• Assay Selection Tool

BellBrook Labs

  • Products
    • Transcreener® HTS Assays
      • Transcreener® ADP² Kinase Assay
      • Transcreener® ADO CD73 Assay
      • Transcreener® AMP²/GMP² Phosphodiesterase Assay
      • Transcreener® cGAMP cGAS Assay
      • Transcreener® EPIGEN SAH Methyltransferase Assay
      • Transcreener® GDP GTPase Assay Kits
      • Transcreener® UDP² Glycosyltransferase Assay
      • Transcreener® 2-5A OAS Assay
    • AptaFluor® HTS Assays
      • AptaFluor® SAH Methyltransferase Assay
    • HTS Assays by Target Family
      • Kinase Assay Kits
      • ATPase Assay Kits
      • Glycosyltransferase Assay Kits
      • GTPase Assay Kits
        • GAP Assay Kits
        • GEF Assay Kits
      • Ligase and Synthetase Assay Kits
      • Methyltransferase Assay Kits
      • Phosphodiesterase Assay Kits
    • HTS Assays by Target
      • Adenosine Kinase Assay Kits
      • AMPK Assay Kits
      • CD39 Assay Kits
      • CD73 Assay Kits
      • cGAS Assay Kits
      • DDX3 Assay Kits
      • ENPP1 Assay Kits
      • EZH2 Assay Kits
      • IKK-beta Assay Kits
      • IRAK4 Assay Kits
      • JAK1 Assay Kits
      • JAK3 Assay Kits
      • NSP13 Assay Kits
      • NUDT5 Assay Kits
      • OAS Assay Kits
      • TBK1 Assay Kits
    • Recombinant Enzymes
      • Human cGAS Enzyme
      • Mouse cGAS Enzyme
      • Human DDX3 Enzyme
      • Human OAS1 Enzyme
    • Assay Plates
    • Ordering Information
  • Services
    • Assay Development Services
    • Lead Discovery Services
    • CD38 Assay Services
    • GTPase Profiling Services
  • Innate Immunity
    • Adenosine Kinase Activity Assays
    • AMPK Activity Assays
    • cGAS Activity Assays
    • CD73 Activity Assays
    • CD38 Activity Assay Services
    • CD39 Activity Assays
    • DDX3 Activity Assays
    • ENPP1 Activity Assays
    • IKK-beta Activity Assays
    • IRAK4 Activity Assays
    • JAK1 Activity Assays
    • JAK3 Activity Assays
    • NSP13 Activity Assays
    • OAS1 Activity Assays
    • TBK1 Activity Assays
  • Resources
    • Technical Manuals
    • Transcreener® Assays – Instrument Compatibility
    • Application Notes
    • Posters and Presentations
    • Publications
    • Transcreener® FAQ’s
    • Guides
      • Residence Time Guide
      • Hit Prioritization Guide
      • Kinases in Innate Immunity
  • Company
    • President’s Message
    • International Distributors
    • Careers
    • Downloads
    • Contact Us
  • Blog
  • MY CART
    No products in cart.

How A PDE Activity Assay Might Help Find New Treatments for Individuals Suffering from Heart Disease

by Bellbrook Labs / Tuesday, 06 August 2019 / Published in HTS Assays
PDE Activity Assay Heart Disease

Heart Disease: The Role of PDEs and a PDE Activity Assay

Heart disease is often misunderstood due to confusion with terminology and the different types of heart disease that exist. While a heart attack can occur quickly, heart failure is a slower progression where the heart weakens over time.

One thing is certain; heart disease is the leading cause of death in the United States. 1 Although important; cholesterol levels, exercise, and eating habits are not the only thing we should be concerned with when it comes to heart disease. Anything that stresses the heart has the ability to weaken it.

