• 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.

ST6GAL1 Drug Discovery to Combat Cancer

by Bellbrook Labs / Wednesday, 08 January 2020 / Published in Emerging Targets, HTS Assays
ST6GAL1 Drug Discovery

The number of cancer hallmarks has increased as the knowledge and understanding of the disease progress. As many of us already know, the basic characteristic is a mutation that causes uncontrollable cell growth causing a tumor. Cancer is truly a multi-step development that enables cells to survive, proliferate and metastasize. Other hallmarks of the disease include:1

  • sustaining proliferative signaling
  • evading growth suppressors
  • resisting cell death
  • enabling replicative immortality
  • inducing angiogenesis
  • activating invasion and metastasis
  • reprogramming of energy metabolism
  • evading immune destruction
  • tumor microenvironment
  • aberrant glycosylation including abnormal sialylation

Scientists have found an overabundance of sialyltransferases (STs) in cancers. This isn’t surprising as many of the necessary functions (cell-cell recognition, protein targeting, and cell adhesion) occurring in our bodies are carried out via sialylation. These same functions along with many others are negatively affected in cancer patients leading to tumor progression and metastasis.

Sialylation is a common reaction that is catalyzed by an ST enzyme with the goal of adding a sialic acid (monosaccharide) to a growing oligosaccharide forming a glycolipid or glycoprotein. There are multiple types of STs named based on the linkage and function. For example, Beta-galactoside alpha-2,6-sialyltransferase 1 (ST6Gal1) transfers a sialic acid from CMP-sialic acid to galactose-containing substrates.

ST6Gal1 Responsibility and Role in Cancer

ST6Gal1 overexpression has been observed in several types of cancers including lung, cervical, ovarian, pancreatic, breast and colon carcinoma. Additionally, it has been reported to promote cancer cell metastasis and inhibit cell death pathways; thereby, supporting cell survival and growth. Specifically, the elevated levels regulate FAS and AKT so that tumor cells are able to evade apoptosis. 1

Furthermore, ST6Gal1 is correlated with high tumor grade, metastasis, and reduced patient prognosis. 1,2  Increased levels of the glycosyltransferase have also been identified to allocate resistance to chemotherapeutic intervention. 2

ST6GAL1 Activity Assay 

Researchers have already started discovering ST6Gal1 inhibitors in order to combat cancer; however, there is much to learn and even more potential for drug discovery. The Transcreener® AMP²/GMP² Assay is capable of detecting ST6Gal1 activity through direct detection of CMP. The enzyme converts CMP-sialic acid to sialic acid in order to create a galactose-containing substrate, forming CMP as a product that can be measured by using a specific antibody labeled with a fluorophore. This advantageous method can assist in the drug discovery that so many cancer patients and their loved ones are waiting for.

References

  1. Garnham R, Scott E, Livermore K, Munkley J. ST6GAL1: A key player in cancer (Review). Oncol Lett. 2019:983-989. doi:10.3892/ol.2019.10458 https://www.ncbi.nlm.nih.gov/pubmed/31423157
  2. Montgomery AP, Skropeta D, Yu H. Transition state-based ST6Gal1 inhibitors: Mimicking the phosphodiester linkage with a triazole or carbamate through an enthalpy-entropy compensation. Sci Rep. 2017;7(1):1-11. doi:10.1038/s41598-017-14560-0 https://www.nature.com/articles/s41598-017-14560-0
Tagged under: Sialyltransferase Assay, ST6GAL1, Transcreener AMP/GMP Assay

What you can read next

Publication: HTS Assay for Rho GEFs
Scientist Using a GTPase Assay
Researchers Employ GTPase Assay to Investigate Rab Proteins
JAK1 Inhibitors for Autoimmune Disease
Battling Autoimmune Disorders Using JAK1 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