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Related Concept Videos

Phosphodiester Linkages01:01

Phosphodiester Linkages

Overview
Phosphodiester bond forms when a phosphoric acid molecule (H3PO4) links with two hydroxyl groups (–OH) of two other molecules, forming two ester bonds. Two water molecules are released in this process. The phosphodiester bond is commonly found in nucleic acids (DNA and RNA) and plays a critical role in their structure and function.
Phosphodiester Bonds Link Nucleotides Together
DNA and RNA are polynucleotides or long chains of nucleotides that are linked together. A nucleotide is...
Intracellular Signaling Cascades01:24

Intracellular Signaling Cascades

Once a ligand binds to a receptor, the signal is transmitted through the membrane and into the cytoplasm. The continuation of a signal in this manner is called signal transduction. Signal transduction only occurs with cell-surface receptors, which cannot interact with most components of the cell, such as DNA. Only internal receptors can interact directly with DNA in the nucleus to initiate protein synthesis. When a ligand binds to its receptor, conformational changes occur that affect the...
GTPases and their Regulation02:14

GTPases and their Regulation

Guanine nucleotide-binding proteins (G-proteins), also known as GTPases, are a superfamily of proteins that regulate many cellular processes, such as cell signaling, vesicular transport, and the regulation of cell shape and motility. Mutation or dysfunction of these proteins can lead to disease. There are around 40,000 known G-proteins that can broadly be classified into two groups ‒  small G-proteins consisting of a single domain and large multi-domain G-proteins.
Large G-proteins, also known...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
cAMP-dependent Protein Kinase Pathways01:25

cAMP-dependent Protein Kinase Pathways

Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

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Related Experiment Video

Updated: May 7, 2026

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
12:26

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay

Published on: May 3, 2018

Cyclic nucleotide phosphodiesterases.

D M Essayan1

  • 1Division of Clinical Trials Design and Analysis, Office of Therapeutics Research and Review, Center for Biologics Evaluation and Research, US Food and Drug Administration, Rockville, MD 20852, USA.

The Journal of Allergy and Clinical Immunology
|November 3, 2001
PubMed
Summary
This summary is machine-generated.

Selective phosphodiesterase (PDE) inhibitors show promise for treating immune and inflammatory diseases by modulating cyclic nucleotide signaling. Research reviews in vitro, preclinical, and clinical data on their immunomodulatory potential.

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Last Updated: May 7, 2026

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
12:26

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay

Published on: May 3, 2018

Mapping the Cellular Distribution of an Optogenetic Protein Using a Light-Stimulation Grid
08:49

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Published on: January 26, 2024

Measurement of Cyclic Guanosine Monophosphate (cGMP) in Solid Tissues using Competitive Enzyme-Linked Immunosorbent Assay (ELISA)
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Measurement of Cyclic Guanosine Monophosphate (cGMP) in Solid Tissues using Competitive Enzyme-Linked Immunosorbent Assay (ELISA)

Published on: July 3, 2025

Area of Science:

  • Biochemistry
  • Pharmacology
  • Immunology

Background:

  • Cyclic nucleotide second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), are crucial in cellular signal transduction.
  • The phosphodiesterase (PDE) enzyme superfamily regulates intracellular levels of cAMP and cGMP.
  • Dysregulation of PDE activity is implicated in various physiological and pathological processes.

Purpose of the Study:

  • To review the therapeutic potential of selective phosphodiesterase (PDE) inhibitors in immune and inflammatory diseases.
  • To summarize current in vitro, preclinical, and clinical evidence supporting PDE inhibitors as immunomodulatory agents.

Main Methods:

  • Literature review of in vitro studies.
  • Analysis of preclinical (animal model) data.
  • Evaluation of clinical trial results.

Main Results:

  • Specific PDE types are validated as therapeutic targets for immune/inflammatory conditions.
  • Selective PDE inhibitors demonstrate immunomodulatory effects across various disease models.
  • Emerging clinical data suggest efficacy in treating inflammatory disorders.

Conclusions:

  • Selective PDE inhibitors represent a promising class of therapeutics for immune and inflammatory diseases.
  • Further clinical investigation is warranted to fully establish the role of PDE inhibitors in managing these conditions.