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Updated: Jul 31, 2026
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Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
Published on: November 5, 2014
Phosphodiesterase-4 as a potential drug target
Kam Y J Zhang1, Prabha N Ibrahim, Sam Gillette
1Plexxikon, Inc., 91 Bolivar Drive, Berkeley, CA 94710, USA. kzhang@plexxikon.com
Expert Opinion on Therapeutic Targets
|November 23, 2005
Summary
Phosphodiesterase-4 (PDE4) regulates cell signaling by degrading cAMP. This review covers PDE4
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Phosphodiesterase-4 (PDE4) is a key enzyme regulating cyclic adenosine monophosphate (cAMP) levels.
- PDE4's role in intracellular signaling makes it a target for therapeutic interventions.
- PDE4 inhibitors are explored for indications including inflammation and cognitive enhancement.
Purpose of the Study:
- To review the biological role, distribution, and regulation of PDE4.
- To discuss the historical development and challenges of PDE4 inhibitors.
- To present advances in PDE4 structural biology for rational drug design.
Main Methods:
- Literature review of PDE4's biological functions and signaling pathways.
- Analysis of historical and current PDE4 inhibitor development.
- Examination of recent structural biology studies of PDE4-inhibitor complexes.
Main Results:
- PDE4 is crucial for cAMP-mediated cellular processes across various tissues.
- Numerous chemical classes of PDE4 inhibitors have been developed, facing therapeutic challenges.
- Structural insights are advancing the design of potent and selective PDE4 inhibitors.
Conclusions:
- PDE4 is a significant target for drug development due to its role in cell signaling.
- Overcoming challenges in PDE4 inhibitor therapy requires understanding its structure-activity relationships.
- Advances in structural biology offer promising avenues for developing effective PDE4-based therapeutics.
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