & allergy drug discovery · 2025Review
- 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
- Potential use of Pichia pastoris strain SMD1168H expressing DNA topoisomerase I in the screening of potential anti‑breast cancer agents.Molecular medicine reports · 2019Article
- Phosphodiesterase 4 and 7 inhibitors produce protective effects against high glucose-induced neurotoxicity in PC12 cells via modulation of the oxidative stress, apoptosis and inflammation pathways.Metabolic brain disease · 2018Article
- Multiple cAMP Phosphodiesterases Act Together to Prevent Premature Oocyte Meiosis and Ovulation.Endocrinology · 2018Article
- Identification and characterization of a potent and biologically-active PDE4/7 inhibitor via fission yeast-based assays.Cellular signalling · 2017Article
- The Concise Guide to PHARMACOLOGY 2013/14: enzymes.British journal of pharmacology · 2013Article
- Article
- 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
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Studies of the phosphodiesterase PDE7 family are impeded by there being only one commercially available PDE7 inhibitor, BRL50481. The authors have employed a high-throughput screen of commercial chemical libraries, using a fission yeast-based assay, to identify PDE7 inhibitors that include steroids, podocarpanes, and an unusual heterocyclic compound, BC30. In vitro enzyme assays measuring the potency of BC30 and 2 podocarpanes, in comparison with BRL50481, produce data consistent with those from yeast-based assays. In other enzyme assays, BC30 stimulates the PDE4D catalytic domain but not full-length PDE4D2, suggesting an allosteric site of action. BC30 significantly enhances the anti-inflammatory effect of the PDE4 inhibitor rolipram as measured by release of tumor necrosis factor alpha from activated monocytes. These studies introduce several new PDE7 inhibitors that may be excellent candidates for medicinal chemistry because of the requirements for drug-like characteristics placed on them by the nature of the yeast-based screen.
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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.