Some factors are listed here:

  • Heart valve disease
  • Congenital heart defects
  • Infections
  • Irregular heartbeat
  • Cardiomyopathy
  • HIV/AIDS
  • Chemotherapy
  • Thyroid disease
  • Alcohol overuse
  • Lung disease

Targeting Phosphodiesterases in Heart Disease

On a cellular level, the heart muscle and its blood pumping function to keep us oxygenated and alive is extremely complex. At the regulation level, there are enzymes known as phosphodiesterases (PDEs) that degrade second messengers such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). These second messengers trigger many cell signaling functions within the body. Specifically, myocardial cells rely on these molecules for a variety of purposes including contraction and relaxation, diastolic stiffness, heart rate, cell growth and survival, interstitial fibrosis, vascular tone, and endothelial permeability and proliferation.2

There are a plethora of ways to treat heart disease. However, each strategy treats a particular symptom and/or cause. Targeting phosphodiesterases is one such strategy. Since PDE3 has been found to regulate cardiac pacemaking and contractility, it’s no surprise that inhibition of PDE3 leads to an increase in heart rate and cardiac contractile ability.3   In fact, there are drugs currently on the market that inhibit PDE3 to improve heart failure. Primacor and Inocor allow for an elevated cAMP pathway that ultimately leads to increased protein kinase A (PKA) activation which further allows for calcium channels to open; thereby increasing cardiac contractility.

How Can A PDE Activity Assay Help?

Even so, more research to understand heart disease on a molecular level, as well as the role of PDEs, is required. BellBrook Labs offers a PDE Activity Assay that can assist scientists in research and drug discovery targeting phosphodiesterases to treat heart disease. These assays can be used to measure enzymatic activity, screen compound libraries for inhibitors, determine inhibitor selectivity, measure inhibitor potency, and inhibitor residence time measurement.

References
  1. Control C for D. Centers for Disease Control: Know the Facts About Heart Disease. 2009:1-2. https://www.cdc.gov/heartdisease/facts.htm
  2. Kim, G. E., & Kass, D. A. (2017). Cardiac phosphodiesterases and their modulation for treating heart disease. In Handbook of Experimental Pharmacology (Vol. 243, pp. 249-269). (Handbook of Experimental Pharmacology; Vol. 243). Springer New York LLC. https://doi.org/10.1007/164_2016_82
  3. Walter Knight, Chen Yan. Manuscript A. Therapeutic potential of PDE modulation in treating heart disease.  2014;5(14):1607-1620. doi:10.4155/fmc.13.127. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4114345/
Tagged under: PDE Activity Assay, Phosphodiesterase Assay, Transcreener AMP/GMP Assay

What you can read next

B4GalT1 A Target to Stop Glioblastoma
B4GalT1 – A Druggable Target for the Treatment of Glioblastoma
Measuring Dissociation Rates and Residence Times for Kinase Inhibitors using a Jump Dilution Protocol
HSP90 Inhibitor Immunotherapy
Enhancing Checkpoint Blockade Immunotherapy: Sensitizing Tumors with HSP90 Inhibitors

Categories

  • Company
  • Emerging Targets
  • Epigenetics
  • HTS Assays
  • Innate Immunity
  • Neurodegenerative Diseases
  • News
  • Products
  • Resources
  • Success Stories
  • Uncategorized

Recent Posts

  • Scientist Studying ALKPK1

    The Role ALPK1 in Health and Disease

    ALPK1 (Alpha Kinase 1) is an atypical serine/th...
  • DHX36 RNA Helicase Unwinds G4 RNA Structures

    Resolving the Many Roles of DHX36

    While most researchers are familiar with canoni...
  • Researcher Studying MAPK14

    MAPK14 in Context

    MAPK14 (or p38 alpha or SAPK2a) is a proline-di...
  • PRMT5 Role with Macrophages

    PRMT5 is Innately Interesting

    PRMT5 is a type II arginine methyltransferase t...
  • IRE1 Proteins in ER

    The Multifaceted Roles of IRE1 Are Unfolding

    IRE1 (Inositol-Requiring Enzyme 1) is one of th...

Archives

BellBrook Labs
5500 Nobel Drive, Suite 230
Madison, Wisconsin 53711 USA
(608) 443-2400

info@bellbrooklabs.com

 Copyright © 2021 BellBrook Labs | All Rights Reserved | Privacy Policy | Terms of Use | FCOI | Sitemap

TOP