Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Antihypertensive Drugs: Vasodilators01:23

Antihypertensive Drugs: Vasodilators

Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

"HRCT predictors of GGO surgical resection: Histopathological and molecular correlation in the era of lung sparing surgery".

Lung cancer (Amsterdam, Netherlands)·2022
Same author

Pleuroparenchymal fibroelastosis (PPFE) associated with giant cell arteritis: A coincidence or a novel phenotype?

Respiratory medicine case reports·2019
Same author

Combined sarcoidosis and idiopathic pulmonary fibrosis (CSIPF): A novel disease phenotype?

Respiratory medicine·2019
Same author

Altered gene expression profiles in the lungs of benzo[a]pyrene-exposed mice in the presence of lipopolysaccharide-induced pulmonary inflammation.

Toxicology and applied pharmacology·2017
Same author

Type II congenital pulmonary airway malformation associated with intralobar pulmonary sequestration: report of a case and review of classification criteria.

Pathologica·2017
Same author

Xanthines and Phosphodiesterase Inhibitors.

Handbook of experimental pharmacology·2016

Related Experiment Video

Updated: Jul 3, 2026

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
08:37

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Published on: November 5, 2014

PDE4 inhibitors: current status.

D Spina1

  • 1King's College London School of Biomedical and Health Science, Pharmaceutical Science Research Division, Sackler Institute of Pulmonary Pharmacology, London, UK. domenico.spina@kcl.ac.uk

British Journal of Pharmacology
|July 29, 2008
PubMed
Summary
This summary is machine-generated.

Phosphodiesterase 4 (PDE4) inhibitors show promise for treating respiratory conditions like asthma. While effective, side effects necessitate developing improved treatments for better patient outcomes.

Related Experiment Videos

Last Updated: Jul 3, 2026

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
08:37

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Published on: November 5, 2014

Area of Science:

  • Pharmacology
  • Respiratory Medicine
  • Drug Development

Background:

  • Phosphodiesterase 4 (PDE4) inhibitors are investigated for respiratory diseases such as asthma and COPD.
  • PDE4's role in inflammatory and resident cells is key to understanding its therapeutic potential.
  • Preclinical studies demonstrate PDE4 inhibitors' ability to mitigate disease features like cell recruitment and lung function changes.

Purpose of the Study:

  • To review the development and clinical translation of PDE4 inhibitors for respiratory diseases.
  • To address the dose-limiting side effects hindering widespread clinical application.
  • To explore strategies for enhancing efficacy and reducing adverse effects of PDE4 inhibitors.

Main Methods:

  • Review of preclinical in vivo studies on PDE4 inhibitors in respiratory disease models.
  • Analysis of Phase II and III clinical trial data for PDE4 inhibitors like roflumilast and cilomilast.
  • Examination of ongoing strategies to improve PDE4 inhibitor therapy.

Main Results:

  • PDE4 inhibitors have shown efficacy in preclinical models and early clinical trials for asthma and COPD.
  • Clinical success has been tempered by dose-limiting side effects including nausea, diarrhea, and headache.
  • Development is ongoing to overcome these limitations.

Conclusions:

  • PDE4 inhibitors represent a viable therapeutic class for respiratory diseases, including asthma and COPD.
  • Strategies such as inhaled delivery and development of non-emetic or mixed PDE inhibitors are crucial for future success.
  • Further research aims to balance efficacy with improved tolerability for these agents.