• 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® GDP GTPase Assay Kits
      • Transcreener® UDP² Glycosyltransferase Assay
      • Transcreener® EPIGEN SAH Methyltransferase 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
      • Methyltransferase Assay Kits
      • Ligase and Synthetase Assay Kits
      • Phosphodiesterase Assay Kits
    • HTS Assays by Target
      • AMPK Assay Kits
      • cGAS Assay Kits
      • CD39 Assay Kits
      • CD73 Assay Kits
      • ENPP1 Assay Kits
      • EZH2 Assay Kits
      • IKK-beta Assay Kits
      • JAK1 Assay Kits
      • JAK3 Assay Kits
      • TBK1 Assay Kits
    • Recombinant cGAS Enzyme
    • Assay Plates
    • Ordering Information
  • Services
    • Assay Development Services
    • Lead Discovery Services
    • GTPase Profiling Services
    • OAS1 Assay Services
  • Innate Immunity
    • cGAS Activity Assays
    • CD73 Activity Assays
    • CD39 Activity Assays
    • ENPP1 Activity Assays
    • IKK-beta Activity Assays
    • JAK1 Activity Assays
    • JAK3 Activity Assays
    • OAS1 Activity Assays
    • TBK1 Activity Assays
  • Resources
    • Application Notes
    • Transcreener® Assays – Instrument Compatibility
    • Posters and Presentations
    • Publications
    • Technical Manuals
    • Transcreener® FAQ’s
    • Guides
      • Residence Time Guide
      • Hit Prioritization Guide
  • 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

Measuring Dissociation Rates and Residence Times for Kinase Inhibitors using a Jump Dilution Protocol
Residence Time Guide
A Guide to Measuring Drug-Target Residence Times with Biochemical Assays
EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain

Categories

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

Recent Posts

  • SLAS 2021

    Join Us for SLAS 2021 Virtual Conference

    BellBrook Labs will be exhibiting at SLAS 2021,...
  • New cGAS TR-FRET Assay

    New TR-FRET Readout Now Available with the Transcreener cGAMP cGAS Assay

    Launched in November 2019, the Transcreener cGA...
  • Webinar Graphic

    Previously Recorded Webinar – Streamline cGAS Inhibitor Discovery with the Transcreener® cGAS Assay

    The immune system uses the recognition of forei...
  • Lab IRAK4 Inhibitors Kinase Assay Kit

    Uncovering IRAK4 Inhibitors with a Transcreener Kinase Assay Kit

    Genentech discovers IRAK4 inhibitors using the ...
  • Assay Development Services - Two Scientists Working In the Lab

    Five Considerations When Choosing a Biochemical Assay Development Services CRO

    There are many options out there for choosing a...

Archives

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

info@bellbrooklabs.com

 Copyright © 2019 BellBrook Labs | All Rights Reserved | Privacy Policy | Terms of Use | FCOI | Sitemap

TOP