ArticleProceedings of the National Academy of Sciences of the United States of America2019
Small-molecule allosteric activators of PDE4 long form cyclic AMP phosphodiesterases.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 78 citations in OpenAlex.
- Review
- KTX207-mediated PDE4D degradation disrupts tumour cell migration, invasion, and angiogenic potential.Cell communication and signaling : CCS · 2026Article
- PDE4B deficiency aids macrophage differentiation and contributes to Cryptococcus neoformans brain infection.PLoS pathogens · 2026Article
- Posttranslational modifications of phosphodiesterase type 4 enzymes represent novel points for therapeutic targeting.The FEBS journal · 2025Review
- Renal tissue-resident macrophages promote cystogenesis in early polycystic kidney disease.Journal of cell science · 2025Article
- Transforming advancing autosomal dominant polycystic kidney disease care: investigating new horizons in treatment and research.Inflammopharmacology · 2025Review
- Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera.The FEBS journal · 2025Article
- Cyclic nucleotide phosphodiesterases as drug targets.Pharmacological reviews · 2025Review
- Biochemical pharmacology of adenylyl cyclases in cancer.Biochemical pharmacology · 2024Review
- Cyclic Adenosine Monophosphate Signaling in Chronic Kidney Disease: Molecular Targets and Therapeutic Potentials.International journal of molecular sciences · 2024Review
- Vinpocetine, a phosphodiesterase 1 inhibitor, mitigates atopic dermatitis-like skin inflammation.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2024Article
- Inactivation of phosphodiesterase-4B gene in rat nucleus accumbens shell by CRISPR/Cas9 or positive allosteric modulation of the protein affects the motivation to chronically self-administer nicotine.Scientific reports · 2024Article
- Article
- The evolution of small molecule enzyme activators.RSC medicinal chemistry · 2023Review
- Loss of PDE4D7 expression promotes androgen independence, neuroendocrine differentiation and alterations in DNA repair: implications for therapeutic strategies.British journal of cancer · 2023Article
- Regulation of cardiac function by cAMP nanodomains.Bioscience reports · 2023Review
- Compartmentalised cAMP signalling in the primary cilium.Frontiers in physiology · 2023Review
- The Complexity and Multiplicity of the Specific cAMP Phosphodiesterase Family: PDE4, Open New Adapted Therapeutic Approaches.International journal of molecular sciences · 2022Review
- A cAMP signalosome in primary cilia drives gene expression and kidney cyst formation.EMBO reports · 2022Article
- Epitope alteration by small molecules and applications in drug discovery.Chemical science · 2022Article
Corrections and comments
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Authors and funding
22 authors at 9 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cyclic AMP (cAMP) phosphodiesterase-4 (PDE4) enzymes degrade cAMP and underpin the compartmentalization of cAMP signaling through their targeting to particular protein complexes and intracellular locales. We describe the discovery and characterization of a small-molecule compound that allosterically activates PDE4 long isoforms. This PDE4-specific activator displays reversible, noncompetitive kinetics of activation (increased
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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